Antibody ID	ANI0FIZAK
Antibody Name	Trastuzumab
Brand Name	HERCEPTIN
Organization	Genentech, Inc.; Roche Holding AG; Roche, F. Hoffmann-La Roche Ltd.
Indication	Gastric cancer; Breast cancer; Colorectal cancer
Approval Date	Sep. 1998
Synonyms	4D5V8; ABP980; ABP 980; ABP-980; ABP-980 (TRASTUZUMAB BIOSIMILAR); BMAB-200; CANHERA; DMB-3111; DMB-3111 (TRASTUZUMAB BIOSIMILAR); EG12014; EG-12014; EG-12014 (TRASTUZUMAB BIOSIMILAR); EG12014 TRASTUZUMAB BIOSIMILAR; HERZUMA; HLX02; HLX 02; HLX-02; HLX-02 TRASTUZUMAB BIOSIMILAR; KANJINTI; OGIVRI; ONTRUZANT; PF-05280014; R-597; RHUMAB HER2; RO0452317; RO-0452317; SB-3 (TRASTUZUMAB BIOSIMILAR); SYD977; SYD-977; TRASTUZUMAB; TRASTUZUMAB ANNS; TRASTUZUMAB-ANNS; TRASTUZUMAB BETA; TRASTUZUMAB BIOSIMILAR (ABP-980); TRASTUZUMAB DKST; TRASTUZUMAB-DKST; TRASTUZUMAB DTTB; TRASTUZUMAB-DTTB; TRASTUZUMAB (HERCEPTIN); TRASTUZUMAB-PFIZER; TRASTUZUMAB PKRB; TRASTUZUMAB-PKRB; TRASTUZUMAB QYYP; TRASTUZUMAB-QYYP; TRASTUZUMAB-ZZXF; TRAZIMERA; ZERCEPAC    Click to Show/Hide
Antibody Type	Monoclonal antibody (mAb)
Antibody Subtype	Humanized IgG1-kappa
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)					Antigen Info
ChEMBI ID	CHEMBL1201585
PDB ID	1fvc , 1n8z , 4hkz , 5xhg , 6bhz , 6bi0 , 6bi2 , 6mh2 , 6oge
DrugBank ID	DB00072
Drug Central ID	4979
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence	EVQLVESGGGLVQPGGSLRLSCAASGFNIKDTYIHWVRQAPGKGLEWVARIYPTNGYTRY ADSVKGRFTISADTSKNTAYLQMNSLRAEDTAVYYCSRWGGDGFYAMDYWGQGTLVTVSS ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGG PSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYN STYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREE MTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRW QQGNVFSCSVMHEALHNHYTQKSLSLSPGK     Click to Show/Hide
Heavy Chain Varible Domain	EVQLVESGGGLVQPGGSLRLSCAASGFNIKDTYIHWVRQAPGKGLEWVARIYPTNGYTRY ADSVKGRFTISADTSKNTAYLQMNSLRAEDTAVYYCSRWGGDGFYAMDYWGQGTLVTVSS     Click to Show/Hide
Heavy Chain Constant Domain 1	ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKV     Click to Show/Hide
Heavy Chain Constant Domain 2	APELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTK PREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAK     Click to Show/Hide
Heavy Chain Constant Domain 3	GQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDS DGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK     Click to Show/Hide
Heavy Chain Hinge Region	EPKSCDKTHTCPPCP     Click to Show/Hide
Heavy Chain CDR 1	GFNIKDTY     Click to Show/Hide
Heavy Chain CDR 2	IYPTNGYT     Click to Show/Hide
Heavy Chain CDR 3	SRWGGDGFYAMDY     Click to Show/Hide
Light Chain Sequence	DIQMTQSPSSLSASVGDRVTITCRASQDVNTAVAWYQQKPGKAPKLLIYSASFLYSGVPS RFSGSRSGTDFTLTISSLQPEDFATYYCQQHYTTPPTFGQGTKVEIKRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC     Click to Show/Hide
Light Chain Varible Domain	DIQMTQSPSSLSASVGDRVTITCRASQDVNTAVAWYQQKPGKAPKLLIYSASFLYSGVPS RFSGSRSGTDFTLTISSLQPEDFATYYCQQHYTTPPTFGQGTKVEIK     Click to Show/Hide
Light Chain Constant Domain	RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQD SKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC     Click to Show/Hide
Light Chain CDR 1	QDVNTA     Click to Show/Hide
Light Chain CDR 2	SAS     Click to Show/Hide
Light Chain CDR 3	QQHYTTPPT     Click to Show/Hide

Antibody Activity Information 1						[1]
Half Maximal Effective Concentration (EC50)	1.35	nM
Antibody Function	Confirm the effect of the drug conjugation with the anti-HER2 (Trastuzumab) Ab on binding activity to HER2.
Antibody Antigen Binding Assay	Evaluate the antigen binding capacity of our ADC by indirect ELISA binding assay.

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.025 nM
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.052 nM
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.513 nM
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Objective Response Rate (ORR)	66.70 42.90 %
Patients Enrolled	Patients with HER2-expresssing advanced solid tumors who had failed prior standard of care therapies.
Administration Dosage	FS-1502 was given IV once in 21-day or 28-day cycle at doses of 0.10-3.50 mg/kg.

Experiment 1 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Objective Response Rate (ORR)	38.20%
Patients Enrolled	Eligible patients must have advanced/metastatic gastric/GEJ adenocarcinoma or colorectal cancer (refractory to standard therapy) with ≥1 measurable lesion (RECIST 1.1), ECOG 0-1, life expectancy ≥3 months, and adequate organ function. Exclusions: unresolved Grade >1 toxicities, prior HER2-ADC exposure, symptomatic CNS/meningeal metastases, or active infections requiring systemic treatment.    Click to Show/Hide
Administration Dosage	There are six pre-defined dose regimens . Subjects will be enrolled with an initial dose
Related Clinical Trial
NCT Number	NCT04513223	Clinical Status	PHASE1
Clinical Description	Safety, Tolerability, Pharmacokinetics, and Antitumour Activity of SHR-A1811, in Patients With HER2-expressing Advanced Gastric or Gastroesophageal Junction Adenocarcinoma and Colorectal Cancer: a Phase 1 Study
Primary Endpoint	The primary endpoints include assessment of dose-limiting toxicities (DLT) and determination of the recommended Phase 2 dose (RP2D) during the first treatment cycle (Days 1-21).
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Objective Response Rate (ORR)	41.90%
Patients Enrolled	Eligible patients (ECOG 0-1, HER2-altered advanced NSCLC post-platinum failure) require ≥1 measurable lesion (RECIST v1.1). Key exclusions: unresolved Grade >1 toxicity (CTCAE v5.0), prior HER2 ADC treatment, symptomatic CNS/meningeal metastases, or active systemic infection.
Administration Dosage	SHR-A1811 was administered intravenously every 3 weeks (Q3W) until discontinuation treatment
Related Clinical Trial
NCT Number	NCT04818333	Clinical Status	PHASE1|||PHASE2
Clinical Description	Phase I/II Clinical Study of the Safety, Tolerability, Pharmacokinetics, and Efficacy of SHR-A1811 for Injection in Subjects With Advanced Non-small Cell Lung Cancer Who Have HER2 Expression , Amplification, or Mutation
Primary Endpoint	Phase 1 evaluates safety/tolerability of SHR-A1811 through incidence/severity of AEs (CTCAE v5.0; monitored Day1-90 post-last dose, ~3 years), MTD determination (DLTs in first 21-day cycle), and RP2D selection (based on safety/PK/efficacy over 12 months). Phase 2 primary endpoint is ORR (RECIST v1.1, IRC-assessed, tumor imaging q6w→q12w post-54w until progression/new therapy/death, ~3 years).    Click to Show/Hide
Other Endpoint	Phase 1 PK analysis includes Tmax, Cmax, AUC0-t (~3 years); immunogenicity (ADA/NAb assessed pre-dose C1D1-C8D1→q3 cycles). Phase 2 secondary endpoints: IRC/investigator-assessed PFS, ORR, DOR, DCR (RECIST v1.1, ~3 years); OS (~5 years post-last enrollment).
Experiment 3 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Objective Response Rate (ORR)	45.90%
Patients Enrolled	Eligible patients must have HER2-positive advanced/metastatic solid tumors refractory to standard therapy, ECOG 0-1, LVEF ≥ 50%, and adequate organ function. Exclusions include significant lung disease, bleeding/thrombotic disorders, and pregnancy or lactation during the study.
Administration Dosage	Patients (pts) with advanced, unresectable, or metastatic HER2-expressing/mutated STs that were refractory or intolerant to standard therapies were treated with SHR-A1811 at 1.0-8.0 mg/kg Q3W (IV).
Related Clinical Trial
NCT Number	NCT04446260	Clinical Status	PHASE1
Clinical Description	A Phase 1 Multi-Country, Multi-Center, Open-Label Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Efficacy of SHR-A1811 in HER2 Expressing or Mutated Advanced Malignant Solid Tumor Subjects
Primary Endpoint	The study monitors the incidence and severity of adverse events (AEs) from Day 1 to 90 days after the last dose, including frequency and seriousness of treatment-emergent adverse events (TEAEs).
Other Endpoint	Pharmacokinetic (PK) parameters such as Tmax, Cmax, and AUC0-t of SHR-A1811 are evaluated over an average of 1 year. Immunogenicity assessments include anti-drug antibodies and neutralizing antibodies. Tumor response is measured per RECIST 1.1 until progression or death, up to 30 months.
Experiment 4 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Objective Response Rate (ORR)	56.1 50 63.6 %
Patients Enrolled	Eligible participants (signed ICF, ECOG 0-1, life expectancy ≥12 weeks) must have measurable advanced/recurrent cervical, ovarian, or endometrial cancer. Exclusions: untreated CNS metastases, prior topoisomerase I inhibitor ADC treatment (e.g., DS-8201a), uncontrolled cardiovascular disease, active autoimmune/HBV/HCV infections, recent severe infections (28 days), or active tuberculosis (1 year).    Click to Show/Hide
Administration Dosage	Pts received SHR-A1811 at 4.8 or 6.4 mg/kg (Q3W, IV). The primary endpoint was ORR per RECIST v1.1.
Related Clinical Trial
NCT Number	NCT05896020	Clinical Status	PHASE2
Clinical Description	Open, Multicenter Phase II Clinical Study of SHR-A1811 for Injection in the Treatment of Gynaecological Malignancies
Primary Endpoint	The primary endpoint is objective response rate (ORR) assessed over a 12-month timeframe as per RECIST v1.1 criteria.
Other Endpoint	Secondary endpoints include progression-free survival (PFS), disease control rate (DCR), duration of response (DOR), overall survival (OS) (all 12-month assessment), and incidence/severity of adverse events (AEs) tracked from Day 1 to 90 days post-last dose.
Experiment 5 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Objective Response Rate (ORR)	66.70%
Patients Enrolled	Eligible patients (women 18-75 years, ECOG 0-1) require histologically confirmed HER2+ breast cancer, measurable lesions (RECIST v1.1), and adequate organ function. Key exclusions: active CNS metastases (unless treated), uncontrolled effusions, recent antitumor therapy (≤4 weeks), autoimmune/cardiovascular diseases, or unresolved toxicity (>CTCAE Gr1). Hepatitis B/C carriers with viral loads >2000 IU/mL or cirrhosis are excluded.    Click to Show/Hide
Administration Dosage	SHR-A1811:Lyophilized powder injection, 100mg / bottle, intravenous drip
Related Clinical Trial
NCT Number	NCT05353361	Clinical Status	PHASE2
Clinical Description	A Phase Ib/II Multicenter, Open-Label Clinical Trial of SHR-A1811 Injection in Combination With Pyrotinib or Pertuzumab or Adebrelimab or Paclitaxel for Injection (Albumin Bound) in Breast Cancer
Primary Endpoint	The Phase I dose-escalation trial evaluates SHR-A1811 safety (DLTs in first 21 days; AEs/SAEs monitored until 40-90 days post-treatment). Phase II assesses ORR (primary endpoint) in HER2+ breast cancer patients at 2 years post-enrollment, with tumor response per RECIST v1.1.
Other Endpoint	Pharmacokinetics (Cmin/Cmax/AUC of SHR-A1811, pyrotinib, and adebrelimab) and immunogenicity (anti-drug antibodies) are secondary endpoints in both phases (tracked for ~2 years). Efficacy metrics include ORR, DoR, PFS (up to 3 years), and Phase II's event-free survival rate (EFSR). Safety monitoring extends to 90 days post-treatment.
Experiment 6 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Objective Response Rate (ORR)	81.50%
Patients Enrolled	Eligible patients aged 18-70 have untreated T2-T3/N0-3/M0, HR+/HER2-low (Ki-67 >14%) invasive breast cancer (ECOG 0-1) and normal organ function. Exclusions: metastatic/inflammatory disease, prior anticancer therapy (excluding cured non-breast malignancies), recent major surgery, severe comorbidities (cardiopulmonary/immunodeficiency), drug allergies, or conditions impairing treatment adherence. WOCBP must use contraception.    Click to Show/Hide
Administration Dosage	SHR-A1811 is administered intravenously at a dose of 6.4 mg/kg once every three weeks for a total of eight cycles.
Related Clinical Trial
NCT Number	NCT05911958	Clinical Status	PHASE2
Clinical Description	Phase II Study of SHR-A1811 as Neoadjuvant Treatment for Patients With HR-Positive, Low HER2 Expression Breast Cancer
Primary Endpoint	The study evaluates ORR per RECIST v1.1 during 24 weeks of neoadjuvant treatment and assesses safety via AE incidence/severity (CTCAE 5.0) from consent through 28 days post-last dose.
Other Endpoint	Key endpoints include residual cancer burden (RCB) and pathological complete response (pCR: ypT0/is ypN0) at surgery, with long-term outcomes tracked over 5 years (EFS from randomization; DFS from surgery) for recurrence/metastasis/death events.
Experiment 7 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Objective Response Rate (ORR)	84.4 72.7 %
Patients Enrolled	Eligible participants are females ≥18 with HER2+/HER2-low advanced breast cancer and measurable untreated intracranial lesions (RANO-BM). Key criteria: no prior cranial radiation/local therapy (unless post-surgery, unirradiated), ≥2 weeks since last systemic treatment, life expectancy ≥6 months, and adequate organ function. Exclusions: leptomeningeal disease, urgent CNS intervention needed, prior DS-8201a/exatecan-ADC use, recent antitumor therapy (≤2 weeks for most, ≤1 week for endocrine), other malignancies (except cured CIS/skin cancers), or uncontrolled comorbidities per investigator judgement.    Click to Show/Hide
Administration Dosage	Between March 31, 2023, and November 3, 2023, 25 patients with HER2+ BCBM were enrolled in Arm 1, and they received SHR-A1811 at a dosage of 6.4mg/kg q3w.
Related Clinical Trial
NCT Number	NCT05769010	Clinical Status	PHASE2
Clinical Description	A Prospective, Open-label Explorative Study of SHR-A1811 in HER2-expression Advanced Breast Cancer with Brain Metastases
Primary Endpoint	The primary endpoint is CNS-ORR, assessed by investigators per RANO-BM criteria at 2 months, defined as the percentage of participants achieving CNS response.
Other Endpoint	Secondary endpoints include ORR (CR/PR per RECIST 1.1 at 2 months), PFS (time to progression/death up to 1.5 years), and safety (adverse events incidence over 1.5 years).
Experiment 8 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Objective Response Rate (ORR)	85.7 30 %
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1, life expectancy &ge;12 weeks) must have histologically confirmed locally advanced/metastatic salivary gland carcinoma: Arm 1 (HER2-altered), Arm 2 (AR-positive), Arm 3 (HER2/AR-negative), or Arm 4 (low HER2 expression), with &ge;1 measurable lesion (RECIST v1.1). Key exclusions: active malignancies (5 years), recent antitumor therapy (28 days prior, or <5 half-lives), uncontrolled cardiac conditions (NYHA &ge;II, LVEF <50%, QTc >450ms&male;/470ms&female;), uncontrolled hypertension, gastrointestinal absorption issues (Arm 2), bleeding risks, or abnormal coagulation (INR/aPTT >1.5&times;ULN). Organ function thresholds: HB &ge;90g/L, ANC &ge;1.5&times;10<sup>9</sup>/L, PLT &ge;80&times;10<sup>9</sup>/L, bilirubin &le;1.5&times;ULN, ALT/AST &le;2.5&times;ULN (&le;5&times;ULN if liver mets), Cr &le;1&times;ULN.    Click to Show/Hide
Administration Dosage	Patients with advanced SGC were stratified into four arms based on genetic subtypes. This analysis focuses on Arm 1 (HER2 overexpression: IHC 3+ or IHC 2+/ISH+) and Arm 4 (HER2-low: IHC 1+ or IHC 2+/ISH-). In Arm 1, patients received SHR-A1811 at 4.8 mg/kg IV on Day 1 of a 21-day cycle. In Arm 4, patients received 4.8 mg/kg or 5.6 mg/kg (if tolerated).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05924256	Clinical Status	PHASE2
Clinical Description	A Phase II Study of Advanced Salivary Gland Carcinoma Based on Molecular Typing
Primary Endpoint	The primary endpoint is objective response rate (ORR) assessed every 2 cycles (21-day cycles for Arms 1/3/4, 28-day for Arm 2) per RECIST 1.0 criteria (confirmed CR/PR).
Other Endpoint	Key secondary endpoints include disease control rate (DCR: CR/PR/SD per RECIST 1.0, same assessment schedule), progression-free survival (PFS: time to progression/death, RECIST v1.1, up to 2 years), overall survival (OS: time to death, up to 2 years), and adverse events (hematologic/non-hematologic per CTCAE 5.0, monitored from consent to 30 days post-last cycle).    Click to Show/Hide
Experiment 9 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Objective Response Rate (ORR)	89.70%
Patients Enrolled	Eligible patients (females aged 18-75) have treatment-naive HER2+ stage II-III breast cancer (ECOG 0-1). Exclusions: prior antitumor therapy, bilateral/Stage IV disease, malignancies in 5 years (exceptions: cured CIS/skin cancer), drug absorption issues, recent trial participation, significant organ dysfunction (cardiac/pulmonary/liver), or drug allergies.    Click to Show/Hide
Administration Dosage	Eligible women aged 18-75 with newly diagnosed stage II-III, untreated HER2+ BC received SHR-A1811 Q3W and daily pyrotinib for six cycles. Initial treatment was SHR-A1811 at 4.8 mg/kg and pyrotinib at 240 mg/day (Cohort A). Dose adjustments followed the 3+3 principle: If tolerated, SHR-A1811 could escalate to 5.6 mg/kg, maintaining pyrotinib (Cohort B). For intolerance or investigator discretion, adjustments included SHR-A1811 at 4.8 mg/kg with pyrotinib at 160 mg/day (Cohort C), or SHR-A1811 at 4.0 mg/kg with pyrotinib at 240 mg/day (Cohort D).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05635487	Clinical Status	PHASE2
Clinical Description	A Phase II Study of SHR-A1811 Monotherapy or Combined With Pyrotinib Maleate as Neoadjuvant Treatment in HER2-positive Breast Cancer Patients
Primary Endpoint	The primary endpoint is total pathological complete response (tpCR: ypT0-is/ypN0), evaluated at surgery following neoadjuvant therapy.
Other Endpoint	Secondary endpoints include breast pCR (bpCR: ypT0-is), RCB, BORR during neoadjuvant treatment (18 weeks), OS/DFS/EFS (5-year follow-up), and HRQOL (assessed via EORTC QLQ-C30 and QLQ-BR23).
Experiment 10 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Disease control rate (DCR)	83.60%
Patients Enrolled	Eligible patients must have advanced/metastatic gastric/GEJ adenocarcinoma or colorectal cancer (refractory to standard therapy) with &ge;1 measurable lesion (RECIST 1.1), ECOG 0-1, life expectancy &ge;3 months, and adequate organ function. Exclusions: unresolved Grade >1 toxicities, prior HER2-ADC exposure, symptomatic CNS/meningeal metastases, or active infections requiring systemic treatment.    Click to Show/Hide
Administration Dosage	There are six pre-defined dose regimens . Subjects will be enrolled with an initial dose
Related Clinical Trial
NCT Number	NCT04513223	Clinical Status	PHASE1
Clinical Description	Safety, Tolerability, Pharmacokinetics, and Antitumour Activity of SHR-A1811, in Patients With HER2-expressing Advanced Gastric or Gastroesophageal Junction Adenocarcinoma and Colorectal Cancer: a Phase 1 Study
Primary Endpoint	The primary endpoints include assessment of dose-limiting toxicities (DLT) and determination of the recommended Phase 2 dose (RP2D) during the first treatment cycle (Days 1-21).
Experiment 11 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Disease control rate (DCR)	88.20%
Patients Enrolled	Eligible patients must have HER2-positive advanced/metastatic solid tumors refractory to standard therapy, ECOG 0-1, LVEF &ge; 50%, and adequate organ function. Exclusions include significant lung disease, bleeding/thrombotic disorders, and pregnancy or lactation during the study.
Administration Dosage	Patients (pts) with advanced, unresectable, or metastatic HER2-expressing/mutated STs that were refractory or intolerant to standard therapies were treated with SHR-A1811 at 1.0-8.0 mg/kg Q3W (IV).
Related Clinical Trial
NCT Number	NCT04446260	Clinical Status	PHASE1
Clinical Description	A Phase 1 Multi-Country, Multi-Center, Open-Label Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Efficacy of SHR-A1811 in HER2 Expressing or Mutated Advanced Malignant Solid Tumor Subjects
Primary Endpoint	The study monitors the incidence and severity of adverse events (AEs) from Day 1 to 90 days after the last dose, including frequency and seriousness of treatment-emergent adverse events (TEAEs).
Other Endpoint	Pharmacokinetic (PK) parameters such as Tmax, Cmax, and AUC0-t of SHR-A1811 are evaluated over an average of 1 year. Immunogenicity assessments include anti-drug antibodies and neutralizing antibodies. Tumor response is measured per RECIST 1.1 until progression or death, up to 30 months.
Experiment 12 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Disease control rate (DCR)	95.30%
Patients Enrolled	Eligible patients (ECOG 0-1, HER2-altered advanced NSCLC post-platinum failure) require &ge;1 measurable lesion (RECIST v1.1). Key exclusions: unresolved Grade >1 toxicity (CTCAE v5.0), prior HER2 ADC treatment, symptomatic CNS/meningeal metastases, or active systemic infection.
Administration Dosage	SHR-A1811 was administered intravenously every 3 weeks (Q3W) until discontinuation treatment
Related Clinical Trial
NCT Number	NCT04818333	Clinical Status	PHASE1|||PHASE2
Clinical Description	Phase I/II Clinical Study of the Safety, Tolerability, Pharmacokinetics, and Efficacy of SHR-A1811 for Injection in Subjects With Advanced Non-small Cell Lung Cancer Who Have HER2 Expression , Amplification, or Mutation
Primary Endpoint	Phase 1 evaluates safety/tolerability of SHR-A1811 through incidence/severity of AEs (CTCAE v5.0; monitored Day1-90 post-last dose, ~3 years), MTD determination (DLTs in first 21-day cycle), and RP2D selection (based on safety/PK/efficacy over 12 months). Phase 2 primary endpoint is ORR (RECIST v1.1, IRC-assessed, tumor imaging q6w→q12w post-54w until progression/new therapy/death, ~3 years).    Click to Show/Hide
Other Endpoint	Phase 1 PK analysis includes Tmax, Cmax, AUC0-t (~3 years); immunogenicity (ADA/NAb assessed pre-dose C1D1-C8D1→q3 cycles). Phase 2 secondary endpoints: IRC/investigator-assessed PFS, ORR, DOR, DCR (RECIST v1.1, ~3 years); OS (~5 years post-last enrollment).
Experiment 13 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Disease control rate (DCR)	100%
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1, life expectancy &ge;12 weeks) must have histologically confirmed locally advanced/metastatic salivary gland carcinoma: Arm 1 (HER2-altered), Arm 2 (AR-positive), Arm 3 (HER2/AR-negative), or Arm 4 (low HER2 expression), with &ge;1 measurable lesion (RECIST v1.1). Key exclusions: active malignancies (5 years), recent antitumor therapy (28 days prior, or <5 half-lives), uncontrolled cardiac conditions (NYHA &ge;II, LVEF <50%, QTc >450ms&male;/470ms&female;), uncontrolled hypertension, gastrointestinal absorption issues (Arm 2), bleeding risks, or abnormal coagulation (INR/aPTT >1.5&times;ULN). Organ function thresholds: HB &ge;90g/L, ANC &ge;1.5&times;10<sup>9</sup>/L, PLT &ge;80&times;10<sup>9</sup>/L, bilirubin &le;1.5&times;ULN, ALT/AST &le;2.5&times;ULN (&le;5&times;ULN if liver mets), Cr &le;1&times;ULN.    Click to Show/Hide
Administration Dosage	Patients with advanced SGC were stratified into four arms based on genetic subtypes. This analysis focuses on Arm 1 (HER2 overexpression: IHC 3+ or IHC 2+/ISH+) and Arm 4 (HER2-low: IHC 1+ or IHC 2+/ISH-). In Arm 1, patients received SHR-A1811 at 4.8 mg/kg IV on Day 1 of a 21-day cycle. In Arm 4, patients received 4.8 mg/kg or 5.6 mg/kg (if tolerated).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05924256	Clinical Status	PHASE2
Clinical Description	A Phase II Study of Advanced Salivary Gland Carcinoma Based on Molecular Typing
Primary Endpoint	The primary endpoint is objective response rate (ORR) assessed every 2 cycles (21-day cycles for Arms 1/3/4, 28-day for Arm 2) per RECIST 1.0 criteria (confirmed CR/PR).
Other Endpoint	Key secondary endpoints include disease control rate (DCR: CR/PR/SD per RECIST 1.0, same assessment schedule), progression-free survival (PFS: time to progression/death, RECIST v1.1, up to 2 years), overall survival (OS: time to death, up to 2 years), and adverse events (hematologic/non-hematologic per CTCAE 5.0, monitored from consent to 30 days post-last cycle).    Click to Show/Hide
Experiment 14 Reporting the Activity Date of This ADC					[15]
Patients Enrolled	Exclusion criteria include prior chemotherapy/radiotherapy, NYHA class II+ heart disease, severe infections, drug allergies, other malignancies (except cervical/non-melanoma skin cancer) in the past 5 years, pregnancy/lactation without contraception, participation in other trials within 30 days, or investigator-deemed unsuitability.
Administration Dosage	SHR-A1811 was administered at a dose of 4.8 mg/kg intravenously (i.v.) every 3 weeks for eight cycles with or without an irreversible dual pan-ErbB receptor TKI, pyrotinib 240 mg orally once daily.
Related Clinical Trial
NCT Number	NCT05582499	Clinical Status	PHASE2
Clinical Description	Fudan University Shanghai Cancer Center Breast Cancer Precision Platform Series Study- Neoadjuvant Therapy (FASCINATE-N)
Primary Endpoint	This study evaluates the pathological complete response rate (pCR) as the primary endpoint within 24 weeks, while secondary endpoints include three-year invasive disease-free survival (iDFS), overall response rate (ORR), adverse effects using CTCAE v4.0, gene expression profiling via RNA-seq, and peripheral blood mononuclear cell (PBMC) counts measured by flow cytometry throughout the treatment period.    Click to Show/Hide
Other Endpoint	Eligible participants must have histologically confirmed stage II-III invasive breast cancer (T2N0-1/T3N0 for stage II; T2N2/T3N1-2 for stage III), aged 18-70, ECOG 0-1, with confirmed ER/PR/HER2 status, LVEF ≥55%, and proper subtyping (SNF or triple-negative based on AR/CD8/FOXC1). Acceptable organ function is required (HB≥90g/L, ANC≥1500/uL, platelets≥75K/uL, bilirubin≤1.5xULN, AST/ALT≤3xULN, creatinine clearance>50mL/min). Fertile women must use contraceptives during and 3 months post-study.    Click to Show/Hide
Experiment 15 Reporting the Activity Date of This ADC					[16]
Patients Enrolled	Eligible patients must have unresectable/metastatic HER2+ breast cancer (prior trastuzumab + taxane treatment), ECOG 0-1, measurable disease (RECIST v1.1), and adequate organ function. Exclusions: uncontrolled effusions, recent antitumor therapy (&le;4 weeks for chemo/immunotherapy, &le;2 weeks for endocrine), active autoimmune/cardiac disease (NYHA &ge;II), HIV/HBV/HCV infection, unresolved toxicity (>CTCAE Gr1), or severe allergies to monoclonal antibodies. WOCBP must use contraception for 7 months post-treatment.    Click to Show/Hide
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NCT Number	NCT05424835	Clinical Status	PHASE3
Clinical Description	A Phase III, Multicenter, Randomized, Open-Label, Parallel Controlled Study of SHR-A1811 Versus Pyrotinib in Combination With Capecitabine for HER2-Positive, Unresectable and/or Metastatic Breast Cancer Subjects Previously Treated With Trastuzumab and Taxane
Primary Endpoint	The primary endpoint is PFS (assessed by BIRC) evaluated from 6 weeks post-first dose until disease progression or death (approximately 2 years) in HER2+ metastatic breast cancer patients.
Experiment 16 Reporting the Activity Date of This ADC					[17]
Patients Enrolled	Inclusion requires HER2-low BC patients (18-75y, ECOG 0-1) with measurable lesions and adequate organ function. Key exclusions: active CNS metastases, uncontrolled effusions, recent major surgery, ILD/pneumonitis, significant comorbidities, unresolved prior toxicity (>CTCAE Gr1), or recent malignancies (exceptions: skin/CIS/thyroid cancers).
Administration Dosage	SHR-A1811:Lyophilized powder injection, 100mg / bottle, intravenous drip
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NCT Number	NCT05792410	Clinical Status	PHASE1|||PHASE2
Clinical Description	An Open, Multicenter Phase Ib/II Clinical Study of SHR-A1811 Combined With Dalpiciclib, Fulvestrant, Bevacizumab or Letrozole/Anastrozole in Patients With HER2 Low Advanced or Metastatic Breast Cancer.
Primary Endpoint	The primary endpoints for Phase I include DLT assessment (cycle 1: 28d for SHR-A1811+fulvestrant, 21d for other combos), AE incidence/severity, and ORR evaluation during efficacy expansion, with follow-up up to 24 months.
Other Endpoint	Secondary measures comprise SHR-A1811/dalpiciclib PK profiles, ADA/NAb detection rates, DoR, and PFS, all monitored over 24 months. Safety and immunogenicity data span from treatment initiation through study completion.
Experiment 17 Reporting the Activity Date of This ADC					[18]
Patients Enrolled	Eligible patients have HR+/HER2-low (IHC 1+ or 2+/ISH-) metastatic breast cancer with 0-1 prior chemotherapy lines in the metastatic setting, measurable lesions, and adequate organ function. Key exclusions: active CNS metastases (unless stable treated), HIV/autoimmune disease, ILD/pneumonitis history, significant CVD, active HBV/HCV infection, or prior malignancies (except low-risk) within 5 years.    Click to Show/Hide
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NCT Number	NCT05814354	Clinical Status	PHASE3
Clinical Description	A Randomized, Open, Parallel-controlled, Multicenter Phase III Trial of SHR-A1811 Versus Investigator Chemotherapy in HER2-low Expressing Recurrent/Metastatic Breast Cancer
Primary Endpoint	The primary endpoint is PFS assessed by BIRC within approximately 2 years of follow-up.
Other Endpoint	Secondary endpoints include OS (time to death up to 3 years), ORR (CR/PR rate within ~2 years), DoR (response duration until progression/death), and CBR (CR/PR/SD rate per RECIST 1.1 over ~2 years).
Experiment 18 Reporting the Activity Date of This ADC					[19]
Patients Enrolled	Eligible patients have ECOG 0-1, HER2 IHC 0 advanced/metastatic breast cancer (never HER2+), measurable lesions (RECIST 1.1), and progression after &ge;1 chemotherapy line (HR+ tumors require prior endocrine therapy). Exclusions: prior anti-HER2 therapy, recent treatments (surgery/RT/systemic therapies within 4w; endocrine therapy within 2w), active CNS metastasis, immunosuppression (>10mg/day prednisone), uncontrolled comorbidities, HIV/HBV/HCV infection, or other malignancies (except cured skin/CIS) within 5 years.    Click to Show/Hide
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NCT Number	NCT05824325	Clinical Status	PHASE1|||PHASE2
Clinical Description	Different Targeted Antibody-drug Conjugates for HER2 Ultra-low or no Expression Advanced Breast Cancer: a Phase Ib/II Study(GALAXY)
Primary Endpoint	Phase 1 focuses on AE incidence (graded per CTCAE v5.0) over 24 months, while Phase 2 evaluates ORR (CR/PR rate per RECIST 1.1 by investigator) until progression (~24 months).
Other Endpoint	Secondary endpoints include investigator-assessed PFS/OS (time to progression/death), DoR/DCR (response duration and control rate), CBR (CR/PR/SD≥24w), safety (AEs graded per CTCAE v5.0), and exploratory HER2-PET analysis, all monitored over 24 months.
Experiment 19 Reporting the Activity Date of This ADC					[20]
Patients Enrolled	Eligible are women aged 18-75 with HER2-low metastatic breast cancer (ECOG 0-1), measurable lesions, and &ge;12-week life expectancy. Exclusions: recent treatments/procedures (within 4 weeks), other cancers (last 5 years), significant comorbidities (cardiac/hepatic diseases), drug allergies, or conditions affecting absorption. WOCBP must use contraception.    Click to Show/Hide
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NCT Number	NCT05845138	Clinical Status	PHASE1|||PHASE2
Clinical Description	An Open-Label, Multi-center Phase Ib/II Study of SHR-A1811 Combined With Capecitabine in Treatment of Unresectable or Metastatic Breast Cancer With Low HER2 Expression.
Primary Endpoint	The Phase I dose exploration focuses on DLT assessment within 21 days of first dose and tracks AE/SAE incidence from Day 1 to 40 days post-last dose, while Phase II evaluates ORR one year post-final enrollment.
Other Endpoint	Efficacy measures include DoR and PFS (assessed one year post-final enrollment), with Phase I also monitoring ORR during this period. Both phases document AE/SAE incidence from Day 1 to 40 days after the last treatment administration.
Experiment 20 Reporting the Activity Date of This ADC					[21]
Patients Enrolled	Eligible female patients (18-75 years) have HER2+ (IHC3+/ISH+) unresectable/metastatic breast cancer (ECOG 0-1, &ge;12-week life expectancy, measurable lesions per RECIST v1.1, adequate organ function). Exclusions: recent malignancies (past 5 years), untreated CNS metastases, early recurrence (<12 months post- (neo)adjuvant therapy), uncontrolled effusions, recent anti-tumor treatments (4 weeks prior), immunodeficiency, severe cardiovascular/interstitial lung disease, unresolved toxicity (>Grade 1), bleeding disorders, active hepatitis/cirrhosis, or other clinically significant comorbidities.    Click to Show/Hide
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NCT Number	NCT06057610	Clinical Status	PHASE3
Clinical Description	A Phase III Multicenter, Randomized, Open-label, Active-Controlled Study of SHR-A1811 With or Without Pertuzumab Versus Trastuzumab, Pertuzumab and Docetaxel in HER2-Positive Recurrent or Metastatic Breast Cancer
Primary Endpoint	The primary efficacy endpoint is blinded independent central review-assessed PFS, measured from first dose until disease progression or death (up to 3 years).
Other Endpoint	Secondary endpoints include investigator-assessed PFS (3 years), OS (6 years), ORR and DoR (3 years), plus AE/SAE incidence/severity tracked from Day 1 until 40-90 days post-last dose.
Experiment 21 Reporting the Activity Date of This ADC					[22]
Patients Enrolled	Eligible participants are women (18-75 years) with HER2+ invasive breast cancer (pre-neoadjuvant stage T1-4/N0-3/M0, excluding T1N0) and residual disease post-surgery/neoadjuvant therapy (&ge;9 weeks taxane + trastuzumab). Exclusions: metastatic/recurrent disease, prior HER2-ADC exposure, high anthracycline doses (>240mg/m2 doxorubicin or >480mg/m2 epirubicin), significant cardiovascular/respiratory disorders, hepatitis/liver cirrhosis, or conditions increasing study risk. HR status and ECOG 0-1 are required.    Click to Show/Hide
Administration Dosage	Lyophilized powder injection, 100mg / bottle, intravenous drip
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NCT Number	NCT06126640	Clinical Status	PHASE3
Clinical Description	A Phase III, Multicenter, Randomized, Open-Label, Active-Controlled Study of SHR-A1811 Versus Trastuzumab Emtansine (T-DM1) in HER2-Positive Primary Breast Cancer Participants With Residual Invasive Disease Following Neoadjuvant Therapy
Primary Endpoint	The primary endpoint is invasive disease-free survival (IDFS), assessed from randomization until disease progression or approximately 77 months post-dose, evaluating long-term recurrence risk in HER2+ breast cancer patients.
Other Endpoint	Secondary endpoints include DFS, OS, and distant recurrence-free interval (DRFI), all tracked over extended periods (77-101 months post-dose), with safety assessed via AE incidence during the same timeframe, ensuring comprehensive monitoring of treatment efficacy and tolerability.
Experiment 22 Reporting the Activity Date of This ADC					[23]
Patients Enrolled	Eligible females (18-75 years, ECOG 0-1) have confirmed metastatic/locally advanced breast cancer (ER+/HER2&plusmn; or TNBC) with measurable lesions (RECIST v1.1) and organ function. Exclusions: uncontrolled brain metastases, active lung/cardiovascular diseases, recent immunosuppression, unresolved treatment toxicity (>Grade 1), active infections/hepatitis, prior malignancies (5 years), autoimmune/immunodeficiency disorders, or severe allergies to study drugs.    Click to Show/Hide
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NCT Number	NCT06222879	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Multi-center, Open-label Phase Ib/II Clinical Study on the Safety, Tolerability, Pharmacokinetics and Efficacy of HRS-8080 or SHR-A2009 Combined With Anti-tumor Therapy in Patients With Unresectable or Metastatic Breast Cancer
Primary Endpoint	The Phase 1 study evaluates dose-limiting toxicity (DLT), maximum tolerated dose (MTD), and recommended Phase 2 dose (RP2D) within the first 21-day cycle, with safety monitored via AE/SAE incidence (CTCAE v5.0) and efficacy assessed by ORR over 12 months.
Other Endpoint	Immunogenicity (ADA/Nab levels for SHR-A1811, SHR-A2009, and adebrelimab) and efficacy (ORR, BOR, DoR, DCR, CBR, PFS) are tracked over 12 months in both Phase 1 and 2, alongside safety (AE/SAE incidence) to ensure comprehensive therapeutic assessment.
Experiment 23 Reporting the Activity Date of This ADC					[24]
Patients Enrolled	Eligible patients are treatment-naive women aged 18-75 with HR+/HER2-low stage II-III breast cancer, ECOG 0-1, and adequate organ function. Exclusions include prior anti-tumor therapy, stage IV disease, concurrent malignancies, significant comorbidities (cardiovascular, lung, liver, or psychiatric disorders), and participation in other trials within 4 weeks.    Click to Show/Hide
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NCT Number	NCT06340230	Clinical Status	PHASE2
Clinical Description	A Phase II Study of SHR-A1811 Alone or in Combination With Adebrelimab as Neoadjuvant Treatment in HR Positive/HER2 Low Breast Cancer
Primary Endpoint	The primary endpoint is total pathological complete response (tpCR: ypT0-is/ypN0) assessed at the time of surgery, measuring the absence of invasive cancer in the breast and lymph nodes.
Other Endpoint	Secondary endpoints include breast pathological complete response (bpCR: ypT0-is), residual cancer burden (RCB), best overall response rate (BORR) during neoadjuvant treatment, and long-term survival outcomes (OS, DFS, EFS) over 5 years. Health-related quality of life (HRQOL) is evaluated using EORTC QLQ-C30 and QLQ-BR23 during the 18-week neoadjuvant phase.    Click to Show/Hide
Experiment 24 Reporting the Activity Date of This ADC					[25]
Patients Enrolled	Eligible patients were &ge;18 years with HER2+ breast cancer and measurable untreated intracranial lesions (RANO-BM criteria), &ge;2 weeks post-systemic therapy, and adequate organ function. Exclusions included prior DS-8201a/ADC therapy, recent trial participation, severe comorbidities (lung disease, uncontrolled hypertension/diabetes), or other safety risks per investigator judgment.    Click to Show/Hide
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NCT Number	NCT06361979	Clinical Status	PHASE2
Clinical Description	A Single-arm, Exploratory Clinical Study of SHR-A1811 Combined With Bevacizumab in the Treatment of HER2-positive Breast Cancer With Brain Metastases
Primary Endpoint	The primary endpoint was CNS-ORR, defined as the percentage of participants achieving CNS response per RANO-BM criteria, assessed over up to 2 years.
Other Endpoint	Secondary outcomes included PFS (time to progression or death), ORR (percentage with CR/PR per RECIST 1.1), and AE incidence (proportion with adverse events), all evaluated over up to 2 years.
Experiment 25 Reporting the Activity Date of This ADC					[26]
Patients Enrolled	Key inclusion lab criteria: ANC &ge;1.5&times;10<sup>9</sup>/L, PLT &ge;70&times;10<sup>9</sup>/L, HGB &ge;90g/L, ALT/AST &le;3&times;ULN, and LVEF &ge;50%. Exclusions also cover interstitial lung disease, &ge;4 ADC toxicity, allergies to study drugs, and other factors deemed by investigators to compromise safety or data integrity.
Administration Dosage	Assess the efficacy and safety of the SHR-A1811 in combination with Adebrelimab regimen in HER2 low-expressing metastatic breast cancer SHR-A1811 : 6.4mg/kg , q3w,d1, ivgtt Adebrelimab : 1200mg, q3w,d1, ivgtt
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NCT Number	NCT06411457	Clinical Status	PHASE2
Clinical Description	Single-arm, Multi-center Phase II Clinical Study of SHR-A1811 in Combination With Adebrelimab for the Treatment of HER2 Low-expressing Metastatic Breast Cancer
Primary Endpoint	The primary endpoint is Overall Response Rate (ORR), assessed every 6 weeks from randomization until first documented progression or death, whichever occurs first, up to 3 years. Secondary endpoints include 3-month Progression-Free Survival (PFS) rate, PFS assessed similarly up to 3 years, Clinical Benefit Rate (CBR), and safety endpoints (incidence of AEs, SAEs, and irAEs).    Click to Show/Hide
Other Endpoint	Eligible participants must be ≥18 years old with ER/PgR ≤10% and low HER2 expression, advanced breast cancer, prior taxane/anthracycline therapy, RECIST 1.1 measurable lesions, ECOG PS 0-1, and adequate organ function. Exclusions include active CNS metastases, prior anti-HER2 ADC treatment, active autoimmune disease, immunosuppressant use, other malignancies, severe ADC-related toxicities, uncontrolled cardiac conditions, active infections, live vaccine receipt within 4 weeks, or psychiatric/substance abuse issues.    Click to Show/Hide
Experiment 26 Reporting the Activity Date of This ADC					[27]
Patients Enrolled	Additional exclusions: interstitial lung disease, uncontrolled cardiovascular conditions, live vaccines within 4 weeks, pregnancy/breastfeeding, or factors compromising study integrity per investigator judgment. Required baseline assessments include ctDNA sampling and negative pregnancy tests for childbearing potential participants.
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NCT Number	NCT06433609	Clinical Status	PHASE2
Clinical Description	A Phase II Study of Antibody-Drug Conjugates (ADCs) Combined With Adebrelimab in HER2-negative Advanced Breast Cancer
Primary Endpoint	The primary endpoint is Objective Response Rate (ORR) by investigator assessment, defined as the percentage of evaluable patients achieving CR or PR per RECIST v1.1, measured from randomization until first progression or death, up to 3.5 years. Secondary endpoints include Disease Control Rate (DCR: CR/PR/SD), Clinical Benefit Rate (CBR: CR/PR/SD≥24 weeks), Duration of Response (DoR), Progression-Free Survival (PFS), Overall Survival (OS), and safety (AE incidence).    Click to Show/Hide
Other Endpoint	Eligible patients are females aged 18-75 with HER2-negative advanced breast cancer, ECOG PS 0-1, prior 1-2 lines of systemic therapy (CDK4/6 inhibitor required if HR-positive), ≥1 measurable lesion per RECIST v1.1, stable brain metastases if present, no prior PD- (L)1 inhibitors, and adequate organ function. Exclusion criteria include active/uncontrolled brain metastases, prior anti-HER2/TROP-2 therapy, unresolved third-space fluid, recent antitumor treatments, active autoimmune/immunodeficiency disorders, HBV/HCV infection, immunosuppressant use, second malignancies, or hypersensitivity to study drugs.    Click to Show/Hide
Experiment 27 Reporting the Activity Date of This ADC					[28]
Patients Enrolled	Additional exclusions: systemic immunomodulators within 4 weeks, immunosuppressants (excluding some corticosteroids), allergies to study drugs, concurrent clinical trials, live vaccines within 30 days, transplants, recent childbirth/breastfeeding, substance abuse, or other conditions increasing study risks per investigator judgment.
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NCT Number	NCT06592625	Clinical Status	PHASE2
Clinical Description	A Multicenter, Single-arm, Phase 2 Study of Neoadjuvant SHR-A1811 Plus Adebrelimab Injection for Early-stage or Locally Advanced HR Negative or Low Expression/HER2 Low Expression Breast Cancer
Primary Endpoint	Primary endpoints include investigator-assessed tpCR at around 18 weeks post-first dose (post-surgery), ORR pre-surgery, Ki-67 index changes post-surgery, and AEs/SAEs per NCI-CTCAE v5.0 from informed consent until 40-90 days post-treatment.
Other Endpoint	Eligible patients are female, aged 18-75, ECOG 0-1, with stage II/III HR-negative/low HER2+ breast cancer (tumor >2 cm), adequate organ function, and contraception compliance. Exclusions include metastatic/inflammatory breast cancer, prior malignancy (except certain carcinomas), interstitial lung disease, severe CVD, uncontrolled infections, bleeding disorders, or recent anticancer therapies.    Click to Show/Hide
Experiment 28 Reporting the Activity Date of This ADC					[29]
Patients Enrolled	Additional exclusions include recent chemo/radiotherapy (within 3 weeks), uncontrolled effusions, unresolved grade &ge;1 toxicities (excluding alopecia), steroid use (>10mg/day prednisone-equivalent), or conditions deemed high-risk by investigators. Fertile females must use contraception during and for 3 months post-treatment. All participants must provide informed consent and comply with follow-up.    Click to Show/Hide
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NCT Number	NCT06649331	Clinical Status	PHASE2
Clinical Description	Platform Study of ADC Rechallenge in ADC-treated Metastatic Breast Cancer:A Prospective, Open-label, Multicenter, Phase II Trial
Primary Endpoint	The primary efficacy endpoints include ORR (complete/partial response per RECIST 1.1), PFS (time to progression/death), CBR (CR/PR/SD ≥24 weeks), DOR (time from response to progression), OS (time to death up to 5 years), and treatment-related toxicity rate (AEs per CTCAEv5), all measured over a 36-month period except OS.
Other Endpoint	Eligible patients are ≥18 with locally advanced/metastatic breast cancer, prior ADC exposure, measurable disease, and adequate organ function (HB ≥90 g/L, ANC ≥1.5x10^9/L, ALT/AST ≤3-5×ULN, LVEF ≥50%). Key exclusions: uncontrolled CNS metastases, significant heart disease, active HBV/HCV/HIV, recent immunosuppressants, autoimmune diseases, major surgery within 3 weeks, pregnancy/lactation, or other malignancies (except non-melanoma skin/cervical carcinoma in situ).    Click to Show/Hide
Experiment 29 Reporting the Activity Date of This ADC					[30]
Patients Enrolled	Eligible patients require ECOG 0-1, adequate organ function (e.g., ANC &ge;1.5&times;10<sup>9</sup>/L, Hgb &ge;9.0 g/dL, LVEF &ge;50%), and exclusion criteria include untreated CNS metastases, significant cardiac conditions, hypersensitivity to SHR-A1811 components, or gastrointestinal issues impairing drug absorption.
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NCT Number	NCT06710990	Clinical Status	PHASE1
Clinical Description	A Multicenter, Open-label, Fixed-sequence Study to Evaluate Drug-drug Interaction of Ritonavir and Itraconazole on the Pharmacokinetics of SHR-A1811 in Subjects With HER2-expressing Advanced Breast Cancer
Primary Endpoint	The study evaluates pharmacokinetic parameters including Cmax and AUC0-16d for SHR-A1811 and its payload, measured during Cycle 2 and Cycle 3 (each lasting 21 days).
Other Endpoint	Additional secondary endpoints include Tmax, t1/2, AUCinf, CL, Vss, and safety assessments (adverse event incidence/severity), tracked from screening until ~3 months post-treatment.
Experiment 30 Reporting the Activity Date of This ADC					[31]
Patients Enrolled	Additional exclusions involve recent anticoagulant use, active malignancies (exceptions: cured cervical/skin cancers), immunodeficiency, uncontrolled HBV/HCV/syphilis, pregnancy/lactation, impaired drug absorption, or investigator-deemed ineligibility. The study prioritizes safety, requiring QTc &le;450/470 msec (M/F) and no allergy to study drugs.
Administration Dosage	In phase Ib, enrolled subjects will received SHR-A1811 combined with pyrotinib at different doses to confirm RP2D and evaluate the safety and tolerance. In phase II, enrolled subjects will received SHR-A1811 combined with pyrotinib and bevacizumab to evaluate the efficacy and safety.
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NCT Number	NCT06718933	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Prospective, Single-arm, Exploratory, Phase Ib/II Study of SHR-A1811 Combined with Pyrotinib and Bevacizumab in Advanced Breast Cancer with Brain Metastasis.
Primary Endpoint	The phase Ib study determines the RP2D based on MTD and subject tolerance, evaluated from first enrollment until Cycle 6 completion, disease progression, or AE-related discontinuation. The phase II primary endpoint is CNS-ORR per RANO-BM, assessed every 6 weeks as the proportion of patients achieving CR/PR.
Other Endpoint	Key inclusion criteria include age >18, ECOG PS 0-2, life expectancy ≥3 months, measurable brain metastases (no prior radiotherapy), stable mannitol/hormone use, adequate organ function, and recovery from prior treatment toxicities (≤G1). Exclusions cover leptomeningeal/cystic metastases, uncontrolled third-space fluid, emergent CNS complications, recent radiotherapy/chemotherapy, unresolved lung disease, bleeding risks, active infections, and significant cardiac/HTN conditions.    Click to Show/Hide
Experiment 31 Reporting the Activity Date of This ADC					[32]
Patients Enrolled	Eligible patients are females aged 18-75 with ECOG 0-2, locally advanced/metastatic breast cancer, no prior systemic therapy, and adequate organ function. Exclusions include uncontrolled diabetes, active infections, prior malignancies (except cured cases), severe comorbidities, pregnancy, or conditions compromising study adherence per investigator judgment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06788197	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Phase Ib/II Study of SHR-A1811 and Fulvestrant in Combination With or Without HS-10352 in Locally Advanced or Metastatic Breast Cancer Patients Who Progressed After Adjuvant Therapy
Primary Endpoint	The study evaluates the Objective Response Rate (ORR) per RECIST v1.1 in the SHR-A1811+fulvestrant and HS-10352 (Phase II) groups over approximately 4 years, defining ORR as the proportion of patients with complete or partial response. Additionally, the Recommended Phase 2 Dose (RP2D) for HS-10352 (Phase Ib) is assessed within a 28-day cycle.
Other Endpoint	Safety and efficacy endpoints include adverse event incidence/severity (CTCAE v5.0), ORR (HS-10352 Phase Ib), Progression-Free Survival (PFS), Overall Survival (OS), Clinical Benefit Rate (CR+PR+SD≥24 weeks), and Duration of Response (DOR) across both treatment groups (Phase Ib/II) over 4 years.
Experiment 32 Reporting the Activity Date of This ADC					[33]
Patients Enrolled	Eligible participants (age 18-75, ECOG 0-1) must have advanced pancreatic cancer with measurable lesions; exclusions include active infections, untreated CNS metastases, uncontrolled comorbidities, recent major surgery, or immunodeficiencies (e.g., HIV, active hepatitis B/C). High pancreatitis risk, recent immunotherapies, or unresolved treatment toxicity also disqualify participation per investigator assessment.    Click to Show/Hide
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NCT Number	NCT06547736	Clinical Status	PHASE2
Clinical Description	A Single-center, Open-label, Exploratory Platform Research on Precision Therapy of Advanced Pancreatic Cancer
Primary Endpoint	The study assesses the Recommended Phase II Dose (RP2D) based on safety and efficacy data from dose escalation stages over approximately 12 months, alongside Objective Response Rate (ORR) evaluated per RECIST v1.1 during the same timeframe.
Other Endpoint	Secondary endpoints include Disease Control Rate (DCR), Duration of Response (DOR), Progression-Free Survival (PFS), and Overall Survival (OS), all evaluated over a 12-month period. Safety is monitored via adverse events (AEs) graded by NCI-CTCAE v5.0 from first drug administration until 90 days post-last ADC dose.
Experiment 33 Reporting the Activity Date of This ADC					[34]
Patients Enrolled	Eligible patients are HR+/HER2- advanced breast cancer females (&ge;18 years) with prior CDK4/6 inhibitor exposure, measurable lesions, and adequate organ function. Exclusions include recent anticancer therapies (except bisphosphonates), uncontrolled CNS/heart disease, persistent toxicities (&ge;Grade 1), major surgery within 3 weeks, pregnancy, or other malignancies (except cured non-melanoma skin/cervical cancers) in 5 years.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05594095	Clinical Status	PHASE2
Clinical Description	Precision Platform Study of HR+/ HER2-advanced Breast Cancer Based on SNF Typing (A Prospective, Open-label, Multi-center, Phase II Platform Study)
Primary Endpoint	The primary endpoint is Overall Response Rate (ORR), defined as the proportion of patients achieving complete or partial remission per RECIST 1.1 criteria, assessed from randomization until disease progression or death over a 3-year study period.
Other Endpoint	Secondary endpoints include Clinical Benefit Rate (CBR: CR+PR+SD lasting ≥24 weeks), Progression-Free Survival (PFS), Overall Survival (OS), safety monitoring via CTCAE v5.0 for 1 year, and exploratory biomarker analysis using tumor/blood/fecal samples to investigate treatment-disease correlations.
Experiment 34 Reporting the Activity Date of This ADC					[35]
Patients Enrolled	Eligible participants are females aged 18-75 with adequate organ function and &ge;12-week life expectancy; exclusions involve active autoimmune/cardiovascular diseases, recent thromboembolic events, gastrointestinal obstruction, immunocompromised status, or other investigator-determined risks to trial integrity.
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NCT Number	NCT06859775	Clinical Status	PHASE1|||PHASE2
Clinical Description	Open-label, Multicenter Phase Ib/II Clinical Study of Injectable SHR-A1811 in Combination Regimens for the Treatment of Recurrent or Metastatic Cervical Cancer
Primary Endpoint	The primary endpoints include Grade ≥3 treatment-related adverse events (TRAEs) and serious adverse events (SAEs) over 3 years, alongside objective response rate (ORR) evaluating tumor shrinkage per RECIST criteria.
Other Endpoint	Secondary outcomes comprise duration of response (DOR), disease control rate (DCR), progression-free survival (PFS), and overall survival (OS), all measured over a 3-year follow-up period.
Experiment 35 Reporting the Activity Date of This ADC					[36]
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1) must have unresectable/metastatic biliary tract cancer, &ge;1 measurable lesion, adequate organ function, and HBV-DNA <500 IU/mL if HBV+. Exclusions cover recent anticancer therapies (<4 weeks), CNS metastases, severe comorbidities (cardiac/hepatic/pancreatic disorders, uncontrolled effusions), active infections, or thromboembolic events within 6 months.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06413745	Clinical Status	PHASE2
Clinical Description	A Phase II Clinical Study of SHR-A1811 in Patients With HER2-expressing/Amplified, Locally Advanced, Unresectable or Metastatic Biliary Tract Cancer (BTC) Who Have Previously Failed First or Second-line Systemic Therapy
Primary Endpoint	The primary endpoint is Objective Response Rate (ORR) assessed by Independent Review Committee (IRC) using RECIST v1.1 criteria over approximately one year.
Other Endpoint	Secondary endpoints include Duration of Response (DoR), Disease Control Rate (DCR), Progression-Free Survival (PFS) evaluated by IRC and researchers (RECIST v1.1, ~1 year), plus Overall Survival (OS, ~2 years) and safety measures (AEs/SAEs, ~1 year).
Experiment 36 Reporting the Activity Date of This ADC					[37]
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1) must have newly diagnosed locally advanced/metastatic biliary tract cancer with &ge;1 measurable lesion and adequate organ function. Key exclusions: concurrent malignancies, recent local therapy (<4 weeks), biliary obstruction, active autoimmune/interstitial lung diseases, uncontrolled HBV, or severe cardiovascular conditions.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06778031	Clinical Status	PHASE2
Clinical Description	An Open, Multicenter Phase II Clinical Study of SHR-A1811 in the Treatment of HER2-positive Locally Advanced or Metastatic Biliary Tract Cancer
Primary Endpoint	The primary endpoint is investigator-assessed Objective Response Rate (ORR) for the SHR-A1811 combination therapy, evaluated during screening through study completion over an average of 3 years per RECIST v1.1 criteria.
Other Endpoint	Secondary outcomes include investigator-assessed DoR, DCR, PFS, and OS for the SHR-A1811 combination (3-year average), alongside adverse events (AEs) monitoring throughout the study period.
Experiment 37 Reporting the Activity Date of This ADC					[38]
Patients Enrolled	Eligible patients must have RAS/RAF wild-type metastatic colorectal cancer (post-oxaliplatin/5-FU/irinotecan &plusmn; anti-PD-1/PD-L1 failure for DMMR/MSI-H), &ge;1 measurable lesion (RECIST 1.1), ECOG 0-1, and adequate organ function. Exclusions: active infections (HBV DNA &ge;500 IU/mL, HCV+), uncontrolled effusions, recent major surgery/immunosuppressants (>10 mg prednisone/day), CNS metastases, or other malignancies within 5 years (excl. non-melanoma skin/cervical carcinoma in situ).    Click to Show/Hide
Administration Dosage	SHR-A1811 (4.8 mg/kg) was administered intravenously on the first day of each cycle, once every 3 weeks (Q3W)
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NCT Number	NCT06199973	Clinical Status	PHASE3
Clinical Description	Injection of SHR-A1811 Versus Physician Choiced Treatment in Patients With Advanced Colorectal Cancer Who Had Failed to Respond to Oxaliplatin, 5-fu, and Irinotecan
Primary Endpoint	The primary endpoint is Independent Review Committee (IRC)-assessed Progression-Free Survival (PFS), evaluated every 6 weeks for up to 3 years.
Other Endpoint	Secondary endpoints include safety (adverse events monitored per cycle, 21-28 days) and investigator-assessed efficacy measures: PFS, Objective Response Rate (ORR), Duration of Response (DoR), and Overall Survival (OS), all tracked every 6 weeks over 3 years.
Experiment 38 Reporting the Activity Date of This ADC					[39]
Patients Enrolled	Eligible participants (18-75 years, ECOG 0-1, life expectancy >3 months) must have histologically confirmed unresectable/metastatic gastric/GEJ adenocarcinoma (Cohorts A/B) with &ge;1 measurable lesion (RECIST 1.1) and adequate organ function (ANC &ge;1.5&times;10<sup>9</sup>/L, PLT &ge;100&times;10<sup>9</sup>/L, LVEF &ge;50%, etc.). Exclusions: untreated/active CNS metastases, uncontrolled effusions, prior topoisomerase I inhibitor ADC therapy (e.g., DS-8201), immunosuppressants (>10 mg/day prednisone within 14 days), unresolved Grade >1 toxicities (excluding alopecia), active HBV/HCV infection, severe cardiovascular disease, or uncontrolled infections (IV antibiotics within 2 weeks).    Click to Show/Hide
Administration Dosage	SHR-A1811 injection will be administered by intravenous infusion. And apatinib will be administered orally.
Related Clinical Trial
NCT Number	NCT06666166	Clinical Status	PHASE2
Clinical Description	Exploratory Clinical Study of SHR-A1811 Combined with Apatinib in the Treatment of Advanced Gastric or Gastroesophageal Junction Adenocarcinoma and Colorectal Cancer
Primary Endpoint	The primary endpoint is Objective Response Rate (ORR), assessed from baseline up to 6 months, to evaluate antitumor efficacy.
Other Endpoint	Secondary endpoints include Duration of Response (DOR) and Overall Survival (OS) (baseline up to 12 months), Disease Control Rate (DCR) and Progression-Free Survival (PFS) (baseline up to 6 months), and incidence of Treatment-Emergent Adverse Events (from first dose to 28 days post-last dose) to assess safety and tolerability.
Experiment 39 Reporting the Activity Date of This ADC					[40]
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1, HER2+, life expectancy &ge;3 months) must have locally advanced/metastatic gastric/GEJ adenocarcinoma-Phase Ib: prior treatment failure/intolerance; Phase II: treatment-na&iuml;ve. Exclusions: uncontrolled effusions, recent major surgery (4 weeks), active autoimmunity, interstitial pneumonia, recent severe infection (4 weeks), tuberculosis (1 year), cardiovascular risks, or recent GI perforation/fistula (6 months).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05671822	Clinical Status	PHASE2
Clinical Description	A Phase Ib/II Study of SHR-A1811 Combinations in Patients With Advanced/Metastatic HER2 Expression Gastric /Gastroesophageal Junction Adenocarcinoma
Primary Endpoint	The Phase Ib study evaluates safety through DLT rates, AEs, and SAEs (assessed over 24 months post-consent), while Phase II primarily measures ORR (average 12-month follow-up).
Other Endpoint	Secondary endpoints include ORR, DOR, PFS (all Phase Ib: 12-18 months), OS (Phase Ib: 30 months); Phase II assesses DOR/PFS (18 months), OS (30 months), and AEs/SAEs (24 months post-consent). Safety remains a cross-phase priority.
Experiment 40 Reporting the Activity Date of This ADC					[41]
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1) must have metastatic NSCLC, measurable lesions, organ function adequacy, and failed standard therapy. Exclusions involve active CNS metastases, recent antitumor therapies, uncontrolled comorbidities, autoimmune/cardiac diseases, infections, pregnancy, or conditions affecting drug absorption/compliance per investigator judgment. Tissue samples are mandatory.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05482568	Clinical Status	PHASE1|||PHASE2
Clinical Description	Phase IB/II Clinical Study of the Safety, Tolerability, Pharmacokinetics, and Efficacy of Injectable SHR-A1811 in Combination With Pyrotinib or SHR-1316 in Subjects With Advanced Non-small Cell Lung Cancer With HER2
Primary Endpoint	The Phase I (dose exploration phase) primary endpoints include DLT (assessed 21 days post-first administration), AE, and SAE incidence/severity (both tracked for two years post-last enrollment). The Phase II (efficacy expansion stage) primary endpoint is objective response rate (evaluated over two years post-last enrollment).
Other Endpoint	Phase I/II secondary endpoints comprise immunogenicity markers (toxin-binding/total/neutralizing antibodies for SHR-A1811/SHR-1316), pharmacokinetic parameters (free toxin SHR169265, pyrotinib, SHR-1316 plasma concentrations), and efficacy outcomes (ORR, DoR, PFS). All assessments span two years post-last enrollment.
Experiment 41 Reporting the Activity Date of This ADC					[42]
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1) must have HER2-mutated advanced/metastatic NSCLC without prior systemic treatment, measurable lesions (RECIST 1.1), and adequate organ function. Exclusions include mixed histology, additional driver mutations (with approved targeted drugs), untreated CNS metastases, uncontrolled pain, concurrent malignancies, interstitial pneumonia, autoimmune/cardiovascular diseases, or active hepatitis B/C.    Click to Show/Hide
Administration Dosage	Drug: SHR-A1811 administered intravenously every 3 weeks (Q3W)
Related Clinical Trial
NCT Number	NCT06430437	Clinical Status	PHASE3
Clinical Description	A Randomized, Open-Label, Multicenter Phase III Study of SHR-A1811 for First-Line Treatment in Subjects With HER2-Mutated Advanced or Metastatic Non-Small Cell Lung Cancer
Primary Endpoint	The primary endpoint is progression-free survival (PFS) assessed by blinded independent central review (BICR) per RECIST 1.1, measured from randomization until progression (evaluation period up to 2 years).
Other Endpoint	Secondary endpoints include overall survival (OS) (until death, up to 3 years), investigator-assessed PFS (up to 2 years per RECIST 1.1), and incidence/severity of AEs/SAEs (graded by CTCAE v5.0, tracked until 90 days post-last dose, up to 3 years).
Experiment 42 Reporting the Activity Date of This ADC					[43]
Patients Enrolled	Eligible subjects must provide informed consent, have measurable disease per RECIST v1.1, ECOG 0-1 performance status, and &ge;12-week life expectancy. Exclusions comprise active CNS metastases, uncontrolled cardiovascular/autoimmune diseases, active hepatitis B/C, severe infections, and tuberculosis.
Related Clinical Trial
NCT Number	NCT06828354	Clinical Status	PHASE3
Clinical Description	An Open-label, Randomized, Multicenter Phase III Clinical Trial of SHR-A1811 Versus Investigator-selected Chemotherapy for Platinum-resistant Relapsed Epithelial Ovarian, Fallopian Tube, or Primary Peritoneal Cancer
Primary Endpoint	The primary endpoint is progression-free survival (PFS) evaluated from day 1 of treatment up to 10 months.
Other Endpoint	Key secondary endpoints include objective response rate (ORR), disease control rate (DCR), duration of response (DOR), overall survival (OS), and response rate (RR) (all assessed from day 1 to 12 months), along with monitoring adverse events (AEs) until 40 days post-last dose.
Experiment 43 Reporting the Activity Date of This ADC					[44]
Patients Enrolled	Eligible participants must provide informed consent, supply tumor tissue for testing, have measurable lesions per RECIST v1.1, an ECOG PS of 0-1, and expected survival &ge;12 weeks. Key exclusions involve uncontrolled CNS metastases, symptomatic effusions, interstitial lung disease, poorly managed hypertension, serious infections, immune deficiency, or other factors compromising study integrity.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06840002	Clinical Status	PHASE1|||PHASE2
Clinical Description	An Open, Multicenter Phase Ib / II Clinical Study of SHR-A1811 Combined With Chemotherapy for Platinum Sensitive Recurrent Ovarian Cancer
Primary Endpoint	The study evaluates dose-limited toxicity (DLT) and recommended Phase II dose (RP2D) within 21 days, alongside objective response rate (ORR) assessed every 9 weeks over approximately one year.
Other Endpoint	Secondary endpoints include duration of response (DoR), disease control rate (DCR), progression-free survival (PFS), and standard response rate (RR), all monitored every 9 weeks for about one year. Overall survival (OS) is tracked for around 3 years post-enrollment, while adverse events (AEs) and serious adverse events (SAEs) are recorded from first dose to 90 days post-treatment.    Click to Show/Hide
Experiment 44 Reporting the Activity Date of This ADC					[45]
Patients Enrolled	Eligible patients must be &ge;18 years old with measurable lesions per RECIST 1.1, ECOG 0-1, life expectancy &ge;12 weeks, and adequate organ function. Exclusions include untreated brain/meningeal metastases, symptomatic effusions requiring drainage, prior malignancies (within 5 years), uncontrolled cardiovascular/autoimmune diseases, active hepatitis, unresolved treatment-related toxicities (CTCAE >1), and recent GI obstruction/perforation.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05349409	Clinical Status	PHASE2
Clinical Description	A Phase Ib/II Clinical Study on the Dosage Exploration and Efficiency Expansion of SHR-A1811 for Injection in Combination With Fluzoparib Capsule in HER2-Expressing Advanced Solid Tumors of Patients
Primary Endpoint	The study evaluates dose-limiting toxicity (DLT) and determines the recommended Phase II dose (RP2D) of SHR-A1811 combined with Fluzoparib within 21 days. Objective response rate (ORR) is assessed based on RECIST v1.1, measured from treatment initiation to disease progression or alternative therapy, up to 6 months.
Other Endpoint	Secondary endpoints include duration of response (DoR), disease control rate (DCR), time to recovery (TTR), progression-free survival (PFS), and overall survival (OS) up to 100 months, along with 12-month survival rate. Safety endpoints track AEs/SAEs per CTCAE v5.0 and dose modifications due to toxicity. Pharmacokinetics (PK) parameters (Cmin, C3h, Cmax, AUC0-t) and immunogenicity (ADA, NAb) of SHR-A1811 and Fluzoparib are monitored over defined periods.    Click to Show/Hide
Experiment 45 Reporting the Activity Date of This ADC					[46]
Patients Enrolled	Eligibility requires age 18-75, ECOG 0-1, HER2-positive advanced/metastatic solid tumors, measurable lesions, and adequate organ function. Key exclusions include active CNS/meningeal metastases, prior HER2 ADC/ TKI use, unresolved toxicities >CTCAE G2, active ILD, uncontrolled infections (HBV/HCV/HIV), recent major surgery, allergies to study drugs, pregnancy, or uncontrolled comorbidities (e.g., hypertension, thrombosis risk). Part B1 further excludes G2+ neuropathy or BP102-related bleeding/thrombosis risks.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06015048	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Phase 1b/2 Study to Evaluate the Safety, Tolerability and Efficacy of SHR-A1811 Combined With Other Antitumor Therapies in Advanced Solid Tumors.
Primary Endpoint	Part A (Phase IB) assesses the maximally tolerated dose (MTD), recommended phase 2 dose (RP2D), adverse events (AEs), and objective response rate (ORR) within 11 months. ORR is evaluated per RECIST v1.1 from treatment initiation to disease progression or last dose.
Other Endpoint	Secondary endpoints include disease control rate (DCR), duration of response (DoR), progression-free survival (PFS), overall survival (OS), and safety (assessed per CTCAE) in both Phase IB and Phase II, with follow-up periods up to 13 months.
Experiment 46 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Objective Response Rate (ORR)	61.60 81.50 55.80 %
Patients Enrolled	Pts were eligible if they had HER2 positive breast cancer (BC), HER2 positive gastric/GEJ carcinoma, HER2 low-expressing BC, HER2-expressing/mutated NSCLC, or other HER2-expressing/mutated solid tumors, and were refractory or intolerant to standard therapy.
Administration Dosage	SHR-A1811 at doses of 1.00-8.00 mg/kg was given Q3W (IV).
Related Clinical Trial
NCT Number	NCT04446260	Clinical Status	Phase 1
Clinical Description	A phase 1 multi-country, multi-center, open-label study to evaluate the safety, tolerability, pharmacokinetics and efficacy of SHR-A1811 in HER2 expressing or mutated advanced malignant solid tumor subjects.
Experiment 47 Reporting the Activity Date of This ADC					[64]
Related Clinical Trial
NCT Number	NCT05424835	Clinical Status	Phase 3
Clinical Description	A phase 3, multicenter, randomized, open-label, parallel controlled study of SHR-A1811 versus pyrotinib in combination with capecitabine for HER2-positive, unresectable and/or metastatic breast cancer subjects previously treated with trastuzumab and taxane.
Experiment 48 Reporting the Activity Date of This ADC					[65]
Related Clinical Trial
NCT Number	NCT05594095	Clinical Status	Phase 2
Clinical Description	Precision platform study of HR+/ HER2-advanced breast cancer based on snf typing (a prospective, open-label, multi-center, phase 2 platform study).
Experiment 49 Reporting the Activity Date of This ADC					[66]
Related Clinical Trial
NCT Number	NCT05749588	Clinical Status	Phase 2
Clinical Description	Precision platform study of refractory triple-negative breast cancer based on molecular subtyping (a phase 2, open-label, single-center platform study).
Experiment 50 Reporting the Activity Date of This ADC					[67]
Related Clinical Trial
NCT Number	NCT05769010	Clinical Status	Phase 2
Clinical Description	A prospective, open-label explorative study of SHR-A1811 in HER2-expression advanced breast cancer with brain metastases.
Experiment 51 Reporting the Activity Date of This ADC					[68]
Related Clinical Trial
NCT Number	NCT05353361	Clinical Status	Phase 2
Clinical Description	A phase 1b/2 multicenter, open-label clinical trial of SHR-A1811 injection in combination with pyrotinib or pertuzumab or SHR-1316 or paclitaxel for injection (albumin bound) in HER2-positive breast cancer.
Experiment 52 Reporting the Activity Date of This ADC					[69]
Related Clinical Trial
NCT Number	NCT05671822	Clinical Status	Phase 2
Clinical Description	A phase 1b/2 study of SHR-A1811 combinations in patients with advanced/metastatic HER2+ gastric /gastroesophageal junction adenocarcinoma.
Experiment 53 Reporting the Activity Date of This ADC					[70]
Related Clinical Trial
NCT Number	NCT05635487	Clinical Status	Phase 2
Clinical Description	A single-arm, phase 2 study of SHR-A1811 combined with pyrotinib maleate as neoadjuvant treatment in HER2-positive breast cancer patients.
Experiment 54 Reporting the Activity Date of This ADC					[71]
Related Clinical Trial
NCT Number	NCT05349409	Clinical Status	Phase 2
Clinical Description	A phase 1b/2 clinical study on the dosage exploration and efficiency expansion of SHR-A1811 for injection in combination with fluzoparib capsule in HER2-expressing advanced solid tumors of patients.
Experiment 55 Reporting the Activity Date of This ADC					[72]
Related Clinical Trial
NCT Number	NCT05582499	Clinical Status	Phase 1/2
Clinical Description	Fudan university shanghai cancer center breast cancer precision platform series study- neoadjuvant therapy (FASCINATE-N).
Experiment 56 Reporting the Activity Date of This ADC					[73]
Related Clinical Trial
NCT Number	NCT05482568	Clinical Status	Phase 1/2
Clinical Description	Phase 1B/2 clinical study of the safety, tolerability, pharmacokinetics, and efficacy of injectable SHR-A1811 in combination with pyrotinib or SHR-1316 in subjects with advanced non-small cell lung cancer with HER2.
Experiment 57 Reporting the Activity Date of This ADC					[74]
Related Clinical Trial
NCT Number	NCT04818333	Clinical Status	Phase 1/2
Clinical Description	Phase 1/2 clinical study of the safety, tolerability, pharmacokinetics, and efficacy of SHR-A1811 for injection in subjects with advanced non-small cell lung cancer who have HER2 expression, amplification, or mutation.
Experiment 58 Reporting the Activity Date of This ADC					[75]
Related Clinical Trial
NCT Number	NCT04513223	Clinical Status	Phase 1
Clinical Description	Safety, tolerability, pharmacokinetics, and antitumour activity of SHR-A1811, in patients with HER2-expressing advanced gastric or gastroesophageal junction adenocarcinoma and colorectal cancer: a phase 1 study.

Experiment 1 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.42 ± 0.10 nM	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of SHR169265 was evaluated in SK-BR-3 cell lines.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.57 ± 0.15 nM	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of SHR169265 was evaluated in NCI-N87 cell lines.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.77 ± 0.10 nM	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of SHR169265 was evaluated in HCC1954 cell lines.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 4 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	11.3 ± 2.7 nM	Low HER2expression (HER2+)
Method Description	The cytotoxicity of SHR169265 was evaluated in CaPAN-1 cell lines.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 5 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	42.5 ± 7.8 nM	Low HER2expression (HER2+)
Method Description	The cytotoxicity of SHR169265 was evaluated in MKN45 cell lines.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 6 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	59.1 ± 17.2 nM	Low HER2expression (HER2+)
Method Description	The cytotoxicity of SHR169265 was evaluated in AGS cell lines.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 7 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	97.3 ± 23.1 nM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of SHR169265 was evaluated in MDA-MB-468 cell lines.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 8 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	132.6 nM	Low HER2expression (HER2+)
Method Description	The cytotoxicity of SHR169265 was evaluated in SNU-16 cell lines.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 9 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	302.9 ± 87 nM	Moderate HER2 expression (HER2++)
Method Description	The cytotoxicity of SHR169265 was evaluated in JIMT-1 cell lines.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0652 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.2344 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	> 100 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	> 100 nM	Negative HER2 expression (HER2-)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.7 ng/mL	Moderate HER2 expression (HER2 ++)
Method Description	In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 and ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 6 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.8 ng/mL	Moderate HER2 expression (HER2 ++)
Method Description	In vitro cytotoxicity of ADCs against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 7 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.1 ng/mL	High HER2 expression (HER2 +++)
Method Description	In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 and ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 8 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.3 ng/mL	Moderate HER2 expression (HER2 ++)
Method Description	In vitro cytotoxicity of DS-8201 plus ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 9 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.1 ng/mL	High HER2 expression (HER2 +++)
Method Description	In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 10 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.7 ng/mL
Method Description	The inhibitory activity of DS-8201a against cancer cell growth was compared with an anti-HER2 Ab and control IgG-ADC-conjugated with DXd against various human cancer cell lines in vitroThe cells were treated with DS-8201a, anti-HER2 Ab, and control IgG-ADC for 6 days.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 11 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.6 ng/mL	High HER2 expression (HER2 +++)
Method Description	In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 and ATR inhibitor BAY1895344 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 12 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.6 ng/mL	Moderate HER2 expression (HER2 ++)
Method Description	In vitro cytotoxicity of DS-8201 plus PARP inhibitor BAY1895344 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 13 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.1 ng/mL	High HER2 expression (HER2 +++)
Method Description	In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 and ATR inhibitor BAY1898344 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 14 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9 ng/mL	High HER2 expression (HER2 +++)
Method Description	In vitro cytotoxicity of DS-8201 plus ATR inhibitor BAY1895344 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 15 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.5 ng/mL	High HER2 expression (HER2 +++)
Method Description	In vitro cytotoxicity of ADCs against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 16 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.1 ng/mL	Moderate HER2 expression (HER2 ++)
Method Description	In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 and ATR inhibitor BAY1895344 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 17 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.7 ng/mL	High HER2 expression (HER2 +++)
Method Description	In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 18 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.9 ng/mL	High HER2 expression (HER2 +++)
Method Description	In vitro cytotoxicity of DS-8201 plus ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 19 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	25.4 ng/mL
Method Description	The inhibitory activity of DS-8201a against cancer cell growth was compared with an anti-HER2 Ab and control IgG-ADC-conjugated with DXd against various human cancer cell lines in vitroThe cells were treated with DS-8201a, anti-HER2 Ab, and control IgG-ADC for 6 days.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 20 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26.8 ng/mL
Method Description	The inhibitory activity of DS-8201a against cancer cell growth was compared with an anti-HER2 Ab and control IgG-ADC-conjugated with DXd against various human cancer cell lines in vitroThe cells were treated with DS-8201a, anti-HER2 Ab, and control IgG-ADC for 6 days.
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310
Experiment 21 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	32.7 ng/mL	High HER2 expression (HER2 +++)
Method Description	In vitro cytotoxicity of ADCs against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 22 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	34.8 ng/mL	Moderate HER2 expression (HER2 ++)
Method Description	In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 23 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	41.7 ng/mL	Moderate HER2 expression (HER2 ++)
Method Description	In vitro cytotoxicity of ADCs against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 24 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	41.8 ng/mL	Moderate HER2 expression (HER2 ++)
Method Description	In vitro cytotoxicity of DS-8201 plus ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 25 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3000 ng/mL	Negative HER2 expression (HER2 -)
Method Description	In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 and ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 26 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3000 ng/mL	Negative HER2 expression (HER2 -)
Method Description	In vitro cytotoxicity of DS-8201 plus ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 27 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3000 ng/mL	High HER2 expression (HER2 +++)
Method Description	In vitro cytotoxicity of DS-8201 plus ATR inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 28 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3000 ng/mL	Negative HER2 expression (HER2 -)
Method Description	In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 29 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3000 ng/mL	High HER2 expression (HER2 +++)
Method Description	In vitro cytotoxicity of DS-8201 plus PARP inhibitor AZD2281 against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 30 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3000 ng/mL	Negative HER2 expression (HER2 -)
Method Description	In vitro cytotoxicity of ADCs against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 31 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3000 ng/mL	High HER2 expression (HER2 +++)
Method Description	In vitro cytotoxicity of ADCs against a panel of multiple human cancer cell lines. IC50 values were determined by sulforhodamine B assay in cells treated with different concentrations of drugs for 120 h.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 32 Reporting the Activity Date of This ADC					[78]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 ug/mL	High HER2 expression (HER2 +++, IHC 3+)
Method Description	Viability of NCI-N87 cells as well as of parental HCT116 cells and their derivatives (Mock, H2L and H2H) after incubation with the indicated concentrations of trastuzumab deruxtecan (DS-8201a) or T-DM1 for 144 h.
In Vitro Model	Colon carcinoma	HCT 116-H2H cells (High HER2 expression)		CVCL_0291
Experiment 33 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL
Method Description	The inhibitory activity of DS-8201a against cancer cell growth was compared with an anti-HER2 Ab and control IgG-ADC-conjugated with DXd against various human cancer cell lines in vitroThe cells were treated with DS-8201a, anti-HER2 Ab, and control IgG-ADC for 6 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 34 Reporting the Activity Date of This ADC					[78]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	97 ug/mL	High HER2 expression (HER2 +++)
Method Description	Viability of NCI-N87 cells as well as of parental HCT116 cells and their derivatives (Mock, H2L and H2H) after incubation with the indicated concentrations of trastuzumab deruxtecan (DS-8201a) or T-DM1 for 144 h.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[48]
Efficacy Data	Objective Response Rate (ORR)	52.90 52.30 %
Patients Enrolled	HER2-low metastatic breast cancer who had received one or two previous lines of chemotherapy.
Administration Dosage	Intravenously every 3 weeks at a dose of 5.40 mg per kilogram of body weight.
Related Clinical Trial
NCT Number	NCT03734029	Clinical Status	Phase 3
Clinical Description	A phase 3, multicenter, randomized, open-label, active controlled trial of DS-8201a, an Anti-HER2-antibody drug conjugate (ADC), versus treatment of physician's choice for HER2-low, unresectable and/or metastatic breast cancer subjects.
Primary Endpoint	In HR+ cohort, for ENHERTU (N=331), median Progression-Free Survival (mFPS)=10.10 months (95% Cl 9.50-11.50), for Chemotherapy (N=163), median Progression-Free Survival (mFPS)=5.40 months(95% Cl 4.40-7.10), hazard radio=0.51 (95% Cl 0.40-0.64) and p-value<0.0001.
Other Endpoint	In HR+ cohort, for ENHERTU (N=331), median overall survival (months)=23.90 (95% Cl 20.80-24.80), Confirmed Objective Response Rate=52.90% (95% Cl 47.30-58.40), Complete Response rate=36.00%, Partial Response rate= 49.50%, median Duration of Response (months)=10.70 (95% Cl 8.50-13.70); for Chemotherapy (N=163), median overall survival (months)=17.50 (95% Cl 15.20-24.80), Confirmed Objective Response Rate=16.60% (95% Cl 11.20-23.20), Complete Response rate=0.60%, Partial Response rate= 16.00%, median Duration of Response (months)=6.80 (95% Cl 6.50-9.90). In HR+ and HR- cohort, for ENHERTU (N=373), median Progression-Free Survival (mFPS)=9.90 months (95% Cl 9.00-11.30), median overall survival (months) = 23.40 (95% Cl 20.00-24.80), Confirmed Objective Response Rate = 52.30% (95% Cl 47.10-57.40), Complete Response rate=35.00%, Partial Response rate= 49.10%, median Duration of Response(months)=10.70 (95% Cl 8.50-13.20); for Chemotherapy (N=184), median Progression-Free Survival (mFPS)=5.40 months(95% Cl 4.20-6.80), median overall survival (months)=16.80(95% Cl 14.50-20.00), Confirmed Objective Response Rate=16.30% (95% Cl 11.30-22.50), Complete Response rate=11.00%, Partial Response rate= 15.20%, median Duration of Response(months)=6.80 (95% Cl 6.00-9.90).    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[49]
Efficacy Data	Objective Response Rate (ORR)	79.70%
Patients Enrolled	HER2-positive unresectable or metastatic breast cancer who were previously treated with trastuzumab and a taxane in the advanced or metastatic setting.
Related Clinical Trial
NCT Number	NCT03529110	Clinical Status	Phase 3
Clinical Description	A phase 3, multicenter, randomized, open-label, active-controlled study of DS-8201a (Trastuzumab Deruxtecan), an Anti-HER2 antibody drug conjugate (ADC), versus Ado Trastuzumab Emtansine (T-DM1) for HER2-positive, unresectable and/or metastatic breast cancer subjects previously treated with trastuzumab and taxane.
Primary Endpoint	The median patient age was 54 years. Approximately 50% of patients were treated with 0-1 prior lines of therapy in the metastatic setting, and 50% were treated with 2 prior treatment regimens. At baseline, 16.50% of patients in the T-DXd group and 14.80% of those in the T-DM1 group had brain metastases. At a median follow-up of 15.90 months, T-DXd significantly improved PFS by 72% compared with T-DM1 across all patient subgroups. Findings were consistent irrespective of hormone receptor status, prior treatment with pertuzumab, number of prior lines of therapy, presence or absence of visceral disease, and presence or absence of brain metastases. The overall response rate (ORR) in the overall study cohort was 79.70% and 34.20% in the T-DXd and T-DM1 groups, respectively, representing an absolute improvement in ORR of 45% with T-DXd Findings were consistent across all patient subgroups, with the absolute improvement in ORR associated with T-DXd relative to T-DM1 ranging from 39% to 52%.    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Objective Response Rate (ORR)	79.70%
Patients Enrolled	HER2-positive metastatic breast cancer previously treated with trastuzumab and a taxane.
Administration Dosage	Intravenously every 3 weeks at a dose of 5.40 mg per kilogram of body weigh.
Related Clinical Trial
NCT Number	NCT03529110	Clinical Status	Phase 3
Clinical Description	A phase 3, multicenter, randomized, open-label, active-controlled study of DS-8201a (Trastuzumab Deruxtecan), an Anti-HER2 antibody drug conjugate (ADC), versus Ado Trastuzumab Emtansine (T-DM1) for HER2-positive, unresectable and/or metastatic breast cancer subjects previously treated with trastuzumab and taxane.
Primary Endpoint	For ENHERTU 5.40 mg/kg, Median Progression-Free Survival (mPFS)=not reached (95% Cl 18.5-not estimable); For Ado-trastuzumab emtansine 3.60 mg/kg, Median Progression-Free Survival (mPFS)=6.80months (95% Cl 5.60-8.20), hazard radio=0.28 (95% Cl 0.22-0.37) and p-value<0.0001.
Other Endpoint	For ENHERTU 5.40 mg/kg, Confirmed Objective Response Rate (ORR)=79.70% (95% Cl 74.30%-84.40%), complete response rate=16.10%, partial response rate=63.60%; For Ado-trastuzumab emtansine 3.60 mg/kg, Confirmed Objective Response Rate (ORR)=34.20% (95% Cl 28.50%-40.30%), complete response rate=8.70%, partial response rate=25.50%.
Experiment 4 Reporting the Activity Date of This ADC					[53]
Efficacy Data	Objective Response Rate (ORR)	43%	Positive HER2 expression (HER2+++/++; HER2 MFI=562)
Patients Enrolled	HER2-positive gastric or gastroesophageal junction adenocarcinoma that had progressed while they were receiving at least two previous therapies, including trastuzumab.
Administration Dosage	6.40 mg per kilogram of body weight every 3 weeks.
Related Clinical Trial
NCT Number	NCT03329690	Clinical Status	Phase 2
Clinical Description	A phase 2, multicenter, open-label study of DS-8201a in subjects with HER2-expressing advanced gastric or gastroesophageal junction adenocarcinoma.
Primary Endpoint	In the trastuzumab deruxtecan group, confirmed objective response rate=43.00% (95% Cl 34.00-52.00%), complete response rate=8.00%, partial response rate=34.00%. In the chemotherapy group, confirmed objective response rate=12.00% (95% Cl 5.00-24.00%), complete response rate=0.00%, partial response rate=12.00%.
Other Endpoint	In the trastuzumab deruxtecan group (N=119), confirmed disease control rate=86.00% (95% Cl 78.00-91.00%), median Duration of Response (mDOR)=11.30 months (95% Cl 5.60-not estimable), median overall survival (mOS)=12.50 months (95% Cl 9.60-14.30), estimated overall survival was 80.00% at 6 months and 52.00% at 12 months, median progression-free survival (mPFS)=5.60 months (95% CI, 4.30-6.90), estimated progression-free survival=43.00% at 6 months and 30.00% at 12 months In the chemotherapy group (N=56), confirmed disease control rate=62.00% (95% Cl 49.00-75.00%), median Duration of Response (mDOR)=3.90 months (95% Cl 3.0-4.9), median overall survival (mOS)=8.40 months (95% Cl 6.90-10.70), estimated overall survival was 66.00% at 6 months and 29.00% at 12 months, median progression-free survival (mPFS)=3.50 months (95% CI, 2.00-4.30), estimated progression-free survival=21.00% at 6 months and 0.00% at 12 months.    Click to Show/Hide
Experiment 5 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Objective Response Rate (ORR)	45.30%	High HER2 expression (HER2 +++)
Patients Enrolled	86 patients with metastatic colorectal cancer (mCRC) were enrolled and received at least 1 dose of T-DXd, including 53 patients in cohort A (HER2-positive, immunohistochemistry [IHC] 3+ or IHC 2+/in situ hybridization [ISH]+), 15 patients in cohort B (HER2 IHC 2+/ISH), and 18 patients in cohort C (HER2 IHC 1+).
Administration Dosage	6.4 mg/kg every 3 weeks
Related Clinical Trial
NCT Number	NCT04744831	Clinical Status	Phase 2
Clinical Description	A phase 2, multicenter, randomized, study of trastuzumab deruxtecan in participants with HER2-overexpressing locally advanced, unresectable or metastatic colorectal cancer (DESTINY-CRC02).
Primary Endpoint	ORR of 45.30% in cohort A
Other Endpoint	No responses occurred in cohorts B or C. Median progression-free survival, overall survival, and duration of response were 6.90, 15.50, and 7.00 months, respectively.
Experiment 6 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Objective Response Rate (ORR)	55%	Positive HER2 expression (HER2+++/++; HER2 MFI=1016)
Patients Enrolled	HER2-overexpressing or HER2-mutant non-small cell lung cancer (NSCLC).
Administration Dosage	Intravenously every 3 weeks at a dose of 6.40 mg per kilogram of body weight.
Related Clinical Trial
NCT Number	NCT03505710	Clinical Status	Phase 2
Clinical Description	A phase 2, multicenter, open-label, 2-cohort study of Trastuzumab Deruxtecan (DS-8201a), an anti-HER2 antibody drug conjugate (ADC), for HER2-over-expressing or -mutated, unresectable and/or metastatic non small cell lung cancer (NSCLC) (DESTINY-Lung01).
Primary Endpoint	Confirmed objective response rate=55.00% (95% CI, 44.00%-65.00%), confirmed complete response rate=1.00%, confirmed partial response=54.00%.
Other Endpoint	Median duration of response (mDOR) = 9.30 months (95% CI, 5.70-14.70), Median progression-free survival (mPFS) = 8.20 months (95% CI, 6.00-11.90), median overall survival=17.80 months (95% CI, 13.80-22.10).
Experiment 7 Reporting the Activity Date of This ADC					[57]
Efficacy Data	Objective Response Rate (ORR)	57.70%	Negative HER2 expression (HER2-; HER2 MFI=10)
Patients Enrolled	HER2-mutated metastatic non-small cell lung cancer (NSCLC).
Administration Dosage	6.40 mg/kg administered by intravenous infusion every 3 weeks (Q3W).
Related Clinical Trial
NCT Number	NCT04644237	Clinical Status	Phase 2
Clinical Description	A phase 2, multicenter, randomized study of trastuzumab deruxtecan in subjects with HER2-mutated metastatic non-small cell lung cancer (NSCLC) (DESTINY-LUNG02).
Primary Endpoint	Confirmed Objective Response Rate=57.70% (95% CI, 43.20-71.30%), Complete Response rate=19.00%, Partial Response=55.80%.
Other Endpoint	Median Duration of Response (mDOR) = 8.70 months (95% Cl 7.10-not estimable).
Experiment 8 Reporting the Activity Date of This ADC					[58]
Efficacy Data	Objective Response Rate (ORR)	60.90%	Positive HER2 expression (HER2+++/++; HER2 MFI=957)
Patients Enrolled	Pathologically documented HER2-positive, unresectable or metastatic breast cancer who had received previous treatment with trastuzumab emtansine.
Administration Dosage	5.4 mg per kilogram administered by intravenous infusion every 3 weeks.
Related Clinical Trial
NCT Number	NCT03248492	Clinical Status	Phase 2
Clinical Description	A phase 2, multicenter, open-label study of DS-8201a, an anti-HER2-antibody drug conjugate (ADC) for HER2-positive, unresectable and/or metastatic breast cancer subjects previously treated with T-DM1 (DESTINY-Breast01).
Primary Endpoint	Confirmed Objective Response Rate=60.90% (95% CI, 53.40%-68.00%), complete response rate=6.00%, partial response rate= 54.90%.
Other Endpoint	Disease-control rate was 97.30% (95% CI, 93.80-99.10), Median Duration of Response (months)=14.80 (95% CI, 13.80-16.90), clinical-benefit rate was 76.10% (95% CI, 69.30-82.10), median duration of progression-free survival was 16.40 months (95% CI, 12.70-not reached), estimated overall survival was 93.90% (95% CI, 89.30-96.60) at 6 months and 86.20% (95% CI, 79.80-90.70) at 12 months.    Click to Show/Hide
Experiment 9 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Objective Response Rate (ORR)	73.33%
Patients Enrolled	HER2-positive breast cancer and newly diagnosed untreated brain metastases or brain metastases progressing after previous local therapy, previous exposure to trastuzumab and pertuzumab and no indication for immediate local therapy.
Administration Dosage	5.40 mg per kg bodyweight once every 3 weeks intravenously.
Related Clinical Trial
NCT Number	NCT04752059	Clinical Status	Phase 2
Clinical Description	Phase 2 study of trastuzumab-deruxtecan (T-DX; DS-8201a) in HER2-positive breast cancer patients with newly diagnosed or progressing brain metastases.
Primary Endpoint	In the ITT population (n=15 patients), intracranial response rate by RANO-BM was 73.33% (95% CI 48.10-89.10%) (11/15 patients; 2 patients in complete remission (13.33%); 9 patients in partial remission (60.00%)). In the per protocol population (PP;n=14 patients), the response rate was 78.57% (95% CI 49.20-95.30%) (11/14). Two patients had stable disease for 6 months and one patient had stable disease at first restaging and progressed after four cycles of trastuzumab deruxtecan. Clinical benefit rate was 13/14 (92.86%; 95% CI 66.10-99.80%) in the PP population.    Click to Show/Hide
Other Endpoint	In patients with extracranial metastases at baseline (n=13), a partial response by RECIST 11 was observed in 5/13 (27.8%; 95% CI 13.9-68.4%) patients, with the remainder having stable disease. None of the patients progressing on trastuzumab deruxtecan had extracranial progression as the first site of progressive disease In patients with measurable extracranial disease at baseline (n=8), a partial remission was observed in 5/8 (62.50%; 95% CI 24.50-91.50%) patients, with the remainder having stable disease.    Click to Show/Hide
Experiment 10 Reporting the Activity Date of This ADC					[60]
Efficacy Data	Objective Response Rate (ORR)	37%	Low HER2 expression (HER2 -)
Patients Enrolled	54 patients with HER2-low breast cancer
Administration Dosage	5.4 or 6.4 mg/kg.
Related Clinical Trial
NCT Number	NCT02564900	Clinical Status	Phase 1
Clinical Description	Phase 1, two-part, multicenter, non-randomized, open-label, multiple dose first-in-human study of DS-8201A, in subjects with advanced solid malignant tumors.
Primary Endpoint	Median duration of response = 10.40 months, median progression free survival (PFS) = 11.10 months, median overall survival = 29.40 months.
Other Endpoint	Confirmed ORR = 24.00 ; DOR, Median=11.00 months; TTR, months Median=2.80 ;PFS, months Median=8.00.
Experiment 11 Reporting the Activity Date of This ADC					[62]
Efficacy Data	Objective Response Rate (ORR)	54.50 70.00 %
Patients Enrolled	Recurrent uterine carcinosarcoma (UCS) with HER2 immunohistochemistry scores 1+ previously treated with chemotherapy were included.
Administration Dosage	6.40 or 5.40 mg/kg was administered intravenously once every 3 weeks.

Experiment 1 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.90%	High HER2 expression (HER2+++; IHC 3+)
Method Description	The antitumor activity of DS-8201a was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 3 mg/kg or 10 mg/kg DS-8201a was i.v. respectively to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX model (PDX: NIBIO G016)
Experiment 2 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.30%	Low HER2 expression (HER2+; IHC 1+)
Method Description	The antitumor activity of DS-8201a was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg DS-8201a was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	Breast cancer PDX model (PDX: ST313)
Experiment 3 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.20%	Low HER2 expression (HER2+; IHC 1+)
Method Description	The antitumor activity of DS-8201a was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg DS-8201a was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	Breast cancer PDX model (PDX: ST565)
Experiment 4 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.60%	Moderate HER2 expression (HER2++; IHC 2+)
Method Description	The antitumor activity of DS-8201a was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg DS-8201a was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	Breast cancer PDX model (PDX: ST225)

Experiment 1 Reporting the Activity Date of This ADC					[78]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Negative HER2 expression (HER2 -)
Method Description	Volume of tumors formed by HCT116-Mock, HCT116-H2L or HCT116-H2H cells in nude mice injected intraperitoneally once every 3 weeks with PBS vehicle or trastuzumab deruxtecan (DS-8201a, 3 mg/kg) beginning at Day 0.
In Vivo Model	HCT116-Mock CDX model
In Vitro Model	Colon carcinoma	HCT 116-Mock cells (Negative HER2 expression)		CVCL_0291
Experiment 2 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 13.50%	Low HER2 expression (HER2+)
Method Description	The antitumor activity of DS-8201a and trastuzumab were evaluated in various mice xenograft models with different HER2 expression levels; CFPAC-1 (low-expression). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 1 mg/kg DS-8201a or 10 mg/kg trastuzumab was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	CFPAC-1 cell line xenograft model
In Vitro Model	Cystic fibrosis	CFPAC-1 cells		CVCL_1119
Experiment 3 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 17.20%	Negative HER2 expression (HER2-)
Method Description	The antitumor activity of DS-8201a was evaluated in various mice xenograft models with different HER2 expression levels; GCIY (negative). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg DS-8201a or Anti-HER2 ADC(same drug-linker as DS-8201a and DAR=3.4) was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	GCIY cell line xenograft model
In Vitro Model	Gastric adenocarcinoma	GCIY cells		CVCL_1228
Experiment 4 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.80%	Positive HER2 expression (HER2+++/++; HER2 MFI=1016)
Method Description	The in vivo antitumor activity of DS-8201a was evaluated in a HER2-positive NCI-N87 xenograft model. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice. The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0 In this group, 0.25 mg/kg DS-8201a was iv to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	HER2-positive NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 58.50%
Method Description	The antitumor activity of DS-8201a was evaluated in various mice xenograft models with different HER2 expression levels; JIMT-1 (moderate positive). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg DS-8201a or Anti-HER2 ADC(same drug-linker as DS-8201a and DAR=3.4) was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	JIMT-1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.60%	Low HER2 expression (HER2+)
Method Description	The antitumor activity of DS-8201a was evaluated in various mice xenograft models with different HER2 expression levels; Capan-1 (weak positive). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg DS-8201a or Anti-HER2 ADC(same drug-linker as DS-8201a and DAR=3.4) was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	Capan-1 cell line xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 7 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.50%	Positive HER2 expression (HER2+++/++; HER2 MFI=1016)
Method Description	The in vivo antitumor activity of DS-8201a was evaluated in a HER2-positive NCI-N87 xenograft model. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice. The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0 In this group, 0.5 mg/kg DS-8201a was iv to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	HER2-positive NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 8 Reporting the Activity Date of This ADC					[78]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.70%	Positive HER2 expression (HER2 +++/++)
Method Description	Trastuzumab deruxtecan (10 mg/kg, every seven days 2) induces efficient tumor cell killing in cell line-derived models of EMT6-hHER2 cells with HER2 expression with high expression.
In Vivo Model	EMT6 CDX model (Expressing hHER2)
In Vitro Model	Mammary gland malignant neoplasms	EMT6 cells (High HER2 expression)		CVCL_1923
Experiment 9 Reporting the Activity Date of This ADC					[78]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 68.70%	Low HER2 expression (HER2 +, IHC 1+)
Method Description	Volume of tumors formed by HCT116-Mock, HCT116-H2L or HCT116-H2H cells in nude mice injected intraperitoneally once every 3 weeks with PBS vehicle or trastuzumab deruxtecan (DS-8201a, 3 mg/kg) beginning at Day 0.
In Vivo Model	HCT116-H2L CDX model
In Vitro Model	Colon carcinoma	HCT 116-H2L cells (Low HER2 expression)		CVCL_0291
Experiment 10 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86%	Positive HER2 expression (HER2+++/++; HER2 MFI=1016)
Method Description	The in vivo antitumor activity of DS-8201a was evaluated in a HER2-positive NCI-N87 xenograft model. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 1 mg/kg DS-8201a was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	HER2-positive NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 11 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.30%	Positive HER2 expression (HER2+++/++; HER2 MFI=95.7)
Method Description	The antitumor activity of DS-8201a was evaluated in various mice xenograft models with different HER2 expression levels; KPL-4 (strong positive). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg DS-8201a or Anti-HER2 ADC(same drug-linker as DS-8201a and DAR=3.4) was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	KPL-4 cell line xenograft model
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310
Experiment 12 Reporting the Activity Date of This ADC					[78]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.10%	High HER2 expression (HER2 +++, IHC 3+)
Method Description	Volume of tumors formed by HCT116-Mock, HCT116-H2L or HCT116-H2H cells in nude mice injected intraperitoneally once every 3 weeks with PBS vehicle or trastuzumab deruxtecan (DS-8201a, 3 mg/kg) beginning at Day 0.
In Vivo Model	HCT116-H2H CDX model
In Vitro Model	Colon carcinoma	HCT 116-H2H cells (High HER2 expression)		CVCL_0291
Experiment 13 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.30%	Positive HER2 expression (HER2+++/++; HER2 MFI=1016)
Method Description	The in vivo antitumor activity of DS-8201a was evaluated in a HER2-positive NCI-N87 xenograft model. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 2 mg/kg DS-8201a was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	HER2-positive NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 14 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.10%	Positive HER2 expression (HER2+++/++; HER2 MFI=1016)
Method Description	The in vivo antitumor activity of DS-8201a was evaluated in a HER2-positive NCI-N87 xenograft model. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 4 mg/kg DS-8201a was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	HER2-positive NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[47]
Efficacy Data	Objective Response Rate (ORR)	21.40%	Positive HER2 expression (HER2 +++/++)
Patients Enrolled	Untreated, asymptomatic BM or controlled brain disease treated with radiotherapy >14 days before enrollment; had received prior HER2-targeted therapy and chemotherapy; and had progressed on or after their most recent treatment of advanced breast cancer.
Administration Dosage	3.6 mg/kg intravenously every 3 weeks.
Related Clinical Trial
NCT Number	NCT01702571	Clinical Status	Phase 3
Clinical Description	A two-cohort, open-label, multicenter study of trastuzumab emtansine (T-DM1) in HER2-positive locally advanced or metastatic breast cancer patients who have received prior anti-HER2 and chemotherapy-based treatment.
Primary Endpoint	Objective response rate=21.40% (95% CI 14.60-29.60), clinical benefit rate=42.90% (95% CI 34.10-52.00).
Other Endpoint	Median PFS=5.50 months (95% CI, 5.30-5.60), overall survival =18.90 months (95% CI, 17.10-21.30).
Experiment 2 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Objective Response Rate (ORR)	5.10%	Positive HER2 expression (HER2+++/++)
Patients Enrolled	HER2 positive advanced urothelial bladder cancer or pancreatic cancer/cholangiocarcinoma
Administration Dosage	Received singleagent TDM1 2.4 mg/kg once weekly (qw) or 3.6 mg/kg every 3 weeks (q3w).
Related Clinical Trial
NCT Number	NCT02999672	Clinical Status	Phase 2
Clinical Description	A study to determine best tumor response with trastuzumab emtansine in human epidermal growth factor receptor 2 (HER2) overexpressing solid tumors (KAMELEON).
Primary Endpoint	BOR, Urothelial bladder cancer (n=13); PR N=5 (38.46%);SD N=1 (7.7%);PD N=6 (46.2%);NE N=1 (7.69%). Pancreatic cancer/cholangiocarcinoma (n=7) PR N=1 (14.29%);SD N=3 (42.86%);PD N=2 (28.57%); NE N=1 (14.29%).
Other Endpoint	PFS, Urothelial bladder cancer (n=13), Median PFS, months (95% CI) 2.20 (1.18-4.30), Median OS, months (95% CI) 7.03 (3.75-NE). Pancreatic cancer/cholangiocarcinoma (n=7), Median PFS, months (95% CI) 2.58 (1.31-9.99), Median OS, months (95% CI) NE (1.45-NE).
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Objective Response Rate (ORR)	5.60%
Patients Enrolled	38 patients were enrolled and 36 included in efficacy analysis.Patients were treated with the standard intravenous dosing of T- DM1, that is 3.6mg/kg every 3 weeks for a 21-day cycle.
Administration Dosage	3.6 mg/kg every 3 weeks for a 21-day cycle, until toxicity or progression.
Related Clinical Trial
NCT Number	NCT02465060	Clinical Status	Phase 2
Clinical Description	Targeted therapy directed by genetic testing in treating patients with advanced refractory solid tumors, lymphomas, or multiple myeloma (the MATCH screening trial).
Primary Endpoint	ORR was 2/36 (5.56%) with 90% confidence interval (90% CI, 1.00% to 16.50%)
Other Endpoint	PFS=23.60%.
Experiment 4 Reporting the Activity Date of This ADC					[54]
Efficacy Data	Objective Response Rate (ORR)	45%	Positive HER2 expression (HER2 +++/++)
Patients Enrolled	An Eastern Cooperative Oncology Group performance status of 0 or 1 and centrally confirmed, measurable, HER2-positive advanced breast cancer previously treated with trastuzumab and a taxane.
Administration Dosage	3.6 mg/kg ( trastuzumab emtansine) and 1200 mg (Atezolizumab) intravenously every 3 weeks.
Related Clinical Trial
NCT Number	NCT02924883	Clinical Status	Phase 2
Clinical Description	A randomized, multicenter, double-blind, placebo-controlled phase II study of the efficacy and safety of trastuzumab emtansine in combination with atezolizumab or atezolizumab-placebo in patients with HER2-positive locally advanced or metastatic breast cancer who have received prior trastuzumab and taxane based therapy.
Primary Endpoint	Median PFS=8.20 months (95% CI 5.80-10.70).
Other Endpoint	Median overall survival was not estimable (95% CI NE-NE); Objective response rate=45.00% (95% CI 28.06-50.30).
Experiment 5 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Objective Response Rate (ORR)	20%	High HER2 expression (HER2+++)
Patients Enrolled	HER2-positive, metastatic breast cancer previously treated with taxane, trastuzumab, and pertuzumab, and were T-DM1-nave.
Administration Dosage	The study consisted of a dose de-escalation (dose-finding) cohort, followed by an expansion cohort at the recommended phase II dose (RP2D), T-DM1 3.60 mg/kg intravenously every 21 days, and pembrolizumab 200mg intravenously every 21 days, if one or fewer DLTs were noted in the first six patients at that dose level, it would be declared the RP2D.
Related Clinical Trial
NCT Number	NCT03032107	Clinical Status	Phase 1b
Clinical Description	A phase 1b study of pembrolizumab in combination with trastuzumab-dm1 in metastatic HER2-positive breast cancer.
Primary Endpoint	OrR=20.00% (95% CI 5.70%-43.70%), and median PFS=9.60 months (95%CI 2.80-16.00 months).
Other Endpoint	There were no dose-limiting toxicities. The RP2D was 3.60 mg/kg T-DM1 plus 200 mg pembrolizumab every 21 days.
Experiment 6 Reporting the Activity Date of This ADC					[63]
Patients Enrolled	Newly diagnosed, HER2-positive, nonmetastatic, histologically confirmed, operable primary invasive breast carcinoma.
Administration Dosage	T-DM1 was dosed at 3.60 mg/kg once every 3 weeks. Trastuzumab was dosed at 6 mg/kg once every 3 weeks after an 8 mg/kg loading dose and started concurrently with the taxane. Pertuzumab was dosed at 420 mg once every 3 weeks after an 840 mg loading dose and administered concurrently with T-DM1 or trastuzumab-plus-taxane. An interval of 3 weeks from the last dose of anthracycline to initiation of HER2-targeted therapy was required. After the taxane-concurrent phase in the trastuzumab-containing arm, trastuzumab-plus-pertuzumab was continued for 1 year. In the T-DM1containing arm, T-DM1-plus-pertuzumab was continued for 1 year.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01966471	Clinical Status	Phase 3
Clinical Description	A randomized, multicenter, open-label, phase 3 trial comparing trastuzumab plus pertuzumab plus a taxane following anthracyclines versus trastuzumab emtansine plus pertuzumab following anthracyclines as adjuvant therapy in patients with operable HER2-positive primary breast cancer.
Primary Endpoint	82 (9.90%) IDFS events had occurred in the AC-THP arm and 80 (9.60%) had occurred in the AC-KP arm.
Other Endpoint	3-year IDFS rates were 94.10% (95% CI, 92.50 to 95.70) with AC-THP and 92.80% (95% CI, 91.00 to 94.50) with AC-KP.

Experiment 1 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 1.10%	Low HER2 expression (HER2+)
Method Description	The antitumor activity of T-DM1 was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	Breast cancer PDX model (PDX: ST565)
Experiment 2 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 19.20%	Low HER2 expression (HER2+)
Method Description	The antitumor activity of T-DM1 was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	Breast cancer PDX model (PDX: ST313)
Experiment 3 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 37.60%	High HER2 expression (HER2+++)
Method Description	The antitumor activity of T-DM1 was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX model (PDX model: NIBIO G016)
Experiment 4 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.20%	Moderate HER2 expression (HER2++)
Method Description	The antitumor activity of T-DM1 was evaluated in various patient-derived xenograft models with different HER2 expression levels. Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	Breast cancer PDX model (PDX: ST225)
Experiment 5 Reporting the Activity Date of This ADC					[77]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.40%	Positive HER2 expression (HER2+++/++)
Method Description	T-DM1 (Genentech) was administered i.p. at 10 mg/kg once per week.
In Vivo Model	Breast cancer PDX model (PDX: PDX12)

Experiment 1 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 7.10%	Low HER2 expression (HER2+)
Method Description	The antitumor activity of T-DM1 was evaluated in various mice xenograft models with different HER2 expression levels; CFPAC-1 (low-expression). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	CFPAC-1 cell line xenograft model
In Vitro Model	Cystic fibrosis	CFPAC-1 cells		CVCL_1119
Experiment 2 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 15.50%	High HER2 expression (HER2+++)
Method Description	The activity of trastuzumab-MCC-DM1 was further investigated in trastuzumab-insensitive mouse xenograft model. After transplantation of MMTV-HER2 Fo5 mammary tumor explants, tumor-bearing nude mice (n = 8 mice per group) were treated once every 3 weeks with 1 mg/kg trastuzmab-MCC-DM1.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus
Experiment 3 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 27.10%	High HER2 expression (HER2+++)
Method Description	Naive female beige nude XID mice were inoculated in the mammary fat pad with 20 million tumor cells suspended in 50% phenol redfree Matrigel mixed with culture medium. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Nude mice with established tumors were dosed i.v. with Tmab-MCC-DM1 0.3 mg/kg for a total of three injections.    Click to Show/Hide
In Vivo Model	Trastuzumab-resistant breast cancer CDX model
In Vitro Model	Invasive breast carcinoma of no special type	BT-474 EEI cells		CVCL_AR96
Experiment 4 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 31.70%	Low HER2 expression (HER2+)
Method Description	The antitumor activity of T-DM1 was evaluated in various mice xenograft models with different HER2 expression levels; Capan-1 (weak positive). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	Capan-1 cell line xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 5 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 33.10%	Negative HER2 expression (HER2-)
Method Description	The antitumor activity of T-DM1 was evaluated in various mice xenograft models with different HER2 expression levels; GCIY (negative). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	GCIY cell line xenograft model
In Vitro Model	Gastric adenocarcinoma	GCIY cells		CVCL_1228
Experiment 6 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 36%	Positive HER2 expression (HER2+++/++)
Method Description	Subcutaneous injection of 100,000 cells mixed in 200 mL PBS solution was performed. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 at a dose of 300 mg/kg via IP injection.
In Vivo Model	SW48 CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 7 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 36%	Low HER2 expression (HER2 +)
Method Description	SW48, HT-29 and LS174T cells were injected into null mice subcutaneously, followed by treatment with cetuximab, trastuzumab and T-DM1. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 at a dose of 300 mg/kg via IP injection.
In Vivo Model	SW48 CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 8 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 42%	Low HER2 expression (HER2+)
Method Description	Subcutaneous injection of 100,000 cells mixed in 200 mL PBS solution was performed. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 (30 mg/kg, once per week i.p.) for 8 weeks.
In Vivo Model	11-18 CDX model
In Vitro Model	Lung adenocarcinoma	11-18 cells		CVCL_6659
Experiment 9 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 42%	Low HER2 expression (HER2 +)
Method Description	11-18 cells (4,000,000 ) and HCC827 cells (2,000,000 ) were injected subcutaneously into the backs on both sides of the mice. T-DM1 (30 mg/kg, once per week i.p.) for 8 weeks.
In Vivo Model	11-18 CDX model
In Vitro Model	Lung adenocarcinoma	11-18 cells		CVCL_6659
Experiment 10 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 43.30%	Positive HER2 expression (HER2 +++/++)
Method Description	Trastuzumab-emtansine (3 mg/kg, every seven days 4) induces efficient tumor cell killing in cell line-derived models of BT-474/R1-7 cells with HER2 expression with high expression.
In Vivo Model	BT-474 CDX model (T-DM1 resistant)
In Vitro Model	Invasive breast carcinoma	BT-474 cells (Trastuzumab emtansine resistant)		CVCL_0179
Experiment 11 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45%	Positive HER2 expression (HER2 +++/++)
Method Description	Trastuzumab-emtansine (3 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of SK-OV-3 cells with HER2 expression with high expression.
In Vivo Model	SK-OV-3 CDX model (Expressing YES1 Y537F)
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells (YES1 Y537F expression)		CVCL_0532
Experiment 12 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.50%	High HER2 expression (HER2+++)
Method Description	Naive female beige nude XID mice were inoculated in the mammary fat pad with 20 million tumor cells suspended in 50% phenol redfree Matrigel mixed with culture medium. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Nude mice with established tumors were dosed i.v. with Tmab-MCC-DM1 1 mg/kg for a total of three injections.    Click to Show/Hide
In Vivo Model	Trastuzumab-resistant breast cancer CDX model
In Vitro Model	Invasive breast carcinoma of no special type	BT-474 EEI cells		CVCL_AR96
Experiment 13 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46.20%	High HER2 expression (HER2+++)
Method Description	The activity of trastuzumab-MCC-DM1 was further investigated in trastuzumab-insensitive mouse xenograft model. After transplantation of MMTV-HER2 Fo5 mammary tumor explants, tumor-bearing nude mice (n = 8 mice per group) were treated once every 3 weeks with 3 mg/kg trastuzmab-MCC-DM1.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus
Experiment 14 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55%	Positive HER2 expression (HER2+++/++)
Method Description	Subcutaneous injection of 100,000 cells mixed in 200 mL PBS solution was performed. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 at a dose of 300 mg/kg via IP injection.
In Vivo Model	HT-29 CDX model
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 15 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55%	Moderate HER2 expression (HER2 ++)
Method Description	SW48, HT-29 and LS174T cells were injected into null mice subcutaneously, followed by treatment with cetuximab, trastuzumab and T-DM1. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 at a dose of 300 mg/kg via IP injection.
In Vivo Model	HT-29 CDX model
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 16 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 58.50%	Moderate HER2 expression (HER2++)
Method Description	The antitumor activity of T-DM1 was evaluated in various mice xenograft models with different HER2 expression levels; JIMT-1 (moderate positive). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	JIMT-1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 17 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 58.70%	High HER2 expression (HER2+++)
Method Description	Naive female beige nude XID mice were inoculated in the mammary fat pad with 20 million tumor cells suspended in 50% phenol redfree Matrigel mixed with culture medium. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Nude mice with established tumors were dosed i.v. with Tmab-MCC-DM1 3 mg/kg for a total of three injections.    Click to Show/Hide
In Vivo Model	Trastuzumab-resistant breast cancer CDX model
In Vitro Model	Invasive breast carcinoma of no special type	BT-474 EEI cells		CVCL_AR96
Experiment 18 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63%	Positive HER2 expression (HER2+++/++)
Method Description	Subcutaneous injection of 100,000 cells mixed in 200 mL PBS solution was performed. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 (30 mg/kg, once per week i.p.) for 8 weeks.
In Vivo Model	H3255 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H3255 cells		CVCL_6831
Experiment 19 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63%	High HER2 expression (HER2 +++)
Method Description	T-DM1 (30 mg/kg, once per week i.p.) for 8 weeks,.
In Vivo Model	H3255 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H3255 cells		CVCL_6831
Experiment 20 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.30%	High HER2 expression (HER2 +++)
Method Description	SW48, HT-29 and LS174T cells were injected into null mice subcutaneously, followed by treatment with cetuximab, trastuzumab and T-DM1. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 at a dose of 300 mg/kg via IP injection.
In Vivo Model	LS174T CDX model
In Vitro Model	Colon adenocarcinoma	LS174T cells		CVCL_1384
Experiment 21 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.70%	Low HER2 expression (HER2+)
Method Description	Subcutaneous injection of 100,000 cells mixed in 200 mL PBS solution was performed. Two weeks after tumour cell injection, mice were treated with trastuzumab, cetuximab or T-DM1 (30 mg/kg, once per week i.p.) for 8 weeks.
In Vivo Model	HCC827 CDX model
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 22 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 74%	High HER2 expression (HER2+++)
Method Description	The activity of trastuzumab-MCC-DM1 was further investigated in trastuzumab-insensitive mouse xenograft model. After transplantation of MMTV-HER2 Fo5 mammary tumor explants, tumor-bearing nude mice (n = 8 mice per group) were treated once every 3 weeks with 10 mg/kg trastuzmab-MCC-DM1.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus
Experiment 23 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 76.54%	Positive HER2 expression (HER2+++/++)
Method Description	Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (1 mg/kg) via the tail vein on Day 0.    Click to Show/Hide
In Vivo Model	KPL-4 CDX model
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310
Experiment 24 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.90%	Positive HER2 expression (HER2+++/++)
Method Description	Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (ADC-211, 1 mg/kg plus ADC-106, 5 mg/kg) via the tail vein on Day 0.    Click to Show/Hide
In Vivo Model	KPL-4 CDX model
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310
Experiment 25 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.90%	High HER2 expression (HER2+++)
Method Description	Mice bearing mammary tumor transplants from the MMTV-HER2 Fo5 line were given a single iv injection (10 mg/kg) of Tmab-SPP-DM1, Tmab-SSNPP-DM3, Tmab-SSNPP-DM4, Tmab-MCC-DM1, or vehicle (n=7 mice per group), and tumor growth was monitored for 25 days.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus
Experiment 26 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.39%	Positive HER2 expression (HER2+++/++)
Method Description	Inoculate 150 mice with KPL-4 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped out into 10 groups of 8-10 mice each. A single treatment will be administered intravenously (ADC-211, 1 mg/kg plus ADC-106, 1 mg/kg) via the tail vein on Day 0.    Click to Show/Hide
In Vivo Model	KPL-4 CDX model
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310
Experiment 27 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.70%	High HER2 expression (HER2+++)
Method Description	The activity of trastuzumab-MCC-DM1 was further investigated in trastuzumab-insensitive mouse xenograft model. After transplantation of MMTV-HER2 Fo5 mammary tumor explants, tumor-bearing nude mice (n = 8 mice per group) were treated once every 3 weeks with 15 mg/kg trastuzmab-MCC-DM1.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus
Experiment 28 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.10%	High HER2 expression (HER2+++)
Method Description	The activity of trastuzumab-MCC-DM1 was further investigated in trastuzumab-insensitive mouse xenograft model. After transplantation of MMTV-HER2 Fo5 mammary tumor explants, tumor-bearing nude mice (n = 8 mice per group) were treated once every 3 weeks with 30 mg/kg trastuzmab-MCC-DM1.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus
Experiment 29 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.70%	High HER2 expression (HER2+++)
Method Description	Naive female beige nude XID mice were inoculated in the mammary fat pad with 20 million tumor cells suspended in 50% phenol redfree Matrigel mixed with culture medium. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Nude mice with established tumors were dosed i.v. with Tmab-MCC-DM1 10 mg/kg for a total of three injections.    Click to Show/Hide
In Vivo Model	Trastuzumab-resistant breast cancer CDX model
In Vitro Model	Invasive breast carcinoma of no special type	BT-474 EEI cells		CVCL_AR96
Experiment 30 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.30%	High HER2 expression (HER2+++)
Method Description	KPL-4 human breast tumor cells were inoculated (3 million cells per mouse, in Matrigel) into the mammary fat pads of SCID beige mice. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Trastuzumab-maytansinoid conjugates were given by single 15 mg/kg iv injection.
In Vivo Model	Breast cancer CDX model
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310
Experiment 31 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.70%	High HER2 expression (HER2+++)
Method Description	Naive female beige nude XID mice were inoculated in the mammary fat pad with 20 million tumor cells suspended in 50% phenol redfree Matrigel mixed with culture medium. All animals were randomly assigned into treatment groups, such that the mean tumor volume for each group was 100 to 200 mm3. Nude mice with established tumors were dosed i.v. with Tmab-MCC-DM1 15 mg/kg for a total of three injections.    Click to Show/Hide
In Vivo Model	Trastuzumab-resistant breast cancer CDX model
In Vitro Model	Invasive breast carcinoma of no special type	BT-474 EEI cells		CVCL_AR96
Experiment 32 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.40%	High HER2 expression (HER2+++)
Method Description	The antitumor activity of T-DM1 was evaluated in various mice xenograft models with different HER2 expression levels; KPL-4 (strong positive). Each cell suspension or tumor fragment was inoculated subcutaneously into specific pathogen-free female nude mice.The tumor-bearing mice were randomized into treatment and control groups based on the tumor volumes, and dosing was initiated on day 0. In this group, 10 mg/kg T-DM1 was i.v. to the tumor-bearing mice.    Click to Show/Hide
In Vivo Model	KPL-4 cell line xenograft model
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310
Experiment 33 Reporting the Activity Date of This ADC					[84]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High HER2 expression (HER2+++)
Method Description	Mice were inoculated subcutaneously in the right flank with either 5x106 cells/mouse of BTC cell line KKU-100, mice were randomized to the control group or treatment with T-DM1 20 mg/kg groups.
In Vivo Model	KMCH-1 CDX model
In Vitro Model	Combined hepatocellular carcinoma and cholangiocarcinoma	KMCH-1 cells		CVCL_7970
Experiment 34 Reporting the Activity Date of This ADC					[85]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive HER2 expression (HER2 +++/++)
Method Description	HER2-positive HCC1954 cells were either treated with vehicle (control) or T-DM1 for 5 days, trypsinized, washed in PBS and sorted by flow cytometry based on the surface ROR1 expression. ROR1- and ROR1+ or unfractionated cells were injected into the subcutaneous site of 6-8-week old Nu/J mice (n=3/group).
In Vivo Model	HCC1954 CDX model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 35 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Minimal Effective Dose (MED)	< 5 mg/kg	Moderate HER2 expression (HER2++)
Method Description	Following the acclimatization period (1 week), the animals were stratified by body weight and randomly assigned to the following group: two T-DM1 groups, treated with 20 mg/kg and 60 mg/kg. Each group consisted of five animals for blood chemistry test as well as five animals for clinical signs and body weight measurements.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 36 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Maximum Tolerated Dose (MTD)	> 20 mg/kg	High HER2 expression (HER2+++)
Method Description	Following the acclimatization period (1 week), the animals were stratified by body weight and randomly assigned to the following group: two T-DM1 groups, treated with 20 mg/kg and 60 mg/kg. Each group consisted of five animals for blood chemistry test as well as five animals for clinical signs and body weight measurements.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.98%	High HER2 expression (HER2 +++)
Method Description	An allograft was propagated from the Fo5 mmty transgenic mouse which does not respond to.or responds poorly to HERCEPTIN therapy. Subjects were treated once with ADC (10 mg/kg); and placebo PBS buffer control (Vehicle) andmonitored over 3 weeks.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5

Experiment 1 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[89]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Low HER2 expression (HER2+; IHC 1+)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. For measurement of apoptosis, BT-474 and SK-BR-3 were exposed to trastuzumab or trastuzumab-DM for 48 h.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[89]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.57 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.76 nM	Moderate HER2 expression (HER2 ++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 8 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.71 nM
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. For measurement of apoptosis, BT-474 and SK-BR-3 were exposed to trastuzumab or trastuzumab-DM for 48 h.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 9 Reporting the Activity Date of This ADC					[89]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.89 nM	High HER2 expression (HER2 +++)
Method Description	To determine the IC50 values of the ADCs, different concentrations of each conjugate was directly added to the culture medium. After the cells were cultured for 3 days at 37°C, the number of viable cells was quantified by using the WST- reagent, and the absorbance was measured at OD450.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 10 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.4 nM	Positive HER2 expression (HER2 +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 11 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.37 nM	Low HER2 expression (HER2+; IHC 1+)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 12 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 13 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2 -)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 14 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	220 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 15 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	317 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 16 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 17 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.00-15.00 ng/mL	High HER2 expression (HER2+++)
Method Description	Exposing mammalian cells having HER2 receptors to ADC in a cell culture medium; culturing the cells for a period from about 6 hours to about 5 days; and measuring cell viability Cell-based in vitro assays were used to measure viability, cytotoxicity, and induction of apoptosis of the ADC of the invention.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 18 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0 ug/mL	Negative HER2 expression (HER2-)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma of no special type	BT-474 EEI cells		CVCL_AR96
Experiment 19 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 ug/mL	Positive HER2 expression (HER2+++/++; HER2 MFI=95.7)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 20 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 ug/mL	Moderate HER2 expression (HER2++; IHC 2+)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Breast inflammatory carcinoma	KPL-4 cells		CVCL_5310
Experiment 21 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 ug/mL	High HER2 expression (HER2+++)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 22 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 ug/mL	High HER2 expression (HER2+++)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 23 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.27 ug/mL	Low HER2 expression (HER2+)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	MKN7 cells		CVCL_1417

Experiment 1 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Tumor-associated calcium signal transducer 2 (TACSTD2)	. . .
Patients Enrolled	Eligibility requires age &ge;18 with ECOG 0-1, HER2+ advanced solid tumors, prior anti-HER2 therapy, and adequate organ function. Key exclusions: LVEF<40%, grade &ge;3 neuropathy, active hepatitis/HIV, recent CYP3A modulators (14 days), anthracycline overexposure, or uncontrolled CNS metastases. Contraception mandated for 6 months post-treatment.
Administration Dosage	DP303c injection, 3.0 mg/kg, every 3 weeks.
Related Clinical Trial
NCT Number	NCT05810103	Clinical Status	PHASE1
Clinical Description	A Multi-center, Single-arm, Phase I Study of DP303c in Patients With HER2-positive Advanced Solid Tumors
Primary Endpoint	Primary pharmacokinetic endpoints include Cmax, AUC0-last, AUC0-inf, and Tmax of the investigational drug measured during multiple dosing cycles (21-day cycles) in patients with HER2-positive advanced solid tumors.
Other Endpoint	Secondary endpoints assess safety (AE incidence over 12 months), efficacy (ORR, DCR, DoR over 12 months), and immunogenicity (ADA/Nab incidence measured during treatment cycles) in this phase I clinical trial.
Experiment 2 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Progression Free Survival	4.44 months
Patients Enrolled	Inclusion: HER2+ (IHC2+/ISH+ or IHC3+) advanced solid tumor patients aged 18-75 with ECOG 0-1, adequate organ function, measurable disease. Exclusion: Active CNS metastases, LVEF<40%, &ge;Grade 2 neuropathy, uncontrolled cardiac/electrolyte disorders, active hepatitis/HIV, recent CYP3A modulators (14 days), or anthracycline exposure &ge;360mg/m2 doxorubicin equivalent. Contraception required for 12 weeks post-treatment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04146610	Clinical Status	PHASE1
Clinical Description	A Phase Ia, Multicenter, Open and Dose-increasing Study of DP303c to Evaluate the Safety , Pharmacokinetics, Immunogenicity and Antitumor Activity of Subjects With HER2-Positive Advanced Solid Tumors
Primary Endpoint	Primary endpoint is MTD determination of DP303c during the first 21-day cycle, defined as the highest dose where <2/6 patients experience DLT in advanced HER2+ solid tumors.
Other Endpoint	Secondary endpoints include PK parameters (Cmax, Tmax, AUC over 2 years), preliminary efficacy (ORR, DoR), and immunogenicity (ADA incidence) in this Phase I study.
Experiment 3 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Objective Response Rate (ORR)	42.90%
Patients Enrolled	Inclusion: HER2+ (IHC2+/ISH+ or IHC3+) advanced solid tumor patients aged 18-75 with ECOG 0-1, adequate organ function, measurable disease. Exclusion: Active CNS metastases, LVEF<40%, &ge;Grade 2 neuropathy, uncontrolled cardiac/electrolyte disorders, active hepatitis/HIV, recent CYP3A modulators (14 days), or anthracycline exposure &ge;360mg/m2 doxorubicin equivalent. Contraception required for 12 weeks post-treatment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04146610	Clinical Status	PHASE1
Clinical Description	A Phase Ia, Multicenter, Open and Dose-increasing Study of DP303c to Evaluate the Safety , Pharmacokinetics, Immunogenicity and Antitumor Activity of Subjects With HER2-Positive Advanced Solid Tumors
Primary Endpoint	Primary endpoint is MTD determination of DP303c during the first 21-day cycle, defined as the highest dose where <2/6 patients experience DLT in advanced HER2+ solid tumors.
Other Endpoint	Secondary endpoints include PK parameters (Cmax, Tmax, AUC over 2 years), preliminary efficacy (ORR, DoR), and immunogenicity (ADA incidence) in this Phase I study.
Experiment 4 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Disease control rate (DCR)	68.10%
Patients Enrolled	Inclusion: HER2+ (IHC2+/ISH+ or IHC3+) advanced solid tumor patients aged 18-75 with ECOG 0-1, adequate organ function, measurable disease. Exclusion: Active CNS metastases, LVEF<40%, &ge;Grade 2 neuropathy, uncontrolled cardiac/electrolyte disorders, active hepatitis/HIV, recent CYP3A modulators (14 days), or anthracycline exposure &ge;360mg/m2 doxorubicin equivalent. Contraception required for 12 weeks post-treatment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04146610	Clinical Status	PHASE1
Clinical Description	A Phase Ia, Multicenter, Open and Dose-increasing Study of DP303c to Evaluate the Safety , Pharmacokinetics, Immunogenicity and Antitumor Activity of Subjects With HER2-Positive Advanced Solid Tumors
Primary Endpoint	Primary endpoint is MTD determination of DP303c during the first 21-day cycle, defined as the highest dose where <2/6 patients experience DLT in advanced HER2+ solid tumors.
Other Endpoint	Secondary endpoints include PK parameters (Cmax, Tmax, AUC over 2 years), preliminary efficacy (ORR, DoR), and immunogenicity (ADA incidence) in this Phase I study.
Experiment 5 Reporting the Activity Date of This ADC					[98]
Patients Enrolled	Inclusion: HER2+ breast cancer patients (IHC 3+ or IHC 2+/ISH+) aged 18-75 with &ge;2 prior anti-HER2 lines (including trastuzumab), measurable disease, ECOG 0-1, LVEF&ge;50%, and adequate organ function. Exclusion: Prior DP303c treatment, active CNS metastases, LVEF<40% history, uncontrolled comorbidities, recent anticancer therapies (4w chemo/2w endocrine), active infections (HBV/HCV), or CYP3A modulator use within 14 days. Contraception required for 6 months post-treatment.    Click to Show/Hide
Administration Dosage	DP303c injection, 3.0 mg/kg, every 3 weeks.
Related Clinical Trial
NCT Number	NCT05334810	Clinical Status	PHASE2
Clinical Description	A Multi-center, Open-lable, Single-arm Phase II Study to Evaluate the Efficacy and Safety of DP303c in Patients With HER2-positive Unresectable Locally Advanced, Relapsed, or Metastatic Breast Cancer
Primary Endpoint	Primary endpoint is ORR assessed by IRC per RECIST v1.1 with tumor evaluations every 6 weeks from baseline.
Other Endpoint	Secondary endpoints include DOR and PFS measured at 6-week intervals from baseline until progression.
Experiment 6 Reporting the Activity Date of This ADC					[99]
Patients Enrolled	Inclusion: HER2+ breast cancer patients (IHC 3+/ISH+) aged &ge;18 with &ge;2 prior systemic therapies, measurable disease, ECOG 0-1, adequate organ function. Exclusion: Pregnancy, recent anticancer treatments (28d systemic/14d TCM therapy), active CNS metastases, LVEF<40%, severe comorbidities (cardiopulmonary/neuropathic/ocular), active infections (HBV/HCV/HIV), or CYP3A modulator use. Contraception required during study participation.    Click to Show/Hide
Administration Dosage	Eligible patients will be treated with trastuzumab IV on day 1 and oral capecitabine twice daily on days 1-14 every 3 weeks, or patients will be treated with trastuzumab IV on day 1 and vinorelbine IV over on days 1 and 8 every 3 weeks.
Related Clinical Trial
NCT Number	NCT05901935	Clinical Status	PHASE3
Clinical Description	A Multicentre, Randomized, Open-label, Controlled Phase III Clinical Study to Evaluate the Efficacy and Safety of DP303cversus Trastuzumab Combined With Vinorelbine/Capecitabine in of HER2-positive Advanced Breast Cancer
Primary Endpoint	Primary endpoint is PFS assessed by BIRC per RECIST v1.1 with follow-up up to 5 years.
Other Endpoint	Secondary endpoints include investigator-assessed PFS, OS, ORR, DoR (all evaluated per RECIST v1.1 over 5 years), and AE incidence/severity monitoring throughout the study period.
Experiment 7 Reporting the Activity Date of This ADC					[100]
Patients Enrolled	Inclusion: HER2+ (IHC3+/ISH+) breast cancer patients &ge;18 years with prior trastuzumab/taxane treatment, ECOG 0-2, adequate organ function. Exclusion: Prior HER2-ADC therapy, active CNS metastases, uncontrolled effusions, Grade&ge;2 neuropathy, recent anticancer therapies (4w immunotherapy/2w chemotherapy), ocular/cardiopulmonary comorbidities, or active infections requiring IV treatment.    Click to Show/Hide
Administration Dosage	DP303c injection, 3.0 mg/kg, Q3W.
Related Clinical Trial
NCT Number	NCT06313086	Clinical Status	PHASE3
Clinical Description	A Multicentre, Randomized, Open-label, Controlled Phase III Clinical Study to Evaluate the Efficacy and Safety of DP303c Versus Trastuzumab Emtansine in Patients With HER2-positive Advanced Breast Cancer
Primary Endpoint	Primary endpoint is BIRC-assessed PFS per RECIST v1.1 with 4-year follow-up in HER2+ advanced/metastatic breast cancer patients.
Other Endpoint	Secondary endpoints include investigator-assessed PFS, OS, ORR, DoR (all per RECIST v1.1) and AE monitoring over 4 years, evaluating both efficacy and safety outcomes.
Experiment 8 Reporting the Activity Date of This ADC					[101]
Patients Enrolled	Eligibility requires age 18-75 with progressed gastric cancer after 1-2 prior therapies (including platinum/fluorouracil), measurable lesions, and organ function adequacy. Key exclusions: trastuzumab intolerance, uncontrolled effusions, active CNS metastases, &ge;Grade 2 neuropathy, recent CYP3A4/UGT1A1 modulator use, or significant ocular/cardiovascular comorbidities.    Click to Show/Hide
Administration Dosage	DP303c injection, dose level 1, intravenous drip, Q3W + simmitinib tablets, dose level 1, oral, QD, taken for 3 weeks, discontinued for 1 week, Q4W
Related Clinical Trial
NCT Number	NCT06577376	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Multicenter, Open-label Phase I/II Clinical Study to Evaluate the Safety and Efficacy of Simmitinib or Irinotecan Liposomes Combined With DP303c Injection in the Treatment of HER2 Expressing Gastric Adenocarcinoma or Gastroesophageal Junction Adenocarcinoma
Primary Endpoint	Primary endpoints include DLT occurrence/incidence, AE/SAE monitoring, and ORR per RECIST 1.1 assessed over 36 months in HER2-positive (IHC 1+/2+/3+) gastric/GEJ adenocarcinoma patients.
Other Endpoint	Secondary outcomes comprise efficacy measures (DCR, DoR, PFS, OS) and pharmacokinetic evaluations (DP303c/simmitinib concentrations, ADA incidence, HER2 expression) tracked for 36 months.
Experiment 9 Reporting the Activity Date of This ADC					[102]
Patients Enrolled	Inclusion: Age 18-75 with histologically confirmed advanced gastric cancer, ECOG 0-1, adequate organ function, measurable lesions (RECIST v1.1), and progression after platinum/taxane-based therapy (HER2-positive cohorts require prior trastuzumab). Exclusion: Active CNS metastases, uncontrolled effusions, &ge;Grade 2 neuropathy, cardiac dysfunction (LVEF<50%), recent CYP3A4 modulators, or prior HER2-ADC therapy. Contraception required for 6 months post-treatment.    Click to Show/Hide
Administration Dosage	Patients with HER2-positive advanced or metastatic gastric cancer after receiving 1st-line treatment will be treated with DP303c injection at 2.0 mg/kg,2.5 mg/kg or 3.0 mg/kg every 3 weeks to determine the recommended dose.
Related Clinical Trial
NCT Number	NCT04826107	Clinical Status	PHASE2
Clinical Description	An Open-label, Multicentre, Phase II Study of DP303c Injection in Patients With Unresectable Locally Advanced, Recurrent or Metastatic Gastric Cancer With HER2 Expression
Primary Endpoint	Primary endpoint is ORR (CR+PR rate) assessed over 2.5 years in HER2-positive/low-expression gastric/GEJ adenocarcinoma patients with progression after ≥1 prior therapy.
Other Endpoint	Secondary endpoints include PFS, OS, DCR, DoR (all measured over 2.5 years) and AE/SAE monitoring, evaluating both efficacy and safety outcomes in this multicenter trial.
Experiment 10 Reporting the Activity Date of This ADC					[103]
Patients Enrolled	Inclusion: Women aged 18-75 with ECOG 0-2, measurable lesions (RECIST v1.1), adequate organ function, and HER2 IHC 1+/2+/3+ status. Exclusion: Active CNS metastases, &ge;Grade 2 neuropathy, LVEF<50%, uncontrolled effusions, recent CYP3A4 modulators (28 days), prior HER2-ADC therapy, or anthracycline exposure >500mg/m2 doxorubicin equivalent. Contraception required for 6 months post-treatment.    Click to Show/Hide
Administration Dosage	Part1:Patients with HER2-expressing advanced ovarian cancer will be treated with DP303c injection at 2.0 mg/kg or 3.0 mg/kg every 3 weeks (Q3W) to determine the recommended phase 2 dose (RP2D).Part2a:Patients with HER2-overexpressing advanced ovarian cancer will be treated with DP303c injection at RP2D.Part2b:Patients with HER2-lowexpressing advanced ovarian cancer will be treated with DP303c injection at RP2D.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04828616	Clinical Status	PHASE2
Clinical Description	An Open-label, Multicentre, Phase II Study of DP303c Injection in Patients With HER2-expressing Advanced Ovarian Cancer
Primary Endpoint	Primary endpoint is ORR (CR+PR rate) assessed over 3 years in HER2-positive/low-expressing ovarian/tubal/peritoneal cancer patients with prior platinum therapy.
Other Endpoint	Secondary endpoints include PFS, OS, DoR (3-year follow-up), AE/SAE monitoring (NCI-CTCAE v5.0), PK parameters (Cmax/Tmax/AUC of DP303c), and ADA incidence in this phase I/II study.
Experiment 11 Reporting the Activity Date of This ADC					[120]
Related Clinical Trial
NCT Number	NCT04826107	Clinical Status	Phase 2
Clinical Description	An open-label, multicentre, phase 2 study of DP303c injection in patients with unresectable locally advanced, recurrent or metastatic gastric cancer with HER2 expression.
Experiment 12 Reporting the Activity Date of This ADC					[121]
Related Clinical Trial
NCT Number	NCT04828616	Clinical Status	Phase 2
Clinical Description	An open-label, multicentre, phase 2 study of DP303c injection in patients with HER2-expressing advanced ovarian cancer.
Experiment 13 Reporting the Activity Date of This ADC					[122]
Related Clinical Trial
NCT Number	NCT05334810	Clinical Status	Phase 2
Clinical Description	A multi-center, open-lable, single-arm phase 2 study to evaluate the efficacy and safety of DP303c in patients with HER2-positive unresectable locally advanced, relapsed, or metastatic breast cancer.
Experiment 14 Reporting the Activity Date of This ADC					[127]
Related Clinical Trial
NCT Number	NCT04146610	Clinical Status	Phase 1
Clinical Description	A phase 1a, multicenter, open and dose-increasing study of DP303c to evaluate the safety , pharmacokinetics, immunogenicity and antitumor activity of subjects with HER2-positive advanced solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 7.60%	Moderate HER2 expression (HER2++)
Method Description	DP001 (10 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 16.20%	Moderate HER2 expression (HER2++)
Method Description	T-DM1 (10 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.47%	High HER2 expression (HER2+++/++)
Method Description	DP001 (10 mg/kg).
In Vivo Model	SK-OV-3 cell line xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 33.60%	High HER2 expression (HER2+++/++)
Method Description	DP001 (10 mg/kg).
In Vivo Model	NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 39%	Moderate HER2 expression (HER2++)
Method Description	DP303c (0.3 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.26%	High HER2 expression (HER2+++/++)
Method Description	DP303c (1 mg/kg).
In Vivo Model	SK-OV-3 cell line xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 54.40%	Moderate HER2 expression (HER2++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 0.1 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 8 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.10%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 1 mg/kg.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 9 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.94%	High HER2 expression (HER2+++/++)
Method Description	DP303c (3 mg/kg).
In Vivo Model	SK-OV-3 cell line xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 10 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.48%	High HER2 expression (HER2+++/++)
Method Description	DP001 (15 mg/kg).
In Vivo Model	HCC1954 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 11 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.60%	High HER2 expression (HER2+++/++)
Method Description	T-DM1 (10 mg/kg).
In Vivo Model	NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 12 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94%	High HER2 expression (HER2+++/++)
Method Description	DP303c (10 mg/kg).
In Vivo Model	NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 13 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94%	High HER2 expression (HER2+++/++)
Method Description	DP303c (5 mg/kg).
In Vivo Model	NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 14 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94%	High HER2 expression (HER2+++/++)
Method Description	DP303c (2.5 mg/kg).
In Vivo Model	NCI-N87 xenograft model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 15 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.10%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 16 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.16%	High HER2 expression (HER2+++/++)
Method Description	T-DM1 (10 mg/kg).
In Vivo Model	SK-OV-3 cell line xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 17 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.30%	High HER2 expression (HER2+++/++)
Method Description	T-DM1 (15 mg/kg).
In Vivo Model	HCC1954 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 18 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97%	High HER2 expression (HER2+++/++)
Method Description	DP303c (3 mg/kg).
In Vivo Model	HCC1954 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 19 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97%	High HER2 expression (HER2+++/++)
Method Description	DP303c (10 mg/kg).
In Vivo Model	HCC1954 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 20 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97%	High HER2 expression (HER2+++/++)
Method Description	DP303c (15 mg/kg).
In Vivo Model	HCC1954 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 21 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.10%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 22 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.50%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 23 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.50%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 2.5 mg/kg.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 24 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.80%	Moderate HER2 expression (HER2++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 1 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 25 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.80%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 26 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.80%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 5 mg/kg.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 27 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.50%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 28 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.54%	High HER2 expression (HER2+++/++)
Method Description	DP303c (10 mg/kg).
In Vivo Model	SK-OV-3 cell line xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 29 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.80%	Moderate HER2 expression (HER2++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 3 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 30 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.10%	High HER2 expression (HER2+++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 15 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 31 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.90%	Moderate HER2 expression (HER2++)
Method Description	Pathogen-free female nude mice were injected subcutaneously with each cell suspension. According to tumor volumes,the mice were randomly divided in two groups: treatment and control groups. Each drug was given to the animals intravenously. The dosing frequency was once a week (qw), qw 2 or qw 3.DP303c induced obvious tumor growth inhibition at a single dose of 10 mg/kg.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 32 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate HER2 expression (HER2++)
Method Description	DP303c (10 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 33 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate HER2 expression (HER2++)
Method Description	DP303c (3 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 34 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate HER2 expression (HER2++)
Method Description	DP303c (1 mg/kg).
In Vivo Model	JIMT -1 cell line xenograft model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Moderate HER2 expression (HER2++; HER2 MFI=157,231)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	High HER2 expression (HER2+++)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	High HER2 expression (HER2+++; HER2 MFI=987,353)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Negative HER2 expression (HER2-; HER2 MFI=256)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 5 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	High HER2 expression (HER2+++)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 6 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	High HER2 expression (HER2+++)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 7 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Negative HER2 expression (HER2-)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	High HER2 expression (HER2+++)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 9 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	High HER2 expression (HER2+++; HER2 MFI=804,573)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 10 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	High HER2 expression (HER2+++; HER2 MFI=892,333)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1 x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1 x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 11 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.39 nM	High HER2 expression (HER2+++)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 12 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.39 nM	Moderate HER2 expression (HER2++)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 13 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	High HER2 expression (HER2+++; HER2 MFI=1,106,494)
Method Description	To obtain a single-cell suspension, the cells were harvested and resuspended. The cell density was adjusted to 1x105 cells/mL and seeded in a 96-well cell culture plate at 100 uL/well (1x104 cells/well). DP303c labeled with DyLight 488 was added into the 96-well plate with a final concentration of 2 ug/mL.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 14 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	High HER2 expression (HER2+++; HER2 MFI=765,629)
Method Description	Comparison of in vitro Activity Between DP303c and T -DM1 in Variable HER2 Cell Lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Progression Free Survival	7 months
Patients Enrolled	Eligible patients were HER2-positive, unresectable/metastatic breast cancer patients progressing after &ge;2 HER2-targeted therapies (including ado-trastuzumab emtansine), with ECOG &le;2 and adequate organ function. Exclusions included prohibited medication use, hypersensitivity to HER2 agents, active pneumonitis, uncontrolled cardiovascular disease (LVEF <50% or elevated troponin), untreated/symptomatic brain metastases, or prior significant lung conditions. Measurable/evaluable disease per RECIST 1.1 was required.    Click to Show/Hide
Administration Dosage	SYD985, every 3 weeks (Q3W)
Related Clinical Trial
NCT Number	NCT03262935	Clinical Status	PHASE3
Clinical Description	A Multi-centre, Open-label, Randomized Clinical Trial Comparing the Efficacy and Safety of the Antibody-drug Conjugate SYD985 to Physician's Choice in Patients With HER2-positive Unresectable Locally Advanced or Metastatic Breast Cancer
Primary Endpoint	Efficacy assessments include progression-free survival (PFS) by central review (RECIST v1.1) and death from randomization through 31March2021, overall survival (OS) monitored until 30June2022, and objective response rate (ORR) via complete/partial responses up to 31March2021. Investigator-assessed PFS and patient-reported quality of life (EORTC QLQ-C30) were also tracked through primary analysis.    Click to Show/Hide
Other Endpoint	Key efficacy endpoints comprised central and investigator-evaluated PFS (both per RECIST v1.1) from randomization until progression/death (primary data cutoff: 31March2021), OS until death (final cutoff: 30June2022), and ORR. Quality of life was measured via EORTC QLQ-C30's 0-100 scale, with positive/negative changes indicating improvement/decline in health status.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Progression Free Survival	9.4 months
Patients Enrolled	Phase I (Part I) enrolls any advanced solid tumor patients refractory to standard therapy, while Phase II (Part II) focuses on HER2-positive breast/gastric/urothelial/endometrial cancers. Key requirements: ECOG &le;1, life expectancy >12 weeks, and adequate organ function. Critical exclusions: recent anthracyclines (<3 months) or cardiotoxicity (LVEF <55% /prior trastuzumab-related declines), active brain metastases, or hypersensitivity to HER2-targeted therapies.    Click to Show/Hide
Administration Dosage	IV (in the vein) infusion every three weeks. Number of Cycles: until cancer progression or unacceptable toxicity develops. Different doses.
Related Clinical Trial
NCT Number	NCT02277717	Clinical Status	PHASE1
Clinical Description	A Two Part First-in-human Phase I Study (With Expanded Cohorts) With the Antibody-drug Conjugate SYD985 to Evaluate the Safety, Pharmacokinetics and Efficacy in Patients With Locally Advanced or Metastatic Solid Tumors
Primary Endpoint	The primary safety endpoint is incidence of dose-limiting toxicities during the first 21-day cycle, establishing the maximum tolerated dose.
Other Endpoint	Secondary outcomes include long-term safety monitoring (AEs over 2 years), pharmacokinetic profiling (AUC and Cmax of SYD985 at multiple timepoints), hematologic/biochemical changes, immunogenicity (anti-drug antibodies), and antitumor activity (ORR assessed every two cycles).
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Objective Response Rate (ORR)	33%
Patients Enrolled	Phase I (Part I) enrolls any advanced solid tumor patients refractory to standard therapy, while Phase II (Part II) focuses on HER2-positive breast/gastric/urothelial/endometrial cancers. Key requirements: ECOG &le;1, life expectancy >12 weeks, and adequate organ function. Critical exclusions: recent anthracyclines (<3 months) or cardiotoxicity (LVEF <55% /prior trastuzumab-related declines), active brain metastases, or hypersensitivity to HER2-targeted therapies.    Click to Show/Hide
Administration Dosage	IV (in the vein) infusion every three weeks. Number of Cycles: until cancer progression or unacceptable toxicity develops. Different doses.
Related Clinical Trial
NCT Number	NCT02277717	Clinical Status	PHASE1
Clinical Description	A Two Part First-in-human Phase I Study (With Expanded Cohorts) With the Antibody-drug Conjugate SYD985 to Evaluate the Safety, Pharmacokinetics and Efficacy in Patients With Locally Advanced or Metastatic Solid Tumors
Primary Endpoint	The primary safety endpoint is incidence of dose-limiting toxicities during the first 21-day cycle, establishing the maximum tolerated dose.
Other Endpoint	Secondary outcomes include long-term safety monitoring (AEs over 2 years), pharmacokinetic profiling (AUC and Cmax of SYD985 at multiple timepoints), hematologic/biochemical changes, immunogenicity (anti-drug antibodies), and antitumor activity (ORR assessed every two cycles).
Experiment 4 Reporting the Activity Date of This ADC					[104]
Patients Enrolled	Eligible patients are &ge;18 with HER2-positive (IHC 1+ for single-arm; IHC 3+/ISH+ for randomized breast cancer cohort) unresectable/metastatic tumors, ECOG &le;1, and adequate organ function. Key exclusions: prohibited medications, trastuzumab hypersensitivity, keratitis, LVEF <50%, pulmonary/cardiovascular diseases, severe systemic illness, or active brain metastases needing steroids/surgery within 8 weeks. Contact lens use is prohibited during treatment.    Click to Show/Hide
Administration Dosage	BYON5667 eye drops should be self-administered daily during waking hours. SYD985, every 3 weeks (Q3W)
Related Clinical Trial
NCT Number	NCT04983238	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Multicenter, Randomized, Double-blind, Placebo-controlled Trial With a Single Arm run-in Period to Evaluate the Safety and Efficacy of Sodium Thiosulfate (BYON5667) Eye Drops to Reduce Ocular Toxicity in Cancer Patients Treated With SYD985
Primary Endpoint	The primary efficacy endpoint evaluates the percentage of patients experiencing SYD985-related ocular adverse events (Grade ≥1) by Day 63 after using BYON5667 eye drops.
Other Endpoint	Secondary assessments include ocular toxicity severity (Day 63/126), tolerability via questionnaire (0-10 discomfort scale), visual function (NEI VFQ-25), time to first ocular AE, discontinuation rates due to toxicity, and SYD985 efficacy/safety endpoints (ORR, PFS, OS, and treatment-emergent AEs) monitored for up to 2 years.
Experiment 5 Reporting the Activity Date of This ADC					[105]
Patients Enrolled	Eligible patients (&ge;18 years) have HER2-positive/low advanced solid tumors (breast, gastroesophageal, etc.), 1-4 prior therapy lines (dependent on subtype), ECOG 0-2, adequate organ function, and measurable disease (expansion cohort). Exclusions: recent anthracyclines, uncontrolled illness, LVEF <50%, active pneumonitis, corneal disease, CNS metastases, or trastuzumab hypersensitivity. Contraception is mandatory.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04602117	Clinical Status	PHASE1
Clinical Description	ISPY-P1.01: Evaluating the Safety of Weekly Paclitaxel With Trastuzumab Duocarmazine (SYD985) in Patients With Metastatic Cancer: A Phase I/Ib Trial
Primary Endpoint	Safety and tolerability of weekly paclitaxel plus tri-weekly trastuzumab duocarmazine (SYD985) will be assessed via CTCAE v5.0 (up to 12 months), focusing on toxicity rates, DLTs, MTD, and RP2D. Preliminary efficacy (RECIST 1.1) includes CBR and ORR at 6 months.
Other Endpoint	Key efficacy endpoints (RECIST 1.1) are PFS and DOR (up to 12 months) in advanced solid tumor patients treated with paclitaxel-SYD985, alongside safety monitoring of treatment-related AEs.
Experiment 6 Reporting the Activity Date of This ADC					[106]
Patients Enrolled	Eligible patients have untreated, measurable (&ge;2.5 cm), stage II-III or non-metastatic stage IV breast cancer, ECOG 0-1, adequate organ function, and meet specific biomarker criteria (e.g., MammaPrint High or ER-/HER2+). Exclusions: prior chemotherapy/radiation, uncontrolled cardiac/medical conditions, pregnancy, or recent investigational drug use within 30 days. MRI-incompatible implants are prohibited.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT01042379	Clinical Status	PHASE2
Clinical Description	I-SPY Trial (Investigation of Serial Studies to Predict Your Therapeutic Response With Imaging And moLecular Analysis 2)
Primary Endpoint	The primary objective is to evaluate if adding experimental agents to standard neoadjuvant chemotherapy improves pathologic complete response (pCR) rates in breast cancer patients, assessed post-surgery after up to 36 weeks of treatment.
Other Endpoint	Secondary goals include developing biomarker-based predictive models for pCR and residual cancer burden (RCB), tracking 3- and 5-year RFS/OS, monitoring treatment-related AEs/SAEs, and assessing tumor dynamics via MRI at four time points (baseline to pre-surgery).
Experiment 7 Reporting the Activity Date of This ADC					[107]
Patients Enrolled	Eligible patients are females with HER2-expressing (IHC 1+/2+/3+ or ISH+) recurrent/metastatic endometrial carcinoma, progressed after first-line platinum therapy (&le;1 prior non-cytotoxic systemic therapy allowed). Key exclusions: LVEF <50%, uncontrolled cardiovascular/pulmonary disease, active brain metastases, or prior trastuzumab hypersensitivity. Measurable disease (RECIST 1.1) and ECOG &le;2 are required.    Click to Show/Hide
Administration Dosage	SYD985, Intravenous, every 3 weeks (Q3W)
Related Clinical Trial
NCT Number	NCT04205630	Clinical Status	PHASE2
Clinical Description	A Single-arm Phase II Trial to Evaluate the Safety and Efficacy of the Antibody-Drug Conjugate (ADC) SYD985 in Patients With Human Epidermal Growth Factor Receptor 2 (HER2)-Expressing Endometrial Carcinoma Who Previously Progressed on or After First Line Platinum-based Chemotherapy
Primary Endpoint	The primary endpoint evaluates Objective Response Rate (ORR) over 2 years, defined as the proportion of patients achieving complete or partial responses per RECIST v1.1 criteria.The primary endpoint evaluates Objective Response Rate (ORR) over 2 years, defined as the proportion of patients achieving complete or partial responses per RECIST v1.1 criteria.    Click to Show/Hide
Other Endpoint	Key secondary endpoints include Progression-Free Survival (PFS) and Overall Survival (OS) over 2 years, measuring time to progression/death and overall mortality, respectively. Treatment-emergent AEs will be graded via CTCAE v5.0.
Experiment 8 Reporting the Activity Date of This ADC					[108]
Patients Enrolled	Eligible patients (&ge;18 years) must have HER2-positive (IHC 1+) advanced/metastatic breast, ovarian, or endometrial cancer (Part 2) or any solid tumor (Part 1) after failing standard therapy, with measurable disease (RECIST 1.1), ECOG &le;1, and adequate organ function. Key exclusions: prior DUBA-ADCs, recent anthracyclines/anticancer therapies, LVEF <50%, significant cardiovascular/pulmonary disease, active brain metastases, or unresolved treatment-related toxicities (>Grade 1). Tumor biopsy (fresh or archival &le;6 months) is mandatory unless unavailable.    Click to Show/Hide
Administration Dosage	SYD985, Intravenous, every 3 weeks (Q3W) Niraparib taken orally and either 100 mg, 200 mg or 300 mg once daily for either 1, 2 or 3 weeks.
Related Clinical Trial
NCT Number	NCT04235101	Clinical Status	PHASE1
Clinical Description	A Two-part Phase I Study With the Antibody-drug Conjugate SYD985 in Combination With Niraparib to Evaluate Safety, Pharmacokinetics and Efficacy in Patients With HER2-expressing Locally Advanced or Metastatic Solid Tumors.
Primary Endpoint	The primary objective is to evaluate dose-limiting toxicities during the first treatment cycle (21-day timeframe) to establish the safety and tolerability profile of the SYD985 and niraparib combination regimen.
Other Endpoint	Secondary objectives include safety assessment (AE incidence over 2 years), pharmacokinetic evaluation (AUC and Cmax of SYD985/niraparib up to 6 months), immunogenicity (anti-SYD985 antibodies), hematologic/clinical chemistry changes, and efficacy (ORR assessed every 2 cycles initially, then every 4 cycles).
Experiment 9 Reporting the Activity Date of This ADC					[119]
Related Clinical Trial
NCT Number	NCT03262935	Clinical Status	Phase 3
Clinical Description	A multi-centre, open-label, randomized clinical trial comparing the efficacy and safety of the antibody-drug conjugate SYD985 to physician's choice in patients with HER2-positive unresectable locally advanced or metastatic breast cancer.
Experiment 10 Reporting the Activity Date of This ADC					[123]
Related Clinical Trial
NCT Number	NCT01042379	Clinical Status	Phase 2
Clinical Description	I-SPY trial (investigation of serial studies to predict your therapeutic response with imaging and molecular analysis 2).
Experiment 11 Reporting the Activity Date of This ADC					[124]
Related Clinical Trial
NCT Number	NCT04205630	Clinical Status	Phase 2
Clinical Description	A single-arm phase 2 trial to evaluate the safety and efficacy of the antibody-drug conjugate (ADC) SYD985 in patients with human epidermal growth factor receptor 2 (HER2)-expressing endometrial carcinoma who previously progressed on or after first line platinum-based chemotherapy.
Experiment 12 Reporting the Activity Date of This ADC					[128]
Related Clinical Trial
NCT Number	NCT02277717	Clinical Status	Phase 1
Clinical Description	A two part first-in-human phase 1 study (with expanded cohorts) with the antibody-drug conjugate SYD985 to evaluate the safety, pharmacokinetics and efficacy in patients with locally advanced or metastatic solid tumors.
Experiment 13 Reporting the Activity Date of This ADC					[129]
Related Clinical Trial
NCT Number	NCT04235101	Clinical Status	Phase 1
Clinical Description	A two-part phase 1 study with the antibody-drug conjugate SYD985 in combination with niraparib to evaluate safety, pharmacokinetics and efficacy in patients with HER2-expressing locally advanced or metastatic solid tumors.
Experiment 14 Reporting the Activity Date of This ADC					[130]
Related Clinical Trial
NCT Number	NCT04602117	Clinical Status	Phase 1
Clinical Description	ISPY-P1.01: evaluating the safety of weekly paclitaxel with trastuzumab duocarmazine (SYD985) in patients with metastatic cancer: a phase 1/Ib trial.
Experiment 15 Reporting the Activity Date of This ADC					[131]
Related Clinical Trial
NCT Number	NCT04983238	Clinical Status	Phase 1
Clinical Description	A multicenter, randomized, double-blind, placebo-controlled trial with a single arm run-in period to evaluate the safety and efficacy of sodium thiosulfate (BYON5667) Eye drops to reduce ocular toxicity in cancer patients treated with SYD985.

Experiment 1 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 33.30%	High HER2 expression (HER2+++; IHC 3+; FISH+)
Method Description	All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model	Breast cancer PDX model (PDX: MAXF-1162)
Experiment 2 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 42.90%	Low HER2 expression (HER2+; IHC +; FISH-)
Method Description	All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model	Breast cancer PDX model (PDX: MAXF 449)
Experiment 3 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65%	Moderate HER2 expression (HER2++; IHC 2+; FISH-)
Method Description	All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model	Breast cancer PDX model (PDX: HBCx-34)
Experiment 4 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.70%	Moderate HER2 expression (HER2++; IHC 2+; FISH-)
Method Description	All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model	Breast cancer PDX model (PDX: ST313)
Experiment 5 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 75%	Low HER2 expression (HER2+; IHC +; FISH-)
Method Description	All treatments were conducted at day 0 by a single dose, i.v, 10 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model	Gastric cancer PDX model (PDX: GXA3057)
Experiment 6 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90%	Moderate HER2 expression (HER2++; IHC 2+; FISH-)
Method Description	All treatments were conducted at day 0 by a single dose, i.v, 10 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model	Gastric cancer PDX model (PDX: GXA3038)
Experiment 7 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High HER2 expression (HER2+++; IHC 3+; FISH+)
Method Description	All treatments were conducted at day 0 by a single dose, i.v, 10 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model	Bladder cancer PDX model (PDX: BXF439)
Experiment 8 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High HER2 expression (HER2+++; IHC 3+; FISH+)
Method Description	All treatments were conducted at day 0 by a single dose, i.v, 10 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model	Gastric cancer PDX model (PDX: GXA3054)
Experiment 9 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate HER2 expression (HER2++; IHC 2+; FISH+)
Method Description	All treatments were conducted at day 0 by a single dose, i.v, 10 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model	Gastric cancer PDX model (PDX: GXA3067)
Experiment 10 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Low HER2 expression (HER2+; IHC +; FISH-)
Method Description	All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model	Breast cancer PDX model (PDX: MAXF-MX1)
Experiment 11 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Low HER2 expression (HER2+; IHC +; FISH-)
Method Description	All treatments were conducted at day 0 by a single dose, i.v, 3 mg/kg x1 injection into the tail vein, Data, depicted as mean tumour volume, consists of 6-8 animals per experimental group.
In Vivo Model	Breast cancer PDX model (PDX: HBCx-10)

Experiment 1 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Objective Response Rate (ORR)	58%
Patients Enrolled	Participants (&ge;18y) must have HER2-altered advanced solid tumors (Phase 1a) or selected HER2-expressing cancers (Phase 1b/2), adequate organ function, and contraception compliance. Exclusions cover recent antitumor therapies (<4 weeks), uncontrolled infections (HIV/HBV/HCV/COVID-19/tuberculosis/syphilis), cardiovascular risks (QTc>480ms, hypertension), or unresolved toxicities (>Grade 1 per CTCAE v5.0).    Click to Show/Hide
Administration Dosage	IBI354 was administered intravenously at 6-15 mg/kg Q3W or Q2W.
Related Clinical Trial
NCT Number	NCT05636215	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Phase 1/2, Multicenter, Open-label Study of IBI354 in Subjects With Locally Advanced Unresectable or Metastatic Solid Tumors
Primary Endpoint	The study assesses safety by tracking serious adverse events (SAEs) and treatment-emergent AEs (TEAEs), defined as any new or worsening clinical incidents occurring up to 30 days post-treatment, along with dose-limiting toxicities (DLTs) within the initial 21-day cycle in Phase Ia.
Other Endpoint	Key efficacy measures include objective response rate (ORR, CR/PR rates), duration of response (DoR, time from response to progression/death), progression-free survival (PFS, time to progression/death), and overall survival (OS, time to death)-all evaluated over a 2-year period.
Experiment 2 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Disease control rate (DCR)	90.90%
Patients Enrolled	Participants (&ge;18y) must have HER2-altered advanced solid tumors (Phase 1a) or selected HER2-expressing cancers (Phase 1b/2), adequate organ function, and contraception compliance. Exclusions cover recent antitumor therapies (<4 weeks), uncontrolled infections (HIV/HBV/HCV/COVID-19/tuberculosis/syphilis), cardiovascular risks (QTc>480ms, hypertension), or unresolved toxicities (>Grade 1 per CTCAE v5.0).    Click to Show/Hide
Administration Dosage	IBI354 was administered intravenously at 6-15 mg/kg Q3W or Q2W.
Related Clinical Trial
NCT Number	NCT05636215	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Phase 1/2, Multicenter, Open-label Study of IBI354 in Subjects With Locally Advanced Unresectable or Metastatic Solid Tumors
Primary Endpoint	The study assesses safety by tracking serious adverse events (SAEs) and treatment-emergent AEs (TEAEs), defined as any new or worsening clinical incidents occurring up to 30 days post-treatment, along with dose-limiting toxicities (DLTs) within the initial 21-day cycle in Phase Ia.
Other Endpoint	Key efficacy measures include objective response rate (ORR, CR/PR rates), duration of response (DoR, time from response to progression/death), progression-free survival (PFS, time to progression/death), and overall survival (OS, time to death)-all evaluated over a 2-year period.
Experiment 3 Reporting the Activity Date of This ADC					[118]
Patients Enrolled	Eligibility requires adult females (&ge;18y, ECOG 0-1) with advanced ovarian cancer, measurable lesions, and adequate organ function. Exclusions involve specific tumor types, recent therapies (chemotherapy/radiotherapy/surgery), uncontrolled comorbidities, infections, prior transplants, or conditions compromising safety/compliance.
Administration Dosage	intravenous infusion of 12 mg/kg on Day 1 of each 3-week treatment cycle
Related Clinical Trial
NCT Number	NCT06834672	Clinical Status	PHASE3
Clinical Description	A Multicenter, Randomized, Open-label Phase III Study of IBI354 Versus Investigator's Choice of Chemotherapy in Patients With Platinum-resistant Ovarian, Primary Peritoneal, or Fallopian Tube Cancer
Primary Endpoint	The primary objectives compare Progression-free Survival (PFS) and Overall Survival (OS) between IBI354 monotherapy and chemotherapy, assessed per RECIST v1.1, with PFS tracked up to 36 months and OS up to 48 months.
Other Endpoint	Secondary endpoints include safety (adverse events, physical exam changes), efficacy (ORR, DCR, DoR, TTR per RECIST v1.1), quality of life (EORTC QLQ-C30/OV28, EQ-5D-5L), pharmacokinetics (Cmax, AUC, Tmax, CL, V, T1/2), and immunogenicity (ADA/Nab incidence and impact on safety/efficacy/PK).

Experiment 1 Reporting the Activity Date of This ADC					[97]
Efficacy Data	Objective Response Rate (ORR)	75.90%
Patients Enrolled	Eligible patients include adults (≥18 years) with HER2-positive/low-expression solid tumors failing standard therapy, measurable lesions (RECIST v1.1), ECOG 0-1, and adequate organ function. Exclusions: recent antitumor therapy (4 weeks/5 half-lives), severe cardiovascular disease, uncontrolled hypertension, active infections, CNS metastasis symptoms, or prior organ transplantation.    Click to Show/Hide
Administration Dosage	This study included subjects with locally advanced or metastatic HER2 expressing (positive/low) breast cancer (BC) and other solid tumors. BL-M07D1 would be administered at doses of 1.0mg/kg Day 1 & Day 8 every 3 weeks (D1D8 Q3W) or 2.6, 3.2, 3.8, 4.4, 5.0, 5.6, 6.2, 6.8 and 7.4 mg/kg Day 1 every 3 weeks (D1Q3W) during dose escalation (D-ESC). A subset of patients (pts) will be enrolled in the dose-expansion phase (D-EXP) at D1 Q3W regimens.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05461768	Clinical Status	PHASE1
Clinical Description	A Phase I Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetic Characteristics, and Preliminary Efficacy of BL-M07D1injection in Patients With Locally Advanced or Metastatic HER2-positive/Low-expression Breast Cancer and Other Solid Tumors
Primary Endpoint	The Phase Ia study evaluates Dose Limiting Toxicity (DLT) and Maximum Tolerated Dose (MTD) over 21 days post-first dose, with MTD selected based on a target DLT rate bound. The Phase Ib study determines the Recommended Phase II Dose (RP2D) using safety, tolerability, efficacy, PK, and PD data from the escalation phase.
Other Endpoint	Key assessments include Treatment-Emergent Adverse Events (TEAEs) over 24 months, PK parameters (Cmax, T1/2, AUC0-t, Tmax, CL, Ctrough) within 21 days, immunogenicity (ADA/Nab), and efficacy measures (ORR, DCR, DOR, PFS) tracked over approximately 24 months.
Experiment 2 Reporting the Activity Date of This ADC					[97]
Efficacy Data	Disease control rate (DCR)	100%
Patients Enrolled	Eligible patients include adults (≥18 years) with HER2-positive/low-expression solid tumors failing standard therapy, measurable lesions (RECIST v1.1), ECOG 0-1, and adequate organ function. Exclusions: recent antitumor therapy (4 weeks/5 half-lives), severe cardiovascular disease, uncontrolled hypertension, active infections, CNS metastasis symptoms, or prior organ transplantation.    Click to Show/Hide
Administration Dosage	This study included subjects with locally advanced or metastatic HER2 expressing (positive/low) breast cancer (BC) and other solid tumors. BL-M07D1 would be administered at doses of 1.0mg/kg Day 1 & Day 8 every 3 weeks (D1D8 Q3W) or 2.6, 3.2, 3.8, 4.4, 5.0, 5.6, 6.2, 6.8 and 7.4 mg/kg Day 1 every 3 weeks (D1Q3W) during dose escalation (D-ESC). A subset of patients (pts) will be enrolled in the dose-expansion phase (D-EXP) at D1 Q3W regimens.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05461768	Clinical Status	PHASE1
Clinical Description	A Phase I Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetic Characteristics, and Preliminary Efficacy of BL-M07D1injection in Patients With Locally Advanced or Metastatic HER2-positive/Low-expression Breast Cancer and Other Solid Tumors
Primary Endpoint	The Phase Ia study evaluates Dose Limiting Toxicity (DLT) and Maximum Tolerated Dose (MTD) over 21 days post-first dose, with MTD selected based on a target DLT rate bound. The Phase Ib study determines the Recommended Phase II Dose (RP2D) using safety, tolerability, efficacy, PK, and PD data from the escalation phase.
Other Endpoint	Key assessments include Treatment-Emergent Adverse Events (TEAEs) over 24 months, PK parameters (Cmax, T1/2, AUC0-t, Tmax, CL, Ctrough) within 21 days, immunogenicity (ADA/Nab), and efficacy measures (ORR, DCR, DOR, PFS) tracked over approximately 24 months.
Experiment 3 Reporting the Activity Date of This ADC					[109]
Patients Enrolled	Enrollment requires HER2+ breast cancer patients (18-75 years) with measurable disease (RECIST 1.1), ECOG 0-1, LVEF &ge;50%, and adequate organ function (INR &le;1.5, urine protein <1000mg/24h). Key exclusions: prior HER2-ADC/camptothecin-ADC treatment, active CNS metastases, cardiovascular risks (QTc prolongation, uncontrolled HTN), ILD history, recent anticancer therapy (varies by modality), infections (HIV/HBV/HCV), anthracycline exposure >360mg/m2, or effusions requiring frequent drainage. Reproductive-age patients must use contraception.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06316531	Clinical Status	PHASE3
Clinical Description	A Randomized Controlled Phase III Clinical Study Comparing BL-M07D1 With T-DM1 in Patients With Unresectable Locally Advanced or Metastatic HER2-positive Breast Cancer
Primary Endpoint	The primary efficacy endpoint is progression-free survival (PFS), evaluated by blinded independent central review (BICR) over 24 months, measuring time from randomization to disease progression or death. Key secondary efficacy measures include overall survival (OS) and objective response rate (ORR) - calculated as complete (CR) and partial responses (PR) proportion in FAS population. Disease control incorporates stable disease (SD) with CR/PR for DCR assessment.    Click to Show/Hide
Other Endpoint	Safety evaluations focus on treatment-emergent adverse events (TEAEs) for 24 months, documenting any clinically significant changes during BL-M07D1 treatment. Immunogenicity is assessed through anti-drug antibody (ADA) frequency. Duration of response (DOR) tracks the period from initial tumor response to progression/death. All efficacy assessments follow RECIST 1.1 criteria, with tumor measurements performed using standardized imaging evaluations.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[110]
Patients Enrolled	Eligible HER2+ breast cancer patients (18-75 years, ECOG 0-1) must have measurable lesions (RECIST 1.1) and adequate organ function (LVEF &ge;50%, INR &le;1.5). Key exclusions involve prior camptothecin-ADC treatment, uncontrolled comorbidities (HTN, QT prolongation), active CNS metastases, recent anticancer therapy (varies by modality), ILD history, anthracycline overdose (>360mg/m2), active infections (HIV/HBV/HCV), or effusions requiring intervention. Reproductive precautions are mandated throughout treatment and for 7 months post-therapy.    Click to Show/Hide
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NCT Number	NCT06445400	Clinical Status	PHASE2
Clinical Description	A Phase II Clinical Trial to Evaluate the Efficacy and Safety of BL-M07D1, BL-M07D1+Pertuzumab and BL-M07D1+Pertuzumab+Docetaxel as First-line Treatment in Patients With Unresectable Locally Advanced or Metastatic HER2-positive Breast Cancer
Primary Endpoint	The study evaluates efficacy through ORR (confirmed CR/PR per RECIST 1.1) and establishes RP2D for BL-M07D1 by integrating safety, tolerability, and pharmacokinetic/pharmacodynamic data from dose escalation. Primary endpoints include tumor response assessment with CR defined as target lesion disappearance and PR as ≥30% reduction in lesion diameter sum.    Click to Show/Hide
Experiment 5 Reporting the Activity Date of This ADC					[111]
Patients Enrolled	Eligible participants are women (18-75 years) with AJCC 8th edition stage T1-4/N0-3 M0 (excluding T1N0) HER2+ invasive breast cancer who completed neoadjuvant therapy and mastectomy, showing residual disease. Exclusions include metastatic disease, prior HER2-ADC therapy, anthracycline overdose (>240mg/m2 doxorubicin equivalent), uncontrolled comorbidities (cardiac/pulmonary disorders, HTN), active infections (HIV/HBV/HCV), or immunosuppressive therapy use. Strict reproductive safeguards are enforced throughout the study period.    Click to Show/Hide
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NCT Number	NCT06830889	Clinical Status	PHASE3
Clinical Description	A Randomized Controlled Phase Ill Clinical Study of BL-M07D1 for Injection Versus Trastuzumab Emtansine (T-DM1) in the Adjuvant Treatment of HER2-positive Breast Cancer With Residual Invasive Cancer After Neoadjuvant Therapy
Primary Endpoint	The primary endpoint is invasive disease-free survival (IDFS), assessing freedom from invasive breast cancer recurrence over 77 months following treatment, ensuring long-term therapeutic efficacy in HER2-positive patients post-neoadjuvant therapy and surgery.
Other Endpoint	Secondary endpoints evaluate disease-free survival (DFS), distant recurrence-free interval (DRFI), and overall survival (OS). Treatment-emergent adverse events (TEAEs) are rigorously monitored per NCI-CTCAE v5.0 criteria, documenting any clinically significant changes during BL-M07D1 administration to assess safety profile over the 77-month follow-up.    Click to Show/Hide
Experiment 6 Reporting the Activity Date of This ADC					[112]
Patients Enrolled	Eligibility requires adults (&ge;18 years) with HER2-expressing (IHC 1+/3+ or gene-amplified) advanced/metastatic solid tumors (e.g., endometrial, breast, gastric cancers) refractory to &ge;2 prior therapies, measurable lesions (RECIST v1.1), ECOG 0-1, and adequate organ function (LVEF &ge;50%, INR/APTT &le;1.5&times;ULN). Exclusions cover recent antitumor therapies (chemotherapy/surgery within 2-6 weeks), uncontrolled comorbidities (QTc >470ms, hypertension, Grade 3 lung disease), active infections (HIV/HBV/HCV), prior anthracyclines (>360mg/m2), CNS metastases unless stable &ge;4 weeks, and allergies to BL-M07D1 components. Reproductive safeguards are mandated.    Click to Show/Hide
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NCT Number	NCT06293898	Clinical Status	PHASE1
Clinical Description	A Phase 1 Open-Label Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Efficacy of BL-M07D1 in Subjects With HER2 Expressing Advanced Malignant Solid Tumors
Primary Endpoint	The study assesses safety parameters including dose-limiting toxicities (DLTs), serious adverse events (SAEs), treatment-emergent AEs (TEAEs), physical exams, vital signs, lab results, ECG, and echocardiograms over 24 months. Key dose objectives include identifying the maximum tolerated dose (MTD) or maximum administered dose (MAD) and at least two recommended expansion doses (RDEs) of BL-M07D1 based on DLT evaluation within 21 days.    Click to Show/Hide
Experiment 7 Reporting the Activity Date of This ADC					[113]
Patients Enrolled	Eligible patients (18-75 years) have HER2-positive/IHC2+/ISH+ or low-expressing (IHC1+/2+ISH-) advanced solid tumors refractory to standard therapy, measurable lesions (RECIST v1.1), ECOG 0-1, and adequate organ function (LVEF&ge;50%, ANC&ge;1.5&times;10<sup>9</sup>/L). Exclusions cover recent antitumor therapies (4 weeks/5 half-lives), cardiovascular risks (QTc>450/470ms, NYHA&ge;2), active infections (HIV/HBV/HCV), prior topoisomerase I inhibitor ADCs (Phase Ib), uncontrolled effusions, or CNS metastases unless stable >4 weeks post-treatment. Reproductive safeguards are mandatory.    Click to Show/Hide
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NCT Number	NCT05631964	Clinical Status	PHASE1
Clinical Description	A Phase I Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetic Characteristics, and Initial Efficacy of BL-M07D1 for Injection in Patients With Locally Advanced or Metastatic Digestive Tract Tumors and Other Solid Tumors
Primary Endpoint	Phase Ia investigates Dose-Limiting Toxicity (DLT) incidence/severity (NCI-CTCAE v5.0) within 21 days post-dosing to determine Maximum Tolerated Dose (MTD), defined as the highest dose below target DLT rate threshold. Phase Ib establishes Recommended Phase II Dose (RP2D) based on integrated safety, efficacy, PK/PD data from escalation studies.
Other Endpoint	Key outcomes include Treatment-Emergent Adverse Events (TEAEs, 24-month monitoring) and pharmacokinetic metrics (Cmax, Tmax, T1/2, AUC0-t, CL, Ctrough within 21 days). Immunogenicity (anti-drug antibody frequency/titer) and efficacy endpoints (ORR, DCR, DOR, PFS, OS per RECIST 1.1) are tracked over 24 months to assess BL-M07D1's therapeutic profile.    Click to Show/Hide
Experiment 8 Reporting the Activity Date of This ADC					[114]
Patients Enrolled	Eligible participants (&ge;18 years) have HER2-positive (IHC3+/IHC2+FISH+) or low-expressing (IHC1+/IHC2+FISH-) advanced solid tumors refractory to standard therapy, measurable lesions (RECIST v1.1), ECOG 0-1, and adequate organ function (LVEF&ge;50%; ANC&ge;1.5&times;10<sup>9</sup>/L). Exclusions include recent antitumor therapies (4 weeks/5 half-lives), severe cardiovascular conditions (QTc>450/470ms, NYHA&ge;II), active infections (HIV/HBV/HCV), uncontrolled effusions, prior topoisomerase I inhibitor ADCs, or CNS metastases. Reproductive precautions are mandatory.    Click to Show/Hide
Administration Dosage	BL-M07D1 was administered by intravenous infusion every 3 weeks in 3-week cycles.
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NCT Number	NCT06031584	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Phase Ib/II Clinical Study to Evaluate the Safety and Efficacy of BL-M07D1 for Injection in Patients With Locally Advanced or Metastatic HER2-positive/Low-expressing Urinary and Gastrointestinal Solid Tumors
Primary Endpoint	The Phase Ib study determines the Recommended Phase II Dose (RP2D) of BL-M07D1 based on integrated safety, tolerability, efficacy, pharmacokinetic (PK), and pharmacodynamic (PD) data over 24 months. Phase II primarily evaluates Objective Response Rate (ORR) per RECIST 1.1, defined as the proportion of participants achieving complete response (CR) or partial response (PR).    Click to Show/Hide
Other Endpoint	Safety and efficacy outcomes include Treatment-Emergent Adverse Events (TEAEs, assessing type/frequency/severity over 24 months), ORR, Disease Control Rate (DCR), Duration of Response (DOR), Progression-Free Survival (PFS), and pharmacokinetic metrics (Cmax, Tmax, T1/2, AUC0-t, CL, Ctrough). Anti-drug antibody (ADA) frequency and titer are monitored to evaluate immunogenicity.    Click to Show/Hide
Experiment 9 Reporting the Activity Date of This ADC					[115]
Patients Enrolled	Eligibility includes HER2-positive gastric/gastroesophageal junction adenocarcinoma patients (&ge;18 years, ECOG 0-1) with &ge;1 measurable lesion (RECIST v1.1), adequate organ function (LVEF&ge;50%), and managed toxicity (&le;CTCAE grade 1). Exclusions: recent antitumor therapy (<4 weeks), severe cardiovascular conditions, active metastases, significant effusions, uncontrolled infections, autoimmune diseases, or prior topoisomerase I inhibitor ADC treatment. Strict contraception and pregnancy testing are required.    Click to Show/Hide
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NCT Number	NCT06423885	Clinical Status	PHASE2
Clinical Description	A Phase II Clinical Study to Evaluate the Efficacy and Safety of BL-M07D1 Combination Therapy in Patients With Unresectable Locally Advanced or Metastatic HER2-positive Gastric or Gastroesophageal Junction Adenocarcinoma
Primary Endpoint	This clinical trial evaluates BL-M07D1's efficacy through Objective Response Rate (ORR) per RECIST 1.1 (CR/PR rates) and establishes the Recommended Phase II Dose (RP2D) based on comprehensive safety, tolerability, efficacy, PK, and PD data collected during dose escalation studies over a 24-month period.
Other Endpoint	Key secondary endpoints include Progression-Free Survival (PFS), Disease Control Rate (DCR), Duration of Response (DOR), and Treatment-Emergent Adverse Events (TEAEs), all assessed over 24 months. TEAEs monitoring includes evaluating type, frequency, and severity of adverse changes during BL-M07D1 treatment, providing essential safety data for therapeutic assessment.    Click to Show/Hide
Experiment 10 Reporting the Activity Date of This ADC					[116]
Patients Enrolled	Eligible participants must be females aged 18-75 with recurrent/metastatic HER2-positive/low-expression gynecologic malignancies, measurable lesions per RECIST 1.1, ECOG 0-1, and adequate organ function. Exclusions include prior topoisomerase I inhibitor ADC therapy, uncontrolled cardiovascular disease, active infections, CNS metastases, recent clinical trial participation, pregnancy/lactation, or conditions deemed unsuitable by investigators.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06131450	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Phase Ib/II Clinical Trial to Evaluate the Safety, Tolerability, Pharmacokinetics and Efficacy of BL-M07D1 for Injection in Patients With HER2-expressing Recurrent or Metastatic Gynecologic Malignancies
Primary Endpoint	In Phase Ib, the Recommended Phase II Dose (RP2D) will be determined based on safety, tolerability, efficacy, PK, and PD data from the dose escalation study of BL-M07D1. In Phase II, the Objective Response Rate (ORR) will measure the percentage of participants achieving complete response (CR) or partial response (PR) per RECIST 1.1 criteria over approximately 24 months.    Click to Show/Hide
Other Endpoint	Treatment-Emergent Adverse Events (TEAEs) will be monitored for changes in body structure, function, or chemistry during BL-M07D1 treatment. Secondary endpoints include ORR, Disease Control Rate (DCR), Duration of Response (DOR), Progression-Free Survival (PFS), pharmacokinetic parameters (Cmax, Tmax, Ctrough), and anti-drug antibody (ADA) frequency over approximately 24 months.    Click to Show/Hide
Experiment 11 Reporting the Activity Date of This ADC					[117]
Patients Enrolled	Eligibility requires confirmed unresectable HER2-mutated NSCLC (stage IIIB/IV), prior platinum/immunotherapy failure, ECOG 0-1, and adequate organ function. Exclusions include recent antitumor therapy, severe cardiopulmonary disease, active infections, CNS metastases requiring treatment, or allergies to BL-M07D1 components.
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NCT Number	NCT06114511	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Phase Ib/II Clinical Trial to Evaluate the Safety, Tolerability, Pharmacokinetics and Efficacy of BL-M07D1 for Injection in Patients With HER2 Mutated, Locally Advanced or Metastatic Non-small Cell Lung Cancer (NSCLC)
Primary Endpoint	The Phase Ib study focuses on determining the Recommended Phase II Dose (RP2D) of BL-M07D1, based on safety, tolerability, efficacy, PK, and PD data within 21 days post-first dose. The Phase II primary endpoint is Objective Response Rate (ORR), assessing complete (CR) or partial response (PR) per RECIST 1.1 over approximately 24 months.
Other Endpoint	Key secondary endpoints include Treatment-Emergent Adverse Events (TEAEs), Disease Control Rate (DCR), Duration of Response (DOR), Progression-Free Survival (PFS), pharmacokinetic measures (Cmax, Tmax, Ctrough), and Anti-Drug Antibody (ADA) incidence, all evaluated over ~24 months except PK parameters (21 days post-dose).
Experiment 12 Reporting the Activity Date of This ADC					[125]
Patients Enrolled	Patients with locally advanced or metastatic HER2-positive/low-expression breast cancer and other solid tumors.
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NCT Number	NCT05461768	Clinical Status	Phase 1
Clinical Description	A phase 1 clinical study to evaluate the safety, tolerability, pharmacokinetic characteristics, and preliminary efficacy of BL-M07D1 injection in patients with locally advanced or metastatic HER2-positive/low-expression breast cancer and other solid tumors.
Experiment 13 Reporting the Activity Date of This ADC					[126]
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NCT Number	NCT05631964	Clinical Status	Phase 1
Clinical Description	A phase 1 clinical study to evaluate the safety, tolerability, pharmacokinetic characteristics, and initial efficacy of BL-M07D1 for injection in patients with locally advanced or metastatic digestive tract tumors and other solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[134]
Patients Enrolled	This study enrolls patients with histologically confirmed advanced/metastatic solid tumors (Part 1) or HER2-overexpressing breast cancer (Cohort A) and gastric/GEJ adenocarcinoma (Cohort B) (Part 2) who failed prior HER2-targeted therapies. Key requirements include: signed informed consent; LVEF &ge;50%; ECOG PS 0-1; life expectancy &ge;3 months; adequate hematologic (ANC &ge;1.5&times;10<sup>9</sup>/L, platelets &ge;100&times;10<sup>9</sup>/L, Hb &ge;90g/L), hepatic (bilirubin &le;1.5&times;ULN, AST/ALT &le;3&times;ULN [&le;5&times;ULN if liver mets]), renal (creatinine &le;1.5&times;ULN or CrCl &ge;60mL/min), and coagulation (INR/PT/APTT &le;1.5&times;ULN) parameters; measurable lesions (required in Part 2, preferred in Part 1); recovery from prior treatment toxicities (CTCAE v5.0 &le;1); and use of effective contraception. Female participants require negative pregnancy testing within 7 days prior to enrollment.    Click to Show/Hide
Administration Dosage	FDA022-BB05, intravenously infusion, q3w
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NCT Number	NCT05564858	Clinical Status	PHASE1
Clinical Description	A PhaseIStudy to Evaluate the Safety, Tolerability, Pharmacokinetics and Efficacy of FDA022-BB05 in Subjects With Advanced Solid Malignant Tumors
Primary Endpoint	The study evaluates dose-limiting toxicity (DLT) per NCI CTCAE v5.0 during Cycle 1 (21 days), with maximum tolerated dose (MTD) defined as the highest dose where ≤1 of 3 patients experience DLT within this observation window. Treatment-related adverse events (AEs) and serious adverse events (SAEs) will be monitored for up to 3 years using NCI CTCAE v5.0 criteria, while the recommended Phase II dose (RP2D) will be determined based on Cycle 1 (21-day) safety data.    Click to Show/Hide
Other Endpoint	The study will assess pharmacokinetic (PK) parameters including peak plasma concentration (Cmax), time to peak concentration (Tmax), area under the curve (AUC), half-life (t1/2), and apparent clearance (CL/F) from Cycle 1 to Cycle 10 (21-day cycles). Immunogenicity will be evaluated through anti-drug antibody (ADA) formation up to 18 months. Efficacy measures include objective response rate (ORR), progression-free survival (PFS), and duration of response (DoR) assessed up to 18 months, with overall survival (OS) monitored for up to 3 years. All PK and safety data will be collected during the 21-day treatment cycles.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[135]
Administration Dosage	Enrolled Subjects will receive a 5.4 mg/kg IV dose of FDA022-BB05 on Day 1 of each cycle Q3W
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NCT Number	NCT06413615	Clinical Status	PHASE2
Clinical Description	A Phase 2, Multicenter, Open-Label Study to Assess the Efficacy, Safety, Tolerability and Pharmacokinetics of FDA022-BB05 in Patients with Advanced/Metastatic Solid Tumors
Primary Endpoint	This clinical trial will evaluate efficacy and safety outcomes over a 24-month period. The primary efficacy endpoint is objective response rate (ORR), defined as the proportion of patients achieving complete response (CR) or partial response (PR) per investigator assessment using RECIST v1.1 criteria. Safety monitoring will include comprehensive evaluation of all adverse events (AEs) and serious adverse events (SAEs), with severity graded according to NCI CTCAE version 5.0 standards throughout the study duration. Both ORR and AE/SAE data will be systematically collected and analyzed to assess the treatment's clinical benefit-risk profile.    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[149]
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NCT Number	NCT05564858	Clinical Status	Phase 1
Clinical Description	A phase study to evaluate the safety, tolerability, pharmacokinetics and efficacy of FDA022-BB05 in subjects with advanced solid malignant tumors.

Experiment 1 Reporting the Activity Date of This ADC					[136]
Patients Enrolled	Eligible patients (18-75yo females) must have HER2+ metastatic breast cancer refractory to anti-HER2 therapy with ECOG 0-1, adequate organ function, and measurable disease. Key exclusions include recent anti-HER2 therapy (T-DM1/trastuzumab within 3 months), anthracycline overdose (doxorubicin >450mg/m2 equivalent), uncontrolled comorbidities (cardiac dysfunction LVEF<50%, NYHA III-IV, uncontrolled HTN, active bleeding disorders), hepatitis/HIV, symptomatic brain metastases, or lab abnormalities (neutrophils <1.5&times;109/L, platelets <100&times;109/L, ALT/AST >2.5&times;ULN). Pregnancy prevention is mandatory for 6 months post-treatment.    Click to Show/Hide
Administration Dosage	Usage: Intravenous infusion; Dose escalation stage: doses 0.6, 1.2, 2.4, 3.6, 4.8 mg / kg, 1-6subjects each. Dose expansion stage: 20 subjects are enrolled and take the recommended dose based on the result of dose escalation stage.
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NCT Number	NCT03953833	Clinical Status	PHASE1
Clinical Description	Phase I Clinical Trial on the Safety, Tolerability, Pharmacokinetics of B003 in the Treatment of HER2-positive Recurrent or Metastatic Breast Cancer
Primary Endpoint	The study will determine the MTD of B003 over 2 years by assessing DLTs during the first 21-day cycle, with extensive PK profiling including Tmax, Cmax, t½, MRT, AUC, elimination rate and CL/F. Immunogenicity will track ADA incidence and titers, while efficacy endpoints measure ORR, DCR, DOR and PFS over 14 months per RECIST v1.1 criteria, requiring confirmation of responses at 4 weeks.    Click to Show/Hide
Experiment 2 Reporting the Activity Date of This ADC					[137]
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1) must have failed standard therapy, measurable lesions, adequate organ function, and controlled toxicities. Exclusion criteria involve recent chemotherapy/radiotherapy, severe comorbidities, active infections, CNS metastases, unresolved ILD, or prior topoisomerase I inhibitors. Strict lab and clinical stability requirements apply.    Click to Show/Hide
Administration Dosage	BL-B01D1 was administered by intravenous infusion on D1 and D8 in a 3-week cycle.
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NCT Number	NCT06042894	Clinical Status	PHASE2
Clinical Description	A Phase II Clinical Trial to Evaluate the Efficacy and Safety of SI-B003 Monotherapy or BL-B01D1+SI-B003 Combination Therapy (BL-B01D1+SI-B003) in Patients With Unresectable Locally Advanced or Recurrent Metastatic HER2 Negative Breast Cancer
Primary Endpoint	The study evaluates ORR (percentage achieving CR/PR per RECIST 1.1) and RP2D (dose determined by sponsor based on safety, efficacy, PK/PD data) over 24 months in HER2-negative breast cancer patients.
Other Endpoint	Key endpoints include PFS (time to progression/death), DCR (percentage with CR/PR/SD per RECIST 1.1), DOR (response duration till progression/death), and TEAEs (adverse events during treatment) tracked over 24 months.
Experiment 3 Reporting the Activity Date of This ADC					[138]
Patients Enrolled	Eligible participants include women aged 18-75 with gynecological malignancies, adequate organ function, and measurable lesions per RECIST 1.1. Key exclusions involve prior ADC therapy, recent antineoplastic treatment, severe comorbidities, uncontrolled infections, active CNS metastases, or conditions deemed unsuitable by investigators.
Administration Dosage	BL-B01D1 was administered by intravenous infusion on D1 and D8 in a 3-week cycle.
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NCT Number	NCT05990803	Clinical Status	PHASE2
Clinical Description	A Phase II Clinical Study to Evaluate the Efficacy and Safety of BL-B01D1 Monotherapy, SI-B003 Monotherapy and BL-B01D1+SI-B003 Combination Therapy (BL-B01D1+SI-B003) in Patients With Recurrent or Metastatic Cervical Cancer and Other Gynecological Malignancies
Primary Endpoint	The primary endpoints include Objective Response Rate (ORR), defined as the percentage of participants achieving complete or partial response per RECIST 1.1, and the Recommended Phase II Dose (RP2D), determined based on safety, tolerability, and efficacy data during dose escalation.
Other Endpoint	Secondary endpoints comprise Progression-Free Survival (PFS), measuring time from treatment initiation to disease progression or death; Disease Control Rate (DCR), capturing stable disease or better responses; Duration of Response (DOR), tracking sustained responses; and Treatment-Emergent Adverse Events (TEAEs), assessing safety profiles.
Experiment 4 Reporting the Activity Date of This ADC					[139]
Patients Enrolled	Eligible participants (18-75 years) must have locally advanced/metastatic gastrointestinal cancer, measurable lesions (RECIST 1.1), ECOG 0-1, and adequate organ function. Key exclusions: prior topoisomerase I inhibitor ADCs, recent antitumor therapy (4 weeks/5 half-lives), severe cardiac/autoimmune diseases, active infections, uncontrolled effusions, CNS metastases, or conditions compromising trial safety per investigator judgment.    Click to Show/Hide
Administration Dosage	Administered by intravenous infusion for a cycle of 3 weeks.
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NCT Number	NCT06008054	Clinical Status	PHASE2
Clinical Description	A Phase II Clinical Study to Evaluate the Efficacy and Safety of SI-B003 Monotherapy, BL-B01D1+SI-B003 Combination Therapy and BL-B01D1+PD-1 Monoclonal Antibody in Patients With Locally Advanced or Metastatic Esophageal Cancer, Gastric Cancer, Colorectal Cancer and Other Gastrointestinal Tumors
Primary Endpoint	The primary endpoints are Objective Response Rate (ORR), defined as the proportion of participants achieving complete or partial response per RECIST 1.1, and Recommended Phase II Dose (RP2D), determined by sponsor-investigator consensus based on safety, tolerability, efficacy, pharmacokinetics, and pharmacodynamics data during dose escalation.
Other Endpoint	Secondary endpoints include Progression-Free Survival (PFS, time from first dose to progression/death), Disease Control Rate (DCR, percentage with CR/PR/SD per RECIST 1.1), Duration of Response (DOR, time from response to progression/death), and Treatment-Emergent Adverse Events (TEAEs, monitoring safety profiles during therapy).
Experiment 5 Reporting the Activity Date of This ADC					[140]
Patients Enrolled	Eligible patients (18-75 years) must have locally advanced/metastatic head and neck squamous cell carcinoma (excluding nasopharyngeal primary), measurable lesions (RECIST 1.1), ECOG &le;1, and adequate organ function. Key exclusions: active CNS metastases, recent anticancer therapy (4 weeks/5 half-lives), uncontrolled hypertension/cardiac conditions, autoimmune diseases, organ transplant history, HIV/HBV/HCV infection, or prior grade &ge;3 immune-related adverse events from immunotherapy.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05668858	Clinical Status	PHASE1|||PHASE2
Clinical Description	Phase Ib/II Clinical Study of SI-B001+SI-B003 Dual-drug No-combination or Combined Chemotherapy in Patients With Locally Advanced or Metastatic Head and Neck Squamous Cell Carcinoma
Primary Endpoint	The Phase Ib study evaluates dose-limiting toxicity (DLT) and determines the maximum tolerated dose (MTD) and recommended Phase II dose (RP2D) for SI-B001+SI-B003 combination therapy based on safety, efficacy, and pharmacokinetic data. Primary efficacy endpoint is objective response rate (ORR), defined per RECIST 1.1 as complete/partial response rates through 24 months.    Click to Show/Hide
Other Endpoint	Safety and efficacy outcomes include treatment-emergent adverse events (TEAEs), disease control rate (DCR), duration of response (DOR), and progression-free survival (PFS) across both phases. Pharmacokinetic measures - Cmax, Tmax, half-life (T1/2), AUC, clearance (CL), trough levels (Ctrough) - and immunogenicity (anti-drug/neutralizing antibodies) will be analyzed for both investigational compounds.    Click to Show/Hide
Experiment 6 Reporting the Activity Date of This ADC					[141]
Patients Enrolled	Eligible participants (18-75 years) must have recurrent/metastatic HNSCC (excluding nasopharyngeal) with measurable lesions (RECIST 1.1), ECOG 0-1, and adequate organ function. Key exclusions: prior topoisomerase I inhibitor ADC treatment, recent anticancer therapy (4 weeks/5 half-lives), uncontrolled cardiovascular/autoimmune conditions, active infections, symptomatic CNS metastases/effusions, or positive HIV/HBV/HCV status with high viral loads.    Click to Show/Hide
Administration Dosage	BL-B01D1 was administered by intravenous infusion on D1, D8, or D1 in 3-week cycles.
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NCT Number	NCT06006169	Clinical Status	PHASE2
Clinical Description	A Phase II Clinical Trial to Evaluate the Efficacy and Safety of BL-B01D1 Monotherapy, SI-B003 Monotherapy and BL-B01D1+SI-B003 Combination Therapy (BL-B01D1+SI-B003) in Patients With Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma and Other Solid Tumors
Primary Endpoint	The primary endpoints evaluate efficacy through Objective Response Rate (ORR) per RECIST 1.1 (complete/partial response rates) and establish the Recommended Phase II Dose (RP2D) based on comprehensive safety, tolerability, and pharmacokinetic data during dose escalation.
Other Endpoint	Secondary assessments include Progression-Free Survival (time to progression/death), Disease Control Rate (complete/partial response or stable disease), Duration of Response (sustained treatment effect), and Treatment-Emergent Adverse Events monitoring (type/frequency/severity of treatment-related toxicities).
Experiment 7 Reporting the Activity Date of This ADC					[142]
Patients Enrolled	Eligible patients (18-75 years) must have recurrent/metastatic HNSCC (excluding nasopharyngeal origin) with measurable lesions (RECIST 1.1), ECOG &le;1, adequate organ function, and controlled prior treatment toxicities. Key exclusions: active CNS metastases, recent anticancer therapy/immunization (4 weeks), uncontrolled infections/autoimmune diseases, effusions requiring drainage, severe cardiovascular conditions, HIV/HBV/HCV positivity with high viral load, or prior grade &ge;3 immune-related adverse events from immunotherapy.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06668961	Clinical Status	PHASE2
Clinical Description	A Phase II Clinical Study to Evaluate the Safety and Efficacy of SI-B001+SI-B003 Combined With Platinum-based Chemotherapy (SI-B001+SI-B003+ Platinum-based Chemotherapy) as First-line Treatment in Patients With Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma
Primary Endpoint	The primary endpoint is objective response rate (ORR) assessed per RECIST 1.1 criteria, measuring complete/partial response rates over 24 months in participants receiving SI-B001+SI-B003 combination therapy.
Other Endpoint	Secondary outcomes include progression-free survival (time to progression/death), disease control rate (complete/partial response or stable disease), duration of response (sustained treatment effect), treatment-emergent adverse events (safety profile), pharmacokinetic parameters (Cmax, Tmax, Ctrough), and immunogenicity assessment (anti-drug antibody frequency/titer).    Click to Show/Hide
Experiment 8 Reporting the Activity Date of This ADC					[143]
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1) must have locally advanced/metastatic solid tumors (NSCLC, nasopharyngeal carcinoma) with measurable lesions (RECIST v1.1) and adequate organ function. Key exclusions: MET exon 14 skipping mutations (Cohort_A), recent anticancer therapy (4 weeks/5 half-lives), uncontrolled hypertension/infections, active CNS metastases, &ge;grade 3 immunotherapy-related toxicities, autoimmune/inflammatory diseases, significant effusions, or HIV/HBV/HCV infections with active viral replication.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05956587	Clinical Status	PHASE2
Clinical Description	A Phase II Clinical Study to Evaluate the Efficacy and Safety of SI-B003 Monotherapy and BL-B01D1+SI-B003 Combination Therapy in Patients With Locally Advanced or Metastatic Non-small Cell Lung Cancer, Nasopharyngeal Carcinoma and Other Solid Tumors
Primary Endpoint	The primary endpoints include Objective Response Rate (ORR) per RECIST 1.1 criteria and determination of Recommended Phase II Dose (RP2D) for SI-B003 based on safety, efficacy, pharmacokinetic and pharmacodynamic data during dose escalation, assessed over 24 months.
Other Endpoint	Secondary endpoints are progression-free survival (time to disease progression/death), disease control rate (complete/partial response or stable disease), duration of response (sustained treatment effect), treatment-emergent adverse events (incidence/severity), all evaluated across the 24-month study period.
Experiment 9 Reporting the Activity Date of This ADC					[144]
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1) must have extensive-stage small-cell lung cancer (SCLC) confirmed histologically/cytologically, with measurable lesions and adequate organ function. Key exclusions: prior HER3/EGFR antibody therapy, recent anticancer treatment (4 weeks/5 half-lives), uncontrolled hypertension/diabetes, active infections, CNS metastases requiring intervention, autoimmune diseases, or other malignancies within 5 years. Cohort-specific criteria apply for prior therapy lines (Cohort_A: &ge;3 lines; Cohort_B: standard therapy failure or treatment-na&iuml;ve).    Click to Show/Hide
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NCT Number	NCT05924841	Clinical Status	PHASE2
Clinical Description	A Phase II Clinical Trial to Evaluate the Efficacy and Safety of BL-B01D1 Monotherapy, SI-B003 Monotherapy and BL-B01D1+SI-B003 Combination Therapy (BL-B01D1+SI-B003) in Patients With Extensive Stage Small Cell Lung Cancer (SCLC)
Primary Endpoint	The primary outcomes include Objective Response Rate (ORR), defined as the proportion of patients achieving complete or partial response per RECIST 1.1, and Recommended Phase II Dose (RP2D) determination based on safety, efficacy, pharmacokinetic, and pharmacodynamic data from the SI-B003 dose-escalation study, both assessed over 24 months.
Other Endpoint	Secondary endpoints comprise Progression-Free Survival (time from treatment initiation to disease progression/death), Disease Control Rate (percentage with response/stable disease per RECIST 1.1), Duration of Response (sustained treatment benefit), and Treatment-Emergent Adverse Events (incidence/severity of new/worsened conditions), all evaluated during the 24-month study period.    Click to Show/Hide
Experiment 10 Reporting the Activity Date of This ADC					[145]
Patients Enrolled	Eligible patients (18-75 years, ECOG 0-1) must have histologically confirmed locally advanced/metastatic NSCLC (Phase Ib: driver-negative post-standard therapy; Phase II Cohort_A: untreated driver-negative; Cohort_B: EGFRmut post-TKI failure). Key exclusions: actionable mutations (ALK/MET/ROS1/BRAF/NTRK/RET), uncontrolled CNS metastases, recent immunotherapy with &ge;G3 irAE, active infections, autoimmunity, or other malignancies within 5 years. Required: measurable lesions, adequate organ function, and ctDNA testing for EGFR/ALK/MET/ROS1/BRAF/NTRK/RET/HER2/KRAS. PD-L1 testing mandated for Phase II Cohort_A.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05949606	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Phase Ib/II Clinical Trial to Evaluate the Safety and Efficacy of SI-B001+SI-B003 With or Without Chemotherapy (SI-B001+SI-B003± Chemotherapy) in the Treatment of Locally Advanced or Metastatic Non-small Cell Lung Cancer (NSCLC)
Primary Endpoint	Phase Ib/II primary endpoints include determining the Recommended Phase II Dose (RP2D) of SI-B001+SI-B003 based on safety, tolerability, efficacy, PK, and PD data. Objective Response Rate (ORR) per RECIST 1.1 assesses confirmed CR/PR rates. Phase Ib evaluates Dose-Limited Toxicity (DLT) incidence/severity via NCI-CTCAE v5.0 and Maximum Tolerated Dose (MTD) or Maximum Administered Dose (MAD) based on DLT rates.    Click to Show/Hide
Other Endpoint	Secondary endpoints include Treatment-Emergent Adverse Events (TEAEs), Disease Control Rate (DCR), Duration of Response (DOR), and Progression-Free Survival (PFS). Pharmacokinetic parameters (Cmax, Tmax, Ctrough, T1/2, AUC0-t, CL) and immunogenicity (anti-drug/neutralizing antibodies) are also analyzed over 24 months to assess drug exposure and immune response.    Click to Show/Hide
Experiment 11 Reporting the Activity Date of This ADC					[146]
Patients Enrolled	Eligible patients (Phase Ia: &ge;18-75 years; Phase Ib: &ge;18 years) must have recurrent/metastatic solid tumors (Phase Ib: gastric/GEJ adenocarcinoma post-platinum/anti-PD- (L)1 or mesothelioma), measurable lesions (Phase Ib), ECOG 0-1, and adequate organ function. Key exclusions: symptomatic CNS metastases, recent anticancer therapy (4 weeks/5 half-lives), uncontrolled infections/autoimmunity, HIV/HBV/HCV, QTc prolongation, or anthracycline exposure >360 mg/m2.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT04606472	Clinical Status	PHASE1
Clinical Description	Phase I Clinical Study to Evaluate the Safety, Tolerability, Pharmacokinetic Characteristics and Preliminary Efficacy of SI-B003, a PD-1/CTLA-4 Bispecific Antibody, in Patients With Advanced Solid Tumors
Primary Endpoint	Phase Ia evaluates Dose-Limiting Toxicity (DLT) and Maximum Tolerated Dose (MTD)/Maximum Administered Dose (MAD) of SI-B003 within 28 days post-dose using NCI-CTCAE v5.0 criteria. Phase Ib determines the Recommended Phase II Dose (RP2D) based on safety, tolerability, efficacy, PK/PD data, while Treatment-Emergent Adverse Events (TEAEs) are monitored over 24 months.    Click to Show/Hide
Other Endpoint	Pharmacokinetic parameters (Cmax, Tmax, T1/2, AUC0-t, CL, Ctrough) are assessed within 28 days post-dose. Immunogenicity (ADA/NAb incidence/titers), efficacy (ORR, DOR, CBR, PFS, OS per RECIST 1.1), and exploratory endpoints (iORR/iCR/iPR per iRECIST 1.1; PK-efficacy correlations) are evaluated over 24 months.
Experiment 12 Reporting the Activity Date of This ADC					[147]
Patients Enrolled	Eligible patients (&ge;18-75 years, ECOG 0-1) must have advanced/metastatic solid tumors (urothelial/prostate/renal cancers post-standard therapy failure/intolerance) with measurable lesions (RECIST 1.1). Key exclusions: prior topoisomerase I inhibitor ADC use, recent chemotherapy/radiotherapy (4 weeks/5 half-lives), unstable CVD, active autoimmunity/infections, uncontrolled diabetes/hypertension, CNS metastases (unless stable post-treatment), or serous effusion requiring drainage. Organ function thresholds: Hb &ge;90g/L, ANC &ge;1.5&times;10<sup>9</sup>/L, platelets &ge;100&times;10<sup>9</sup>/L, Cr &le;1.5 ULN (Ccr &ge;40 mL/min), LVEF &ge;50%. HIV/HBV/HCV active infections disqualify.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05965856	Clinical Status	PHASE2
Clinical Description	A Phase II Clinical Study to Evaluate the Efficacy and Safety of SI-B003 Monotherapy and BL-B01D1+SI-B003 Combination Therapy (BL-B01D1+SI-B003) in Patients With Locally Advanced or Metastatic Urothelial Carcinoma and Other Solid Tumors
Primary Endpoint	The study evaluates Objective Response Rate (ORR) per RECIST 1.1 (confirmed CR/PR rates) and determines the Recommended Phase II Dose (RP2D) of SI-B003 based on safety, efficacy, PK/PD data, with assessments spanning 24 months.
Other Endpoint	Key outcomes include Progression-Free Survival (PFS), Disease Control Rate (DCR), Duration of Response (DOR), and Treatment-Emergent Adverse Events (TEAEs). TEAEs-defined as adverse structural/functional changes or pre-existing condition exacerbations-are monitored for type, frequency, and severity over 24 months.
Experiment 13 Reporting the Activity Date of This ADC					[148]
Related Clinical Trial
NCT Number	NCT03953833	Clinical Status	Phase 1
Clinical Description	Phase 1 clinical trial on the safety, tolerability, pharmacokinetics of B003 in the treatment of HER2-positive recurrent or metastatic breast cancer.

Experiment 1 Reporting the Activity Date of This ADC					[150]
Patients Enrolled	Eligibility: HER2+ (IHC3+/ISH+) metastatic breast cancer patients (&ge;18y, ECOG 0-2) progressing post-trastuzumab, with adequate organ function (ANC &ge;1.5&times;109/L, platelets &ge;100&times;109/L, LVEF >50%). Exclusion: Significant cardiac disease, CNS metastases, prior trastuzumab hypersensitivity &ge;G3, recent anticancer therapy (<4 weeks), HIV/HCV/HBV infection, pregnancy, or investigator-assessed safety concerns.    Click to Show/Hide
Administration Dosage	BI-CON-02 prescribed as intravenous infusion once per 3 weeks. Investigational product therapy during 1 year (up to 18 cycles, duration of 21 days each).
Related Clinical Trial
NCT Number	NCT03062007	Clinical Status	PHASE1
Clinical Description	Open-label Study of Safety, Tolerability and Pharmacokinetics of Multiple Doses of BI-CON-02 in Patients With HER2-positive Metastatic Breast Cancer, Previously Treated With Trastuzumab
Primary Endpoint	The study evaluates treatment-emergent AEs (CTCAE-graded) and determines MTD/RD of BI-CON-02 over 55 weeks, with MTD defined as the highest dose where ≤1/6 patients experience DLTs by Week 3 Day 1, including lab abnormalities and ECG findings.
Other Endpoint	PK parameters (AUC, Cmax, T1/2, Vss, CL) and immunogenicity (anti-BI-CON-02 antibodies) will be analyzed up to 55 weeks to characterize drug exposure and immune response.
Experiment 2 Reporting the Activity Date of This ADC					[152]
Related Clinical Trial
NCT Number	NCT03062007	Clinical Status	Phase 1
Clinical Description	Open-label study of safety, tolerability and pharmacokinetics of multiple doses of BI-CON-02 in patients with HER2-positive metastatic breast cancer, previously treated with trastuzumab.

Experiment 1 Reporting the Activity Date of This ADC					[151]
Administration Dosage	There were a total of 4 dose-escalation sequences, 1.2 mg/kg, 2.4 mg/kg, 3.6 mg/kg and 4.8 mg/kg
Related Clinical Trial
NCT Number	CTR20191558	Clinical Status	PHASE1
Clinical Description	.
Experiment 2 Reporting the Activity Date of This ADC					[153]
Patients Enrolled	HER2-positive locally advanced or metastatic breast cancer (positivity for HER2 was defined as a score of 2+ in immunohistochemical analysis and a positive result in fluorescence in situ hybridization or a score of 3+ in immunohistochemical analysis), the standard treatment was invalid or there was no effective standard treatment plan, the Eastern Cooperative Oncology Group performance status score was 0-1.    Click to Show/Hide
Administration Dosage	4 dose-escalation sequences, 1.20 mg/kg, 2.40 mg/kg, 3.60 mg/kg and 4.80 mg/kg, once every 21days, as a 90-min intravenous infusion.

Experiment 1 Reporting the Activity Date of This ADC					[154]
Efficacy Data	Partial Response (PR)	27%
Patients Enrolled	Eligible patients must have HER2-positive advanced solid tumors with exhausted treatment options, measurable disease (RECIST 1.1), ECOG 0-1, and available tumor tissue. Exclusions include hypersensitivity to study drugs, prior TLR7/8 agonist treatment, cardiac dysfunction, active infections (HIV, HBV, HCV, SARS-CoV-2), and untreated CNS metastases. Other protocol-specific criteria may apply.    Click to Show/Hide
Administration Dosage	Pts with HER2+ (protein or gene) or HER2-low solid tumors progressing after standard therapies (Txs) were enrolled. BDC-1001 was given IV q3w, q2w, or q1w as monotherapy (mono; n=94) and q2w or q1w with nivolumab 240mg q2w (combo; n=37).
Related Clinical Trial
NCT Number	NCT04278144	Clinical Status	PHASE1|||PHASE2
Clinical Description	Phase 1/2 Study of BDC-1001 As a Single Agent and in Combination with Nivolumab in Patients with Advanced HER2-Expressing Solid Tumors
Primary Endpoint	The study evaluates safety (AEs, SAEs, DLTs, and immune-related toxicities) and determines the maximum tolerated dose (MTD) during the escalation phase, alongside assessing ORR of complete/partial responses (CR/PR) in the expansion phase over a 2-year timeframe.
Other Endpoint	Pharmacokinetic parameters (Cmax, Cmin, AUC, CL, Vz, t1/2) of BDC-1001 are measured during both escalation and expansion periods, alongside efficacy outcomes (ORR, DOR, DCR, PFS per RECIST 1.1) and immunogenicity (anti-BDC-1001 antibodies) over 2 years.
Experiment 2 Reporting the Activity Date of This ADC					[155]
Patients Enrolled	Eligible participants must have confirmed HER2+ breast adenocarcinoma (IHC 3+/ISH+/NGS+) with ≥2 prior anti-HER2 therapies (including trastuzumab deruxtecan), measurable disease, ECOG 0-1, and biopsy/archival tissue. Key exclusions cover hypersensitivity to BDC-1001/pertuzumab, prior TLR7/8 agonist treatment, significant cardiac disease, active viral infections, and unstable CNS metastases.    Click to Show/Hide
Administration Dosage	BDC-1001 administered intravenously (IV) every 2 weeks
Related Clinical Trial
NCT Number	NCT05954143	Clinical Status	PHASE2
Clinical Description	Phase 2, Multi-Center, Randomized, Open-Label Trial of BDC-1001 As a Single Agent and in Combination with Pertuzumab in Subjects with HER2-Positive Metastatic Breast Cancer Previously Treated with Trastuzumab Deruxtecan
Primary Endpoint	The efficacy of BDC-1001 alone and combined with pertuzumab is evaluated through Objective Response Rate (ORR) per RECIST v1.1 at 12 weeks.
Other Endpoint	Additional endpoints include long-term efficacy (DOR, DCR, PFS, OS up to 24 months), safety (TEAEs/TESAEs), pharmacokinetics (Cmin, Cmax), and immunogenicity (anti-BDC-1001 ADAs) during the 24-month period for both single-agent and combination therapy.
Experiment 3 Reporting the Activity Date of This ADC					[156]
Patients Enrolled	Patients with advanced metastatic HER2-expressing (IHC2/3+) or amplified solid tumors. Patients had received a median of 4 prior therapies.
Administration Dosage	4 dose levels (0.15-5.00 mg/kg) every 3 weeks.
Related Clinical Trial
NCT Number	NCT04278144	Clinical Status	Phase 1/2
Clinical Description	Phase 1/2 study of BDC-1001 as a single agent and in combination with nivolumab in patients with advanced HER2-expressing solid tumors.

Experiment 1 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.60%	High HER2 expression (HER2+++)
Method Description	25 mice with T226 tumor (P12.1.4/0) between 75 and 196 mm3 were allocated, according to their tumor volume to give homogenous mean and median tumor volume in each treatment arm (5 mice/group). Treatments were initiated when the median tumor volume was 126 mm3 by intravenous injection with either vehicle (control), and trastuzumab-SYNtansine 3 mg/kg.    Click to Show/Hide
In Vivo Model	Breast cancer PDX model (PDX: T226)
Experiment 2 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High HER2 expression (HER2+++)
Method Description	25 mice with T226 tumor (P12.1.4/0) between 75 and 196 mm3 were allocated, according to their tumor volume to give homogenous mean and median tumor volume in each treatment arm (5 mice/group). Treatments were initiated when the median tumor volume was 126 mm3 by intravenous injection with either vehicle (control), and trastuzumab-SYNtansine 9 mg/kg.    Click to Show/Hide
In Vivo Model	Breast cancer PDX model (PDX: T226)

Experiment 1 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Positive HER2 expression (EPHA2+++/++)
Method Description	To establish lung adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 11.25 mg/kg, i.v.
In Vivo Model	NCI-H1975 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 2 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.50%	Positive EGFR expression (EGFR+++/++)
Method Description	To establish lung adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3.75 mg/kg, i.v.
In Vivo Model	NCI-H1975 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 3 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99%	Positive HER2 expression (EPHA2+++/++)
Method Description	To establish gastric tubular adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3.75 mg/kg, i.v.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.70%	Positive EGFR expression (EGFR+++/++)
Method Description	To establish lung adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 11.25 mg/kg, i.v.
In Vivo Model	NCI-H1975 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511

Experiment 1 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	435.86 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the NCI-N87 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Positive CD20 expression (CD20+++/++)
Method Description	Daudi human NHL fragments were implanted subcutaneously in theright flank of the mice. Mice were divided into 4 treatment groups (N=8/group), as follows: trastuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (1 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (5 mg/kg, iv, qd x 1).
In Vivo Model	Daudi CDX model
In Vitro Model	Burkitt lymphoma	Daudi cells		CVCL_0008
Experiment 2 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 25.30%	Positive CD33 expression (CD33+++/++)
Method Description	HL-60 human AML fragments were implanted subcutaneously in theright flank of the mice. Mice were divided into 4 treatment groups (N=8/group), as follows: trastuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (1 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (5 mg/kg, iv, qd x 1).
In Vivo Model	HL-60 CDX model
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 3 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.76%	High HER2 expression (HER2+++)
Method Description	BT474 human breast carcinomas fragments were implanted subcutaneously in theright flank of the mice. Mice were divided into 4 treatment groups (N=8/group), as follows: trastuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); pertuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1).
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	25 pM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	High HER2 expression (HER2 +++)
Method Description	We also tested the OHPAS ADCs in in vivo xenograft mouse models using N87 cell lines. The experiment was followed up to 110 days after administration of ADCs at two different doses (0.5 mg/kg) on day one (initial tumor volume 100 mm3).
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 71.10%	High HER2 expression (HER2 +++)
Method Description	We also tested the OHPAS ADCs in in vivo xenograft mouse models using N87 cell lines. The experiment was followed up to 110 days after administration of ADCs at two different doses (2 mg/kg) on day one (initial tumor volume 100 mm3).
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Moderate HER2 expression (HER2 ++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.58 nM	Negative HER2 expression (HER2 -)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 1.62%	High HER2 expression (HER2+++)
Method Description	For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 0.5 mg/kg of antibody drug conjugates treated four times everyfour days.    Click to Show/Hide
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 43.50%	High HER2 expression (HER2+++)
Method Description	For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 1.56 mg/kg of antibody drug conjugates treated four times everyfour days.    Click to Show/Hide
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.91%	High HER2 expression (HER2+++)
Method Description	For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 3 mg/kg of antibody drug conjugates treated four times everyfour days.    Click to Show/Hide
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.62 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.75 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	506.44 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 3.53%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 15.69%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 22.02%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.11%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.13%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 52.51%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 30 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	27.4 nM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 4%	Positive HER2 expression (EPHA2+++/++)
Method Description	To establish lung adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 11.25 mg/kg, i.v.
In Vivo Model	NCI-H1975 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 2 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 71.20%	Positive EGFR expression (EGFR+++/++)
Method Description	To establish lung adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3.75 mg/kg, i.v.
In Vivo Model	NCI-H1975 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 3 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92%	Positive HER2 expression (EPHA2+++/++)
Method Description	To establish gastric tubular adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3.75 mg/kg, i.v.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92%	Positive EGFR expression (EGFR+++/++)
Method Description	To establish lung adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 11.25 mg/kg, i.v.
In Vivo Model	NCI-H1975 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511

Experiment 1 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the NCI-N87 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 8.74%	High HER2 expression (HER2+++)
Method Description	For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 0.5 mg/kg of antibody drug conjugates treated four times everyfour days.    Click to Show/Hide
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.85%	High HER2 expression (HER2+++)
Method Description	For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 1.56 mg/kg of antibody drug conjugates treated four times everyfour days.    Click to Show/Hide
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.84%	High HER2 expression (HER2+++)
Method Description	For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 3 mg/kg of antibody drug conjugates treated four times everyfour days.    Click to Show/Hide
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.73 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.83 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 10.10%	Negative HER2 expression (HER2 -)
Method Description	Tra-IR700 (3.6 ug/g) or T-DM1-IR700 (3.6 ug/g) was administered intravenously to mice on Day 1 (without NIR light, 6 days after tumor cell transplantation). The dose similar to that of T-DM1 administered to humans (3.6 mg/kg). The NIR-light was irradiated at 1 and 2 days after the drug administration.
In Vivo Model	MDA-MB-468GFP CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468GFP cells		CVCL_DH83
Experiment 2 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 36.40%	Negative HER2 expression (HER2 -)
Method Description	Tra-IR700 (3.6 ug/g) or T-DM1-IR700 (3.6 ug/g) was administered intravenously to mice on Day 1 (without NIR light, 6 days after tumor cell transplantation). The dose similar to that of T-DM1 administered to humans (3.6 mg/kg). The NIR-light was irradiated at 1 and 2 days after the drug administration.
In Vivo Model	MDA-MB-468GFP CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468GFP cells		CVCL_DH83

Experiment 1 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 - 10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 2 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 - 10 nM	Low HER2 expression (HER2+)
Method Description	Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 - 10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 4 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10 - 10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model	Lung squamous cell carcinoma	NCI-H2170 cells		CVCL_1535
Experiment 5 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.5 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model	Breast adenocarcinoma	3T3/HER2-luc-GFP cells		Mus musculus
Experiment 6 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100 nM	Negative HER2 expression (HER2 -)
Method Description	Cells (100,000) were seeded in 12-well dishes and incubated with Tra-IR700 (10 ug/ml) or T-DM1-IR700 (10 ug/ml) for 6 h at 37°C. For NIR-PIT, cells were irradiated with 4 J/cm2 of NIR light from a 690 nm-Laser.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468GFP cells		CVCL_DH83

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 11.68%	High HER2 expression (HER2+++)
Method Description	For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 0.5 mg/kg of antibody drug conjugates treated four times everyfour days.    Click to Show/Hide
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 39.11%	High HER2 expression (HER2+++)
Method Description	For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 1.56 mg/kg of antibody drug conjugates treated four times everyfour days.    Click to Show/Hide
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 76.82%	High HER2 expression (HER2+++)
Method Description	For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 3 mg/kg of antibody drug conjugates treated four times everyfour days.    Click to Show/Hide
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.56 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.92 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.18 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[162]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 13.34%	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of trastuzumab-gelonin against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 2.5 mg/kg.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric cancer	Gastric cancer cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[162]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50.57%	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of trastuzumab-gelonin+LE8 against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 2.5 mg/kg.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric cancer	Gastric cancer cells		Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC					[162]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.79%	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of trastuzumab-gelonin+1HE against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 2.5 mg/kg.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric cancer	Gastric cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[162]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22±0.08 nM	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of trastuzumab-gelonin against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[162]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	555.00±69.60 nM	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of unconjugated rGel against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 15.01%	Positive HER2 expression (HER2 +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 1 mg/kg, i.p.ONCE of one of the conjugates listed above or with PBS only.
In Vivo Model	SK-BR-3 CDX model
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46.22%	Positive HER2 expression (HER2 +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3 mg/kg, i.p.*2 of one of the conjugates listed above or with PBS only.
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.77%	Positive HER2 expression (HER2 +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 10 mg/kg, i.p.*2 of one of the conjugates listed above or with PBS only.
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.40%	Positive HER2 expression (HER2 +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 6 mg/kg, i.p.ONCE of one of the conjugates listed above or with PBS only.
In Vivo Model	SK-BR-3 CDX model
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 17.49%	High HER2 expression (HER2+++)
Method Description	For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 0.5 mg/kg of antibody drug conjugates treated four times everyfour days.    Click to Show/Hide
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.28%	High HER2 expression (HER2+++)
Method Description	For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 1.56 mg/kg of antibody drug conjugates treated four times everyfour days.    Click to Show/Hide
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.20%	High HER2 expression (HER2+++)
Method Description	For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 3 mg/kg of antibody drug conjugates treated four times everyfour days.    Click to Show/Hide
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.77 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.85 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.93 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 19.82%	Positive HER2 expression (HER2 +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 1 mg/kg, i.p.ONCE of one of the conjugates listed above or with PBS only.
In Vivo Model	SK-BR-3 CDX model
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.38%	Positive HER2 expression (HER2 +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 6 mg/kg, i.p.ONCE of one of the conjugates listed above or with PBS only.
In Vivo Model	SK-BR-3 CDX model
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 20.29%	High HER2 expression (HER2+++)
Method Description	For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 0.5 mg/kg of antibody drug conjugates treated four times everyfour days.    Click to Show/Hide
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55.70%	High HER2 expression (HER2+++)
Method Description	For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 1.56 mg/kg of antibody drug conjugates treated four times everyfour days.    Click to Show/Hide
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.48%	High HER2 expression (HER2+++)
Method Description	For efficacy study, 7.5 million tumor cells in 50% matrigel are implanted subcutaneously into 6-8 weeks old nude mice until the tumor sizes reach between 250 and 350 mm3. Dosing is done through bolus tail vein injection. Depending on the tumor response totreatment, animals are injected with 3 mg/kg of antibody drug conjugates treated four times everyfour days.    Click to Show/Hide
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.76 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.99 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.22 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[164]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.53%	High HER2 expression (HER2 +++)
Method Description	A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 30 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[164]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.60%	High HER2 expression (HER2 +++)
Method Description	A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 150 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 37%	High HER2 expression (HER2 +++)
Method Description	We also tested the OHPAS ADCs in in vivo xenograft mouse models using N87 cell lines. The experiment was followed up to 110 days after administration of ADCs at two different doses (0.5 mg/kg) on day one (initial tumor volume 100 mm3).
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.60%	High HER2 expression (HER2 +++)
Method Description	We also tested the OHPAS ADCs in in vivo xenograft mouse models using N87 cell lines. The experiment was followed up to 110 days after administration of ADCs at two different doses (2 mg/kg) on day one (initial tumor volume 100 mm3).
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Moderate HER2 expression (HER2 ++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[164]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 37.30%	High HER2 expression (HER2 +++)
Method Description	A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 30 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[164]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 76.05%	High HER2 expression (HER2 +++)
Method Description	A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 150 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 37.39%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.15%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 44.70%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.05 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 63.20%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.5 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 65.80%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.88 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 45%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.5 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 47.50%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.05 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 87.50%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	4.17 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 47.50%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.05 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 67.50%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.5 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 75%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	11.3 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 53.99%	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (2 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.50%	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (5 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.27 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.33 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 54.50%	Negative HER2 expression (HER2 -)
Method Description	Tra-IR700 (3.6 ug/g) or T-DM1-IR700 (3.6 ug/g) was administered intravenously to mice on Day 1 (with NIR light 6 days after tumor cell transplantation). The dose similar to that of T-DM1 administered to humans (3.6 mg/kg). The NIR-light was irradiated at 1 and 2 days after the drug administration.
In Vivo Model	MDA-MB-468GFP CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468GFP cells		CVCL_DH83
Experiment 2 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.80%	Negative HER2 expression (HER2 -)
Method Description	Tra-IR700 (3.6 ug/g) or T-DM1-IR700 (3.6 ug/g) was administered intravenously to mice on Day 1 (with NIR light 6 days after tumor cell transplantation). The dose similar to that of T-DM1 administered to humans (3.6 mg/kg). The NIR-light was irradiated at 1 and 2 days after the drug administration.
In Vivo Model	MDA-MB-468GFP CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468GFP cells		CVCL_DH83

Experiment 1 Reporting the Activity Date of This ADC					[164]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55.08%	High HER2 expression (HER2 +++)
Method Description	A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 30 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[164]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.16%	High HER2 expression (HER2 +++)
Method Description	A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 150 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.18%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.50%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 58.68%	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (2 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.39%	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (5 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 58.75%	High HER2 expression (HER2+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	High HER2 expression (HER2+++/++)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	High HER2 expression (HER2+++/++)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	73.11 nM	Low HER2 expression (HER2-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	73.11 nM	Low HER2 expression (HER2-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[169]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59%	Negative HER2 expression (HER2 -)
Method Description	T moiety (We conducted a four-week (day 1, 8, 15, 22, and 29) intermittent intravenous dose toxicity study of exatecan mesylate in rats (six animals/group) with a four-week recovery period (three of the six animals).
In Vivo Model	MDA-MB-468 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[170]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 60%	Positive HER2 expression (HER2 +++/++)
Method Description	Docetaxel and trastuzumab (5 and 1.9 mg/kg, respectively,every seven days 3) induces efficient tumor cell killing in cell line-derived models of SKBR3 cells with HER2 expression with high expression.
In Vivo Model	SKBR-3 CDX model
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 62.50%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.05 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 62.50%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.5 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 80%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	4.75 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.77%	Positive HER2 expression (HER2 +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3 mg/kg, i.p.*2 of one of the conjugates listed above or with PBS only.
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 76.32%	Positive HER2 expression (HER2 +++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 10 mg/kg, i.p.*2 of one of the conjugates listed above or with PBS only.
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.72%	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (2 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.72%	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (5 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.40%	Low HER2 expression (HER2-)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 68.86%	High HER2 expression (HER2+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96%	Low HER2 expression (HER2-)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High HER2 expression (HER2+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	High HER2 expression (HER2+++/++)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	High HER2 expression (HER2+++/++)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	28.1 nM	Low HER2 expression (HER2-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	39.91 nM	Low HER2 expression (HER2-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 68%	Positive HER2 expression (EPHA2+++/++)
Method Description	To establish gastric tubular adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3 mg/kg, i.v., qw*4.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.79 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.59 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 70%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.05 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 77.50%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 0.5 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 80%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	4.73 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[164]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 71.25%	High HER2 expression (HER2 +++)
Method Description	A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 30 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[164]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.43%	High HER2 expression (HER2 +++)
Method Description	A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 150 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 74.10%	High HER2 expression (HER2 +++)
Method Description	We also tested the OHPAS ADCs in in vivo xenograft mouse models using N87 cell lines. The experiment was followed up to 110 days after administration of ADCs at two different doses (0.5 mg/kg) on day one (initial tumor volume 100 mm3).
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.50%	High HER2 expression (HER2 +++)
Method Description	We also tested the OHPAS ADCs in in vivo xenograft mouse models using N87 cell lines. The experiment was followed up to 110 days after administration of ADCs at two different doses (2 mg/kg) on day one (initial tumor volume 100 mm3).
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.6 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Moderate HER2 expression (HER2 ++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.60%	High HER2 expression (HER2+++)
Method Description	Mice bearing mammary tumor transplants from the MMTV-HER2 Fo5 line were given a single iv injection (10 mg/kg) of Tmab-SPP-DM1, Tmab-SSNPP-DM3, Tmab-SSNPP-DM4, Tmab-MCC-DM1, or vehicle (n=7 mice per group), and tumor growth was monitored for 25 days.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus

Experiment 1 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.60%	High HER2 expression (HER2+++)
Method Description	Mice bearing mammary tumor transplants from the MMTV-HER2 Fo5 line were given a single iv injection (10 mg/kg) of Tmab-SPP-DM1, Tmab-SSNPP-DM3, Tmab-SSNPP-DM4, Tmab-MCC-DM1, or vehicle (n=7 mice per group), and tumor growth was monitored for 25 days.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus

Experiment 1 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.60%	High HER2 expression (HER2+++)
Method Description	Mice bearing mammary tumor transplants from the MMTV-HER2 Fo5 line were given a single iv injection (10 mg/kg) of Tmab-SPP-DM1, Tmab-SSNPP-DM3, Tmab-SSNPP-DM4, Tmab-MCC-DM1, or vehicle (n=7 mice per group), and tumor growth was monitored for 25 days.
In Vivo Model	MMTV-HER2 Fo5 CDX model (Trastuzumab resistant)
In Vitro Model	Breast cancer	MMTV-HER2 cells		Mus musculus

Experiment 1 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	High HER2 expression (HER2+++)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. For measurement of apoptosis, BT-474 and SK-BR-3 were exposed to trastuzumab or trastuzumab-DM for 48 h.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.26 nM	High HER2 expression (HER2+++)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. For measurement of apoptosis, BT-474 and SK-BR-3 were exposed to trastuzumab or trastuzumab-DM for 48 h.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	41.37 nM	Negative HER2 expression (HER2-)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Low HER2 expression (HER2+)
Method Description	The effects of trastuzumab and trastuzumab-maytansinoid conjugates on tumor cell viability were assessed using Cell Titer-Glo. Cells were plated in black-walled 96-well plates (20,000 per well for BT-474; 10,000 cells per well for all other lines) and allowed to adhere overnight at 37°C in a humidified atmosphere of 5% CO2. Medium was then removed and replaced by fresh culture medium containing different concentrations of trastuzumab, trastuzumab ADC, or free DM1, and the cells incubated for varying periods of time.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.82%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.97%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.39%	High HER2 expression (HER2+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.41%	Moderate HER2 expression (HER2++)
Method Description	Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.1036 [4.0] was injected once i.v. at a doseof 30 ug/kg with respect to amanitin at day 14.
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.97%	Moderate HER2 expression (HER2++)
Method Description	Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.1036 [4.0] was injected once i.v. at a doseof 150 ug/kg with respect to amanitin at day 14.
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate HER2 expression (HER2++)
Method Description	Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.1036 [4.0] was injected once i.v. at a doseof 150 ug/kg with respect to amanitin at day 14.
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate HER2 expression (HER2++)
Method Description	Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.1036 [4.0] was injected once i.v. at a doseof 30 ug/kg with respect to amanitin at day 14.
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.1 nM	Moderate HER2 expression (HER2++)
Method Description	Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[173]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.83%	Moderate HER2 expression (HER2++)
Method Description	Six days after JIMT-3 cell implantation, when tumors reached an average size of 220-230 mm3, the animals were divided into groups of 6 mice according to tumor sizeand aspect. All compounds were injected intraperitoneally (i.p.). In this example, the anti-tumor activity of Tratuzumab mAb coupled with E-13 at about DAR 4 was evaluated after 1 injections of a 3 mg/kg dose at D6.    Click to Show/Hide
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[173]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive HER2 expression (HER2+++/++)
Method Description	Six days after Calu-3 cell implantation, when tumors reached an average size of 250-260 mm3, the animals were divided into groups of 6 mice according to tumor sizeand aspect. All compounds were injected intraperitoneally (i.p.). In this example, the anti-tumor activity of Tratuzumab mAb coupled with E-13 at about DAR 4 was evaluated after 1 injections of a 3 mg/kg dose at D6.    Click to Show/Hide
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609

Experiment 1 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.97%	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (1 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[173]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.41%	Moderate HER2 expression (HER2++)
Method Description	Six days after JIMT-3 cell implantation, when tumors reached an average size of 220-230 mm3, the animals were divided into groups of 6 mice according to tumor sizeand aspect. All compounds were injected intraperitoneally (i.p.). In this example, the anti-tumor activity of Tratuzumab mAb coupled with G-13 at about DAR 4 was evaluated after 1 injections of a 3 mg/kg dose at D6.    Click to Show/Hide
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[173]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive HER2 expression (HER2+++/++)
Method Description	Six days after Calu-3 cell implantation, when tumors reached an average size of 250-260 mm3, the animals were divided into groups of 6 mice according to tumor sizeand aspect. All compounds were injected intraperitoneally (i.p.). In this example, the anti-tumor activity of Tratuzumab mAb coupled with G-13 at about DAR 4 was evaluated after 1 injections of a 3 mg/kg dose at D6.    Click to Show/Hide
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609

Experiment 1 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.60%	Positive HER2 expression (EPHA2+++/++)
Method Description	To establish gastric tubular adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3 mg/kg, i.v., qw*4.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.16 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.96 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[164]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.62%	High HER2 expression (HER2 +++)
Method Description	A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 30 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[164]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.16%	High HER2 expression (HER2 +++)
Method Description	A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 150 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.84%	Positive HER2 expression (HER2+++/++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with OVCAR-3 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (1 mg/kg) on day 1.
In Vivo Model	OVCAR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.51%	Moderate HER2 expression (HER2++)
Method Description	Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.0643 [4.4] was injected once i.v. at a doseof 30 ug/kg with respect to amanitin at day 14.
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.05%	Moderate HER2 expression (HER2++)
Method Description	Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.0643 [4.4] was injected once i.v. at a doseof 150 ug/kg with respect to amanitin at day 14.
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate HER2 expression (HER2++)
Method Description	Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.0643 [4.4] was injected once i.v. at a doseof 150 ug/kg with respect to amanitin at day 14.
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Moderate HER2 expression (HER2++)
Method Description	Six-week old intact female NMRI nu/nu athymic mice were purchaseo and randomly divided into three groups of eight mice each. 5,000,000 JIMT-cells were injected s.c. into the flank of each mouse. The Her-30.0643 [4.4] was injected once i.v. at a doseof 30 ug/kg with respect to amanitin at day 14.
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.02 nM	High HER2 expression (HER2 +++)
Method Description	Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1 nM	Moderate HER2 expression (HER2++)
Method Description	Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[164]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.64%	High HER2 expression (HER2 +++)
Method Description	A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 30 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[164]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.16%	High HER2 expression (HER2 +++)
Method Description	A mouse tumor xenograft model, wherein 250,000,000 SKOV-3 ovarial carcinoma cellsare implated sub-cutaneously (s.c,) into SCID mice and allowed to grow for 10 days. After 10 days a single dose of 150 ug/kg body weight of various a-amanitin-Herceptin conjugates.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.05%	High HER2 expression (HER2+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.79%	High HER2 expression (HER2+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, i.p.x1) via the tail vein on Day 0.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	High HER2 expression (HER2+++/++)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	76.7 nM	Low HER2 expression (HER2-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[175]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.10%	High HER2 expression (HER2+++)
Method Description	The efficacy of T-PBA was evaluated in two HER2-positive xenograft models at different doses and schedules. T-PBA (10 mg/kg), trastuzumab (10 mg/kg), and saline were injected by tail vein to balb/C nude mice for 0, 3, 6, and 9 days.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[175]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.20%	High HER2 expression (HER2+++)
Method Description	The efficacy of T-PBA was evaluated in two HER2-positive xenograft models at different doses and schedules. T-PBA (10 mg/kg), trastuzumab (10 mg/kg), and saline were injected by tail vein to balb/C nude mice for 0, 3, 6, and 9 days.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[175]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.4 nM	High HER2 expression (HER2+++)
Method Description	Cell Counting Kit-8 (Dojindo Laboratories) was used to measure cell viability. Exponentially growing cells were seeded in 96-well plates (100 muL/well) and incubated at 37°C for 24 h.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[175]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	56.1 nM	High HER2 expression (HER2+++)
Method Description	Cell Counting Kit-8 (Dojindo Laboratories) was used to measure cell viability. Exponentially growing cells were seeded in 96-well plates (100 muL/well) and incubated at 37°C for 24 h.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[175]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	344.6 nM	High HER2 expression (HER2+++)
Method Description	Cell Counting Kit-8 (Dojindo Laboratories) was used to measure cell viability. Exponentially growing cells were seeded in 96-well plates (100 muL/well) and incubated at 37°C for 24 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[176]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94%	Low HER2 expression (HER2+)
Method Description	The in vivo efficacy of trastuzumab-C239i-SG3249 was investigated after single-dose injections (0.30 mg/kg) in female athymic mice bearing NCI-N87 HER2-positive subcutaneous xenografts. NCI-N87 cells (5 x106) in 50% Matrigel were inoculated subcutaneously into 46 week-old female athymic nude mice. Five mice per group were dosed intravenously five days after their tumors reached a volume of 200 mm3.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[176]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.20%	Low HER2 expression (HER2+)
Method Description	The in vivo efficacy of trastuzumab-Flexmab-SG3710 and trastuzumab-C239i-SG3249 ADCs was investigated after single-dose injections (1 mg/kg) in female athymic mice bearing NCI-N87 HER2-positive subcutaneous xenografts,and tumor growth was monitored for 85 days. NCI-N87 cells (5 x106) in 50% Matrigel were inoculated subcutaneously into 46 week-old female athymic nude mice. Five mice per group were dosed intravenously five days after their tumors reached a volume of 200 mm3.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[176]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.4 pM	Low HER2 expression (HER2+)
Method Description	The cytotoxic effect of Trastuzumab-C239i-SG32490 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing breast and gastric cancers. The potency of trastuzumab-Flexmab-SG3710 was assessed on the SKBR-3 cell line after five days of incubation.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[177]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.80%	Positive HER2 expression (HER2+++/++)
Method Description	10 mg/kg TS-L6 administrated once weekly2 inhibited tumor growth in nude and nave mice.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[177]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Positive HER2 expression (HER2+++/++)
Method Description	The cytotoxicity of MF-6, TS, and TS-L6 was assessed with three human cancer cell lines and a mouse cell line.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[177]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	Positive HER2 expression (HER2+++/++)
Method Description	The cytotoxicity of MF-6, TS, and TS-L6 was assessed with three human cancer cell lines and a mouse cell line.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[177]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.5 nM	Positive HER2 expression (HER2+++/++)
Method Description	The cytotoxicity of MF-6, TS, and TS-L6 was assessed with three human cancer cell lines and a mouse cell line.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[177]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.25 nM	Low HER2 expression (HER2+)
Method Description	The cytotoxicity of MF-6, TS, and TS-L6 was assessed with three human cancer cell lines and a mouse cell line.
In Vitro Model	Colon adenocarcinoma	CT26.WT cells		CVCL_7256

Experiment 1 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96%	Positive HER2 expression (EPHA2+++/++)
Method Description	To establish gastric tubular adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3 mg/kg, i.v., qw*4.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.79 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.22 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96%	Positive HER2 expression (EPHA2+++/++)
Method Description	To establish gastric tubular adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3 mg/kg, i.v., qw*4.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	29.01 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	52.21 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[178]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.20%	High HER2 expression (HER2+++)
Method Description	Approximately 2 million cells (100 L of the mixture) were implanted subcutaneously to the right flank of 68 weeks old female SCID/beige mice. After the tumors reached about 200 to 400 mm3 ,the mice were treated with either anti-HER2_vc-1 or non-targeted ADC at 3 mpk (IP,Q5dx3).
In Vivo Model	Breast cancer CDX model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[178]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High HER2 expression (HER2+++)
Method Description	Approximately 2 million cells (100 L of the mixture) were implanted subcutaneously to the right flank of 68 weeks old female SCID/beige mice. After the tumors reached about 200 to 400 mm3 ,the mice were treated with either anti-HER2_vc-1 or non-targeted ADC at 10 mpk (IP,Q5dx3).
In Vivo Model	Breast cancer CDX model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.52%	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (2 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.72%	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (5 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.44 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.95%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.30%	Positive HER2 expression (EPHA2+++/++)
Method Description	To establish gastric tubular adenocarcinoma model, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 3 mg/kg, i.v., qw*4.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.42 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.49 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≐ 100%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 20 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≏ 100%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≎ 100%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1.25 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	4.77 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≍ 100%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 20 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≌ 100%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≋ 100%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1.25 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	6.28 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≊ 100%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 20 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≉ 100%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 5 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive HER2 expression (HER2+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1.25 mg/kg, iv.*1 to thetail of each mouse.
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	9.47 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High HER2 expression (HER2+++)
Method Description	Female CB-17 SCID mice were inoculated subcutaneously with NCI-N87 cells (n=10 for each group). Mice inoculated subcutaneously with NCI-N87 cells (n=10 for each group) after IV administration as a single dose (1.5 mg/kg) on day 1.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.53 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[179]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive HER2 expression (HER2 +++/++)
Method Description	NOD-SCID mice with heterotopic SKBR-3 tumor xenografts were injected intravenously with either ADC 12 (1.12 mg/kg; group A), PBS 1x (vehicle; group B) or Kadcyla (1.12 mg/kg; group C) and tumor volume was measured every 2-3 days for 30 days.
In Vivo Model	SKBR-3 CDX model
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[179]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[179]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[180]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High HER2 expression (HER2+++)
Method Description	Athymic mice were inoculated with HER2-positive N87 tumor cells. When tumors reached approximately 300 mm3, mice were administered PBS vehicle or the indicated ADCs at 1 mg/kg every 4 days (days 1, 5, 9, 13).
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[181]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive HER2 expression (HER2 +++/++)
Method Description	1,000,000 EMT6 mouse breast cancer cells expressing human HER-2 previously determined to be suitable for in vivo growth, were implanted into theright mammary fat pads of female Balb/c mice. Animals were treated onthe same day (day 13) and 7 days later (day 20) byintravenous injection of the reference ADC Kadcyla (15 mg/kg), Trastuzumab-PNU-EDA-Glys (1 mg/kg) or vehicle control.    Click to Show/Hide
In Vivo Model	EMT6 CDX model (Expressing hHER2)
In Vitro Model	Mammary gland malignant neoplasms	EMT6 cells (High HER2 expression)		CVCL_1923

Experiment 1 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Effective Concentration (EC50)	6.9 ng/mL	High CD30 expression (CD30 +++)
Method Description	Dose response of the cytotoxic effects of the indicated ADCs on human Non-Hodgkin lymphoma cell line Karpas-299, and on human Hodgkin lymphoma cell line L428 cells.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[207]
Efficacy Data	Half Maximal Effective Concentration (EC50)	< 10 ug/mL	Low CD30 expression (CD30 +)
Method Description	Dose response of the cytotoxic effects of the indicated ADCs on human Non-Hodgkin lymphoma cell line Karpas-299, and on human Hodgkin lymphoma cell line L428 cells.
In Vitro Model	Hodgkin lymphoma	L-428 cells		CVCL_1361

Experiment 1 Reporting the Activity Date of This ADC					[182]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High HER2 expression (HER2+++; 170,000 HER2 molecules/cell)
Method Description	JIMT-1 cells were transplanted subcutaneously into CB17.SCID mice and tumors were allowed to grow to a volume of 100-150 mm3. Mice were then treated intravenously 3 times weekly with the 1 mg/kg ADC preparations.
In Vivo Model	Trastuzumab-resistant breast cancer CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[182]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.7 ng/mL	High HER2 expression (HER2+++; 694,000 HER2 molecules/cell)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[182]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.7 ng/mL	Moderate HER2 expression (HER2++; 32,000 HER2 molecules/cell)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Minimal Effective Dose (MED)	< 5 mg/kg	High HER2 expression (HER2+++)
Method Description	Following the acclimatization period (1 week), the animals were stratified by body weight and randomly assigned to the following group: three trastuzumab-AJICAP-maytansinoid groups, treated with 20 mg/kg, 60 mg/kg, and 120 mg/kg. Each group consisted of five animals for blood chemistry test as well as five animals for clinical signs and body weight measurements.    Click to Show/Hide
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Maximum Tolerated Dose (MTD)	> 120 mg/kg	High HER2 expression (HER2+++)
Method Description	Following the acclimatization period (1 week), the animals were stratified by body weight and randomly assigned to the following group: three trastuzumab-AJICAP-maytansinoid groups, treated with 20 mg/kg, 60 mg/kg, and 120 mg/kg. Each group consisted of five animals for blood chemistry test as well as five animals for clinical signs and body weight measurements.    Click to Show/Hide
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	53.68%	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (0.5 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	89.84%	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (2 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.27 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.33 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	58.23%	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (0.5 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	87.94%	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (2 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	64.86%	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (2 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	95.44%	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (5 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	96.08%	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (2 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	99.23%	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (5 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.21 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.44 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 9 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 5.82%	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 1 mg/kg ADC dosing on day 0.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5
Experiment 2 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 31.56%	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 3 mg/kg ADC dosing on day 0.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5
Experiment 3 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 47.90%	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 6 mg/kg ADC dosing on day 0.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5

Experiment 1 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	102.78 ug/mL	High HER2 expression (HER2 +++)
Method Description	Certain cells are seeded at 1000-2000/well or 2000-3000/well in a 96-well plate, 50 uL/well. After one or two days, ADCs are added with "no ADC" control wells receiving medium alone. Conditions are in duplicate or triplicate After 3-5 days, 100 uL/well Cell TiterGlo ll isadded.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 ug/mL	Negative HER2 expression (HER2 -)
Method Description	Certain cells are seeded at 1000-2000/well or 2000-3000/well in a 96-well plate, 50 uL/well. After one or two days, ADCs are added with "no ADC" control wells receiving medium alone. Conditions are in duplicate or triplicate After 3-5 days, 100 uL/well Cell TiterGlo ll isadded.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[185]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.98%	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 1 mg/kg ADC dosing on day 0.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5
Experiment 2 Reporting the Activity Date of This ADC					[185]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.86%	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 3 mg/kg ADC dosing on day 0.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5
Experiment 3 Reporting the Activity Date of This ADC					[185]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.16%	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 6 mg/kg ADC dosing on day 0.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5

Experiment 1 Reporting the Activity Date of This ADC					[185]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 75.29%	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 0.3 mg/kg ADC dosing on day 0.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5
Experiment 2 Reporting the Activity Date of This ADC					[185]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.01%	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 1 mg/kg ADC dosing on day 0.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5
Experiment 3 Reporting the Activity Date of This ADC					[185]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.39%	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 3 mg/kg ADC dosing on day 0.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5

Experiment 1 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.27%	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. When tumor sreached desired volumes, the tumor-bearing mice were randomized and given a single dose by IV 1 mg/kg injection of the ADC.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5
Experiment 2 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.68%	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. MMTV-HER2 Fo5 mammary allograft tumors inoculated into CRL nu/nu mice aftersingle,then iv 1 mg/kg ADC dosing on day 0.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5
Experiment 3 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.51%	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. When tumor sreached desired volumes, the tumor-bearing mice were randomized and given a single dose by IV 3 mg/kg injection of the ADC.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5
Experiment 4 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.92%	High HER2 expression (HER2 +++)
Method Description	Before being used for an in vivo efficacy study, the MMTV-HER2 Fo5 transgenic mammary tumor was surgically transplanted into the mammary fat pad of nu/nu mice in fragments that measured approximately 2x2 mm. When tumor sreached desired volumes, the tumor-bearing mice were randomized and given a single dose by IV 10 mg/kg injection of the ADC.
In Vivo Model	Breast cancer model MMTV-HER2 Fo5

Experiment 1 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.12 ug/mL	High HER2 expression (HER2 +++)
Method Description	Certain cells are seeded at 1000-2000/well or 2000-3000/well in a 96-well plate, 50 uL/well. After one or two days, ADCs are added with "no ADC" control wells receiving medium alone. Conditions are in duplicate or triplicate After 3-5 days, 100 uL/well Cell TiterGlo ll isadded.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[184]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 ug/mL	Negative HER2 expression (HER2 -)
Method Description	Certain cells are seeded at 1000-2000/well or 2000-3000/well in a 96-well plate, 50 uL/well. After one or two days, ADCs are added with "no ADC" control wells receiving medium alone. Conditions are in duplicate or triplicate After 3-5 days, 100 uL/well Cell TiterGlo ll isadded.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	62.80%	Positive HER2 expression (HER2 +++/++)
Method Description	Seeding cells (HCC1569) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	HCC1569 cells		CVCL_1255
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	4.36 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Seeding cells (HCC1569) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	HCC1569 cells		CVCL_1255

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	66.40%	Positive HER2 expression (HER2 +++/++)
Method Description	Seeding cells (HCC1569) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	HCC1569 cells		CVCL_1255
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	78.60%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.68 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.15 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Seeding cells (HCC1569) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	HCC1569 cells		CVCL_1255

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	74.40%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.68 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	79%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.5 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	79.10%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.52 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	81.10%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.2 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	82.10%	Low HER2 expression (HER2 +)
Method Description	Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	92.50%	Moderate HER2 expression (HER2 ++)
Method Description	Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.15 nM	Moderate HER2 expression (HER2 ++)
Method Description	Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.56 nM	Low HER2 expression (HER2 +)
Method Description	Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	83%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.21 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	83.10%	Low HER2 expression (HER2 +)
Method Description	Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	88.40%	Moderate HER2 expression (HER2 ++)
Method Description	Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Max inhibition rate (MIR)	95.30%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.03 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.17 nM	Moderate HER2 expression (HER2 ++)
Method Description	Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.94 nM	Low HER2 expression (HER2 +)
Method Description	Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	83.20%	Low HER2 expression (HER2 +)
Method Description	Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	94%	Moderate HER2 expression (HER2 ++)
Method Description	Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.08 nM	Moderate HER2 expression (HER2 ++)
Method Description	Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.3 nM	Low HER2 expression (HER2 +)
Method Description	Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	83.20%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.19 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	83.60%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.21 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	84.70%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.21 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	84.80%	Low HER2 expression (HER2 +)
Method Description	Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	91.70%	Moderate HER2 expression (HER2 ++)
Method Description	Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.09 nM	Moderate HER2 expression (HER2 ++)
Method Description	Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.84 nM	Low HER2 expression (HER2 +)
Method Description	Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	85.60%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.23 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	85.80%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.23 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	86.10%	Low HER2 expression (HER2 +)
Method Description	Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	94.40%	Moderate HER2 expression (HER2 ++)
Method Description	Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.09 nM	Moderate HER2 expression (HER2 ++)
Method Description	Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.3 nM	Low HER2 expression (HER2 +)
Method Description	Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	86.30%	Low HER2 expression (HER2 +)
Method Description	Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	94.20%	Moderate HER2 expression (HER2 ++)
Method Description	Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.07 nM	Moderate HER2 expression (HER2 ++)
Method Description	Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.29 nM	Low HER2 expression (HER2 +)
Method Description	Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	86.50%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.14 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	87.10%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.19 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	87.80%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.11 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	87.90%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.17 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	88.10%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.12 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	88.90%	Moderate HER2 expression (HER2 ++)
Method Description	Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	91.70%	Low HER2 expression (HER2 +)
Method Description	Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 3 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.18 nM	Moderate HER2 expression (HER2 ++)
Method Description	Seeding cells (JIMT-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.07 nM	Low HER2 expression (HER2 +)
Method Description	Seeding cells (Capan-1) into 96-well plate, at 2E3 cell per well (80 uL/well). Overnight incubation.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	89.10%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.23 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	89.80%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.12 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	90.30%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.27 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	90.60%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.21 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	91.20%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.24 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	91.50%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.14 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	91.50%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.11 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	91.80%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.13 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	92.30%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	92.30%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	92.30%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	92.30%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.12 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.12 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.12 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 8 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.12 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	93.30%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.1 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	93.60%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.1 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	94.20%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.22 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	94.20%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.26 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	95.20%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.23 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	95.50%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.08 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Maximum inhibition efficiency (MIE)	96.80%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.43 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Max inhibition rate (MIR)	76.50%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.26 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Max inhibition rate (MIR)	90.70%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.13 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Max inhibition rate (MIR)	91.30%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.1 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Max inhibition rate (MIR)	95.70%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.02 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Max inhibition rate (MIR)	96.30%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.02 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Max inhibition rate (MIR)	96.50%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.02 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Max inhibition rate (MIR)	97.40%	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[186]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.01 nM	High HER2 expression (HER2+++)
Method Description	The in vitro potency of ADC was measured in a panel of cancer cell lines usingthe CellTiter-Glo Luminescent Viability Assay.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Inhibition rate (100nM)	0%	High TRKB expression (TRKB+++); Negative HER2 expression (HER2-)
Method Description	Given the finding of TrkB antibody internalization following binding, the functional activity of the TrkB-targeting DVD-ADC was evaluated in vitro with respect to mediating breast cancer cell death. In this assay, the breast cancer cells were incubated in growth medium with 100 nM of each of the four reagents for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Inhibition rate (100nM)	0%	High TRKB expression (TRKB+++); Negative HER2 expression (HER2-)
Method Description	Given the finding of TrkB antibody internalization following binding, the functional activity of the TrkB-targeting DVD-ADC was evaluated in vitro with respect to mediating breast cancer cell death. In this assay, the breast cancer cells were incubated in growth medium with 100 nM of each of the four reagents for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[187]
Efficacy Data	Inhibition rate (100nM)	> 50%	High HER2 expression (HER2+++); Moderate TRKB expression (TRKB++)
Method Description	Given the finding of TrkB antibody internalization following binding, the functional activity of the TrkB-targeting DVD-ADC was evaluated in vitro with respect to mediating breast cancer cell death. In this assay, the breast cancer cells were incubated in growth medium with 100 nM of each of the four reagents for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	1.74 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxic effect of Her-SG3249 was assessed in cell viability assays for breast cancer. The potency of Her-SG3249 was assessed on the SKBR-3 cell line. Process aggregation assessed by SEC.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[188]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	2.62 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxic effect of site-specific Her-SG3249 was assessed in cell viability assays for breast cancer. The potency of site-specific Her-SG3249 was assessed on the SKBR-3 cell line. Process aggregation assessed by SEC.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.8 pM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15 pM	High HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	61 pM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	High grade ovarian serous adenocarcinoma	FU-OV-1 cells		CVCL_2047
Experiment 5 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	High HER2 expression (HER2+++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13 pM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[189]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.7 pM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[189]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20 pM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[189]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.1 pM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[189]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	27.2 pM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	74 pM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[190]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	88 pM	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[190]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.9 ng/mL	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[190]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Low HER2 expression (HER2+)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Moderate HER2 expression (HER2 ++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	With OHPAS ADCs 1-4 , we first performed cell-based MTT assays against a series of HER2 positive/negative cell lines using the commercially available HER2 ADC, T-DM1 (average DAR 3.5), which we purchased as a positive control.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[191]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	High HER2 expression (HER2+++)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[191]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.47 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.56 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.18 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.82 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[191]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High HER2 expression (HER2+++)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[191]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.6 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.78 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.5 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.7 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.33 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.76 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.49 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.49 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.19 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.84 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.3 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.3 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.64 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.73 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.95 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.64 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.73 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.95 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.4 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	79 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.08 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.54 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.96 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.6 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.6 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.25 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.88 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.42 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Esophageal adenocarcinoma	OE19 cells		CVCL_1622
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.75 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.19 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.37 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 9 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 10 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.25 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.88 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.44 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.97 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.21 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.44 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.97 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.21 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.18 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.3 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.4 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.8 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.6 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	118.8 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[193]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive HER2 expression (HER2 +++/++)
Method Description	To quantify cellular cytotoxicity, dose-response curves were generated with HER2-positive SKBR3 cells and HER2-negative MDA-MB-468 cells after treating with ADC and cholesterol-linked endosome-disruptive peptide (Chol-EDP) for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[193]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00±5.00 nM	Positive HER2 expression (HER2 +++/++)
Method Description	To quantify cellular cytotoxicity, dose-response curves were generated with HER2-positive SKBR3 cells and HER2-negative MDA-MB-468 cells after treating with ADC for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[193]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.00±8.00 nM	Negative HER2 expression (HER2 -)
Method Description	To quantify cellular cytotoxicity, dose-response curves were generated with HER2-positive SKBR3 cells and HER2-negative MDA-MB-468 cells after treatment for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.76 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.05 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.64 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.64 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.27 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.1 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.7 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.42 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Esophageal adenocarcinoma	OE19 cells		CVCL_1622
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.75 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.19 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[190]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[190]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.8 ng/mL	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[190]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Low HER2 expression (HER2+)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	High HER2 expression (HER2+++/++)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Low HER2 expression (HER2-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.97 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.04 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.97 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.01 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 9 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.53 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	762.24 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.4 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	29.4 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	105 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	353 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[190]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[190]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.4 ng/mL	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[190]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Low HER2 expression (HER2+)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	High HER2 expression (HER2+++/++)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Low HER2 expression (HER2-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.52 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.7 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[194]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.18 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.09 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.63 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.87 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.79 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.9 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.41 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	31.6 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	233 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.01 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	High HER2 expression (HER2+++/++)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	High HER2 expression (HER2+++/++)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Low HER2 expression (HER2-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[168]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Low HER2 expression (HER2-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[195]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	Positive HER2 expression (HER2+++/++)
Method Description	The cells, at a predetermined concentration, were plated into 96 well plates, and, after overnight incubation at 37°C/5% CO2, serial dilutions of each test article (TA) were added to the cells. Cells were incubated with test articles for 72 hours. and viability was detected with CellTiter-Gloreagent.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.34 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.63 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 8 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 9 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.51 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.79 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.01 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.21 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.65 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	796 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.95 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.25 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.81 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	539.32 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 652.88 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.25 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.9 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	30 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	30 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	77 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.47 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.69 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 8 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	241 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 9 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	275 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.27 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.27 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[196]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.27 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Human HER2 positive or negative cell lines and B14.3 HER2 cell lines were seeded at 1x104 cells per well in 96-well plates. Serial dilutions of vehicle control, isotype control, ODN, Trastuzumab and Trastuzumab-ODN conjugates were added and cells were incubated at 37°C, 5% CO2 for 48h.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[196]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Human HER2 positive or negative cell lines and B14.3 HER2 cell lines were seeded at 1x104 cells per well in 96-well plates. Serial dilutions of vehicle control, isotype control, ODN, Trastuzumab and Trastuzumab-ODN conjugates were added and cells were incubated at 37°C, 5% CO2 for 48h.
In Vitro Model	Esophageal adenocarcinoma	OE19 cells		CVCL_1622
Experiment 3 Reporting the Activity Date of This ADC					[196]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2 -)
Method Description	Human HER2 positive or negative cell lines and B14.3 HER2 cell lines were seeded at 1x104 cells per well in 96-well plates. Serial dilutions of vehicle control, isotype control, ODN, Trastuzumab and Trastuzumab-ODN conjugates were added and cells were incubated at 37°C, 5% CO2 for 48h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.04 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.34 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.63 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.3 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.51 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	37 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.3 nM	Positive HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[191]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.3 nM	High HER2 expression (HER2+++)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[191]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[183]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.33 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.91 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.94 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.85 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	646 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	836 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.32 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	Positive HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.69 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 850 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	Positive HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.39 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.8 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	467.4 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	977.31 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.39 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.68 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	38.18 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.39 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.55 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.39 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.71 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.13 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 nM	Positive HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.44 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.73 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	78.29 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	297.62 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.44 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.73 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.44 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.13 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	645 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.46 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.73 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.76 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[191]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.46 nM	High HER2 expression (HER2+++)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[191]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.47 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.69 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	241 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[167]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	275 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.47 nM	Positive HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.48 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.1 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.48 nM	Positive HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.49 nM	Positive HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.52 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.03 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	123 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	580.3 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.53 nM	Positive HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.56 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.04 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.13 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	749 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.57 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	38.7 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	626 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	734 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.6 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.03 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.64 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.27 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.64 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.26 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.65 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.3 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.67 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.71 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.68 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.92 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	678.88 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 971.38 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.73 nM	Positive HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.75 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.79 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	650.25 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	909.59 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.76 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.22 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	247.49 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.78 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.01 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.05 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.78 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.18 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.83 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.79 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.34 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 517.93 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.82 nM	Positive HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.86 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.58 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	180.13 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	329.21 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.91 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.94 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	323.99 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.94 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.39 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	220.98 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.95 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.39 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.97 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.09 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	25.12 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	55.12 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[194]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.04 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.32 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.07 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.29 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	180.28 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.07 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.09 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.1 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.1 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.1 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.15 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.35 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.12 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.29 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.15 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.48 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.27 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.1 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.16 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.36 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.17 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.52 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.18 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.9 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	704.93 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.2 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.36 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	44.69 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	86.59 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.22 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.88 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.26 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.02 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.33 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.96 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.28 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	29.45 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.36 nM	Positive HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.37 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	292.35 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.41 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.68 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.72 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.43 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.46 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.83 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[194]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.45 nM	Negative HER2 expression (HER2-)
Method Description	Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.45 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.1 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.49 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.06 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.58 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.7 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	166.11 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	253.89 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.86 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[171]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.58 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.91 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.33 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.62 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[194]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.4 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.64 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500.46 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.96 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.01 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.1 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.23 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.28 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.61 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.8 nM	Positive HER2 expression (HER2 +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063

Experiment 1 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.8 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	124 nM	Negative HER2 expression (HER2-)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[192]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	300 nM	High HER2 expression (HER2+++)
Method Description	Cells were counted and seeded in 96 well plates at densities of 2600-3600 cells/well in 100 ul of cell culture medium, A duplicate plate was generated for a day 0 measurement and all plates were incubated in a tissue culture incubator at 37°C with 5% CO2 overnight. Following this incubation, 50 ul/well of Cell titer Glo reagent was added to the day 0 plates, which were then shaken gently for 10 min and the resulting luminescence intensity was measured.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.54 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.3 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.52 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.88 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.05 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.52 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	40.99 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.96 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.73 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.97 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.99 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	29.39 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.99 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	35.58 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.35 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	95.43 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.06 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.91 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.07 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	27.7 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	29.14 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.3 nM	Positive HER2 expression (HER2 +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.4 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	68.25 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14 nM	Positive HER2 expression (HER2 +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	487 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[197]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.21 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.62 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	369.9 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	697.16 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.02 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	525.65 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[179]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[179]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100 nM	Negative HER2 expression (HER2-)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	27.27 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	33.94 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 100 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 100 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 100 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 100 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 100 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 100 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 100 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 100 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 100 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 100 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at 5,000, 2,500, and 2,500 cells/well, respectively, and allowed to rest for 24 h. Five-fold serial dilutions of the antibodies were added starting at 150 nM and incubated for 72-144 h.
In Vitro Model	Bone marrow neuroblastoma	SH-SY5Y cells		CVCL_0019
Experiment 2 Reporting the Activity Date of This ADC					[198]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	144 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were plated at 5,000, 2,500, and 2,500 cells/well, respectively, and allowed to rest for 24 h. Five-fold serial dilutions of the antibodies were added starting at 150 nM and incubated for 72-144 h.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[199]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100 nM	High HER2 expression (HER2+++)
Method Description	The inhibitory activity of Trastuzumab-RSL3-NH2 against cancer cell growth was evaluated by MTT cytotoxicity assay.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	115.99 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the NCI-N87 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	116.33 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the NCI-N87 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	135.3 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the NCI-N87 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	162.74 nM	Positive HER2 expression (HER2+++/++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Amelanotic melanoma	MDA-MB-435 cells		CVCL_0417
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	370.55 nM	Positive HER2 expression (HER2+++/++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Amelanotic melanoma	MDA-MB-435 cells		CVCL_0417

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	162.75 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 517.76 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	203 nM	Positive HER2 expression (HER2 +++/++)
Method Description	SK-BR-3 cells were incubated with 500 nM of trastuzumab and 39 respectively for 30 min at rt, followed by incubation After washing 3 times with PBS, cells were stained with DAPI (300 uL, 10 ug/mL) at rt for 7 min.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[200]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2 -)
Method Description	MCF7 cells were incubated with 500 nM of trastuzumab and 39 respectively for 30 min at rt, followed by incubation After washing 3 times with PBS, cells were stained with DAPI (300 uL, 10 ug/mL) at rt for 7 min.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 300 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 300 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 300 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 300 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 300 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 300 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 300 nM	Moderate HER2 expression (HER2++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 300 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 300 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[174]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 300 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	311.48 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	367.92 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	500.49 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	501.26 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 502.15 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 507.59 nM	High HER2 expression (HER2+++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Moderate HER2 expression (HER2 ++)
Method Description	Target expressing or non-expressing cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compounds (i.e, no antibody conjugated to the drug) in duplicate at 10 concentrations. Cell viability was determined by CellTiter 96 AQueous One Solution Cell Proliferation MTS Assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[182]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 ng/mL	High HER2 expression (HER2+++; 694,000 HER2 molecules/cell)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[182]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12 ng/mL	Moderate HER2 expression (HER2++; 32,000 HER2 molecules/cell)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.11 ng/mL	Moderate HER2 expression (HER2 ++)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 2 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Low HER2 expression (HER2 +)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 3 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Low HER2 expression (HER2 +)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 4 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Moderate HER2 expression (HER2 ++)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.14 ng/mL	Moderate HER2 expression (HER2 ++)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 2 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Low HER2 expression (HER2 +)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 3 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Low HER2 expression (HER2 +)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 4 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Moderate HER2 expression (HER2 ++)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.16 ng/mL	Moderate HER2 expression (HER2 ++)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 2 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Low HER2 expression (HER2 +)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 3 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Low HER2 expression (HER2 +)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 4 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Moderate HER2 expression (HER2 ++)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.48 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxic effect of Trastuzumab-SG3227 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing breast and gastric cancers. The potency of Trastuzumab-SG3227 was assessed on the NCI-N87 cell line.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[202]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2130 ng/mL	Negative expression (HER2-)
Method Description	The cytotoxic effect of Trastuzumab-SG3227 was assessed in cell viability assays for a diverse panel of human solid tumor cell lines representing breast and gastric cancers. The potency of Trastuzumab-SG3227 was assessed on the MDA-MB-468 cell line.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[182]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.8 ng/mL	High HER2 expression (HER2+++; 694,000 HER2 molecules/cell)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[182]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.8 ng/mL	High HER2 expression (HER2+++; 694,000 HER2 molecules/cell)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.6 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.37 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.9 ng/mL	Low HER2 expression (HER2+)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	36.1 ng/mL	Negative expression (HER2-)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[203]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Negative expression (HER2-)
Method Description	The cytotoxicity of the HER2-targeting ADCs was examined in vitro. Every cell line after treatment for 144h with doses ranging from 0.01 to 10, 000 ng/mL. Results are meanSEM of three replicate experiments.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.4 ng/mL	Moderate HER2 expression (HER2 ++)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620
Experiment 2 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Low HER2 expression (HER2 +)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 3 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Low HER2 expression (HER2 +)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 4 Reporting the Activity Date of This ADC					[201]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Moderate HER2 expression (HER2 ++)
Method Description	Tumor cell lines were seeded in 96-well culture plates at 2000, 1600 and 5000 per well in 80 l, respectively, allowed to adhere overnight and treated on the following day with 20 l of serial dilutions of ADCs in duplicate.
In Vitro Model	Breast adenocarcinoma	MDA-MB-361 cells		CVCL_0620

Experiment 1 Reporting the Activity Date of This ADC					[182]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18 ng/mL	High HER2 expression (HER2+++; 694,000 HER2 molecules/cell)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[182]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 110 ng/mL	Moderate HER2 expression (HER2++; 32,000 HER2 molecules/cell)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO2 atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	81.64 ng/mL	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[204]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 800 ng/mL	Negative HER2 expression (HER2 -)
Method Description	Cells were seeded at 5000 per well in a 96-well plate in complete RPMI 1640. Antibody-ZAP complexes (Advanced Targeting Systems; produced according to manufacturer's instructions) or ADCs were added to the cells and plates incubated for 72 hours and 5% carbon dioxide.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.5 uM	Negative HER2 expression (HER2-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted Tras-Me-PRX (10 mg/mL antibody) for 24 h.
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030
Experiment 2 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.75 uM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted Tras-Me-PRX (10 mg/mL antibody) for 24 h.
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 3 Reporting the Activity Date of This ADC					[205]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.02 uM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted Tras-Me-PRX (10 mg/mL antibody) for 24 h.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[206]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 ug/mL	Positive HER2 expression (HER2 +++/++)
Method Description	Paclitaxel, nab-paclitaxel and trastuzumab/nab-paclitaxel, respectively, at a concentration of 0.24 ug/ml paclitaxel equivalent for 48 h.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.01 nM	High HER2 expression (HER2 +++)
Method Description	Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Half Maximal Effective Concentration (EC50)	7.9 nM	Moderate HER2 expression (HER2++)
Method Description	Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.11 nM	High HER2 expression (HER2 +++)
Method Description	Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 nM	Moderate HER2 expression (HER2++)
Method Description	Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[172]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 nM	High HER2 expression (HER2 +++)
Method Description	Cell viability was determined after -72 h -incubation with different concentrations of conjugates at 37°C and 5% CO2 by measurement of fixed andpermeabilized cells with an ant-BrdU-HRP antibody.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.89 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	5.13 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	5.18 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	5.72 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	5.74 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	6.7 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	7 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	7.09 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	10.3 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	12.7 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	13 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.3 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[166]
Efficacy Data	Half Maximal Effective Concentration (EC50)	68.4 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[208]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[208]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.04 7.13 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[208]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[208]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.05 8.79 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[208]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[208]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.08 12.68 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[208]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[208]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.10 16.05 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[209]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[209]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.07 10.67 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[209]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.41 6.20 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[209]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[209]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.04 6.08 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[209]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.07 11.07 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[209]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[209]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.04 6.39 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[209]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.07 10.67 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[209]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[209]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.05 7.06 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[209]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.07 11.07 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[210]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 30%
Method Description	ADC3 was examined in a MDA-MB-231 (Triple Negative Breast Cancer), target antigen + model at 6 mg/kg single doses and was found to reduce the rate of tumor growth compared to vehicle
In Vivo Model	MDA-MB-231 Xenograft Model
Experiment 2 Reporting the Activity Date of This ADC					[210]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 60%
Method Description	ADC3 was examined in a MDA-MB-231 (Triple Negative Breast Cancer), target antigen + model at 10 mg/kg single doses and was found to reduce the rate of tumor growth compared to vehicle
In Vivo Model	MDA-MB-231 Xenograft Model
Experiment 3 Reporting the Activity Date of This ADC					[210]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 60%
Method Description	ADC3 was examined in a MDA-MB-231 (Triple Negative Breast Cancer), target antigen + model after three doses at 10 mg/kg was found to reduce the rate of tumor growth compared to vehicle
In Vivo Model	MDA-MB-231 Xenograft Model
Experiment 4 Reporting the Activity Date of This ADC					[210]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 80%
Method Description	ADC3 was examined in a MDA-MB-231 (Triple Negative Breast Cancer), target antigen + model after three doses at 6 mg/kg was found to reduce the rate of tumor growth compared to vehicle
In Vivo Model	MDA-MB-231 Xenograft Model
Experiment 5 Reporting the Activity Date of This ADC					[210]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 90%
Method Description	ADC3 was examined in a MDA-MB-231 (Triple Negative Breast Cancer), target antigen + model after three doses at 3 mg/kg was found to reduce the rate of tumor growth compared to vehicle
In Vivo Model	MDA-MB-231 Xenograft Model

Experiment 1 Reporting the Activity Date of This ADC					[210]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 50%
Method Description	mean tumour volume versus time after multiple doses of ADC2 (either Days 1, 8 and 15 or Days 1, 22 and 43) against MDA-MB-231 at 5 mg/kg.
In Vivo Model	MDA-MB-231 Xenograft Model
Experiment 2 Reporting the Activity Date of This ADC					[210]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 75%
Method Description	one dose of ADC2 (Day 1) against MDA-MB-231 at 5 mg/kg, single IV.
In Vivo Model	MDA-MB-231 Xenograft Model
Experiment 3 Reporting the Activity Date of This ADC					[210]
Efficacy Data	Complete Remission (CR)	. . .
Method Description	one dose of ADC2 (Day 1) against MDA-MB-231 at 10 mg/kg, single IV.
In Vivo Model	MDA-MB-231 Xenograft Model
Experiment 4 Reporting the Activity Date of This ADC					[210]
Efficacy Data	Complete Remission (CR)	. . .
Method Description	mean tumour volume versus time after multiple doses of ADC2 (either Days 1, 8 and 15 or Days 1, 22 and 43) against MDA-MB-231 at 10 mg/kg.
In Vivo Model	MDA-MB-231 Xenograft Model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 50%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 1 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	< 10%	Negative HER2 expression (HER2-)
Method Description	Growth inhibition test of HER2-negative human breast cancer cell line (MDA-MB-231). The cells were seeded at 1000 cells / 100 pL / well. The cells were cultured at 37 0 C overnight, then the medium was exchanged with new one (95 uL/well), and the cells were treated with a test compound, which was adjusted to 2 ug/mL with PBS , at 5 uL/well (treatment concentration: 100 ng/mL). The cells were cultured for 6 days, then CellTiter-Glo was added thereto at 100 uL/well, and the luminescence amount of each well was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	97%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 50%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 1 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	< 10%	Negative HER2 expression (HER2-)
Method Description	Growth inhibition test of HER2-negative human breast cancer cell line (MDA-MB-231). The cells were seeded at 1000 cells / 100 pL / well. The cells were cultured at 37 0 C overnight, then the medium was exchanged with new one (95 uL/well), and the cells were treated with a test compound, which was adjusted to 2 ug/mL with PBS , at 5 uL/well (treatment concentration: 100 ng/mL). The cells were cultured for 6 days, then CellTiter-Glo was added thereto at 100 uL/well, and the luminescence amount of each well was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	100%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 50%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 1 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	< 10%	Negative HER2 expression (HER2-)
Method Description	Growth inhibition test of HER2-negative human breast cancer cell line (MDA-MB-231). The cells were seeded at 1000 cells / 100 pL / well. The cells were cultured at 37 0 C overnight, then the medium was exchanged with new one (95 uL/well), and the cells were treated with a test compound, which was adjusted to 2 ug/mL with PBS , at 5 uL/well (treatment concentration: 100 ng/mL). The cells were cultured for 6 days, then CellTiter-Glo was added thereto at 100 uL/well, and the luminescence amount of each well was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	101%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 50%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 1 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 50%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 50%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 50%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 50%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 50%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 50%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Tumor Growth lnhibition value (TGl)	55%	Positive her2 expression (her2+++/++)
Method Description	NOD/SCID mice were implanted with estrogen pellets (17p-estradiol, 60 day release, 0.36mg) subcutaneously in the right flank one day before the tumour inoculation.On day -8 each mouse was then inoculated in the right mammary fat pad with 1x107 (BT474) tumor cells,and treatment with 2.5mpk ADC (once per week for four weeks)after tumor volume about 149.78mm3. Determined tumor volume after the experiment, measured at day 23.    Click to Show/Hide
In Vivo Model	BT474 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Tumor Growth lnhibition value (TGl)	109%	Positive her2 expression (her2+++/++)
Method Description	NOD/SCID mice were implanted with estrogen pellets (17p-estradiol, 60 day release, 0.36mg) subcutaneously in the right flank one day before the tumour inoculation.On day -8 each mouse was then inoculated in the right mammary fat pad with 1x107 (BT474) tumor cells,and treatment with 5mpk ADC (once per week for four weeks)after tumor volume about 149.78mm3. Determined tumor volume after the experiment, measured at day 23.    Click to Show/Hide
In Vivo Model	BT474 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0004 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0005 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0007 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0008 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 5 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0022 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 6 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0029 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 7 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0037 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 8 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0044 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 9 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0046 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 10 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0068 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 11 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0093 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 12 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0187 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 13 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0226 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 14 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 0.05 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 15 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 0.05 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 16 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 0.05 uM
Method Description	Patient derived gastric cancer organoids (PDXOs) GA0429B are sheared to uniform sizes and the required number of organoids are combined 1:1 with 50% Matrigel to produce the right size of the organoids to perform the screen. Add 40 pL of CTG 3D per well by Multidrop dispenser, mix the contents for 5 min on the plate shaker, and incubate the plates for 30 min at room temperature in dark. Read luminescent signal on Envision plate reader.    Click to Show/Hide
In Vitro Model	Gastric cancer	Patient derived gastric cancer cells		Homo sapiens
Experiment 17 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.172 uM	Positive her2 expression (her2+++/++)
Method Description	BT-474 cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 18 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 0.2 uM
Method Description	ZR-75-30 Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.    Click to Show/Hide
In Vitro Model	Breast carcinoma	ZR-75-30 cells		CVCL_1661
Experiment 19 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.791 uM	Positive her2 expression (her2+++/++)
Method Description	NCI N87 Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 20 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.581 uM
Method Description	NCI H2170 Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.    Click to Show/Hide
In Vitro Model	Lung squamous cell carcinoma	NCI-H2170 cells		CVCL_1535
Experiment 21 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	52.07 uM	Positive her2 expression (her2+++/++)
Method Description	JIMT 1 Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 22 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	153.55 uM	Positive her2 expression (her2+++/++)
Method Description	Cell line-derived xenograft models were established in female nude mice (BALB/C),by subcutaneous injection of 1x107 (NCI-N87) tumor cells, and treatment with 2.5mg/kg (QW&#422) ADC after tumor volume about 168.08mm3. Determined tumor volume after the experiment, measured at day 35.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 23 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	224.01 uM	Positive her2 expression (her2+++/++)
Method Description	Cell line-derived xenograft models were established in female nude mice (BALB/C),by subcutaneous injection of 1x107 (NCI-N87) tumor cells, and treatment with 5mg/kg (QW&#422) ADC after tumor volume about 168.08mm3. Determined tumor volume after the experiment, measured at day 35.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Tumor Growth lnhibition value (TGl)	62.36%	Low HER2 expression (HER2+)
Method Description	Investigated the antitumour effect of 12 MG/KG AZO-ADC-2 in a Herceptin-resistant, HER2low JIMT-1 xenograft tumour model.
In Vivo Model	Herceptin-resistant, HER2-low JIMT-1 xenograft tumour model
Experiment 2 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Tumor Growth lnhibition value (TGl)	90.97%	High HER2 expression (HER2+++)
Method Description	In the HER2high NCI-N87 xenograft model, Herceptin, AZO-ADC-2 and VC-ADC were administered once a week at a dose of 5 or 10 mg/kg for four consecutive weeks. Compared with the control group, AZO-ADC-2 (5 mg/kg) treatment group displayed significant and sustained suppression of tumour growth with an inhibition rate of 90.97 %
In Vivo Model	HER2high NCI-N87 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.016 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to HER2+ SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.027 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to HER2+ BK474 cells
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.053 nM
Method Description	Cytotoxicity of AZO-ADC-2 to SKOV3/MCF-7 co-culture under 0.1% O2
In Vitro Model	Ovarian serous cystadenocarcinoma; Invasive breast carcinoma of no special type	SKOV3/MCF-7 co-culture cells		CVCL_0532; CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.063 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to SKOV-3 cells under 0.1 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.069 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to HER2+ NCI-N87 cells
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.079 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to SKOV-3 cells under 1 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.088 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 0.1 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.19 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to BT474-HDR cells under 0.1% O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 9 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.28 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to BT474-HDR cells under 0.1 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 10 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.57 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to BT474-HDR cells under 1 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 11 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.74 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to SKOV-3 cells under 5 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 12 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	9.12 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to BT474-HDR cells under 5 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 13 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	11.05 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 toBT474-HDR cells under 20 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 14 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	27.67 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 20 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 15 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	66.8 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to SKOV-3 cells under 20 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 16 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	109.1 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to BT474-HDR cells under 20 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 17 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	115.4 nM	Low HER2 expression (HER2+)
Method Description	Cytotoxicity of AZO-ADC-2 to HER2- MCF-7 cells
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 18 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	134.7 nM
Method Description	Cytotoxicity of AZO-ADC-2 to SKOV3/MCF-7 co-culture under 20% O2
In Vitro Model	Ovarian serous cystadenocarcinoma; Invasive breast carcinoma of no special type	SKOV3/MCF-7 co-culture cells		CVCL_0532; CVCL_0031
Experiment 19 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	266.93 nM
Method Description	Cytotoxicity of AZO-ADC-2 to normal cells, LO2 cells
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	LO2 cells		CVCL_6926
Experiment 20 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 666 nM	Low HER2 expression (HER2+)
Method Description	Cytotoxicity of AZO-ADC-2 to HER2- MDA-MB-231 cells
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 21 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 666 nM
Method Description	Cytotoxicity of AZO-ADC-2 to normal cells, NIH3T3 cells
In Vitro Model	Normal	NIH3T3 cells		CVCL_0594
Experiment 22 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 666 nM
Method Description	Cytotoxicity of AZO-ADC-2 to normal cells, 293T cells
In Vitro Model	Normal	293T cells		CVCL_0063

Experiment 1 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Tumor Growth lnhibition value (TGl)	63.07%	Positive HER2 expression (HER2+++/++)
Method Description	In the SKOV3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	SKOV3 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Tumor Growth lnhibition value (TGl)	63.07%	Positive HER2 expression (HER2+++/++)
Method Description	In the SKOV3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	SKOV3 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Tumor Growth lnhibition value (TGl)	65%	Low HER2 expression (HER2+)
Method Description	Investigated the antitumour effect of 3mg/kg T-ADC in a HER2low JIMT-1 xenograft NUNU mice tumour model, D26.
In Vivo Model	HER2-low JIMT-1 xenograft NUNU mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Tumor Growth lnhibition value (TGl)	≈ 73.30%	Positive HER2 expression (HER2+++/++)
Method Description	Female nude mice (5 ~ 6 weeks old, weight about 20g) were included in the experiment after 1 week of adaptive feeding. It's going to be about 5 x 10Six SKOV-3 cells were inoculated under the skin of the right hind limb of mice to observe the tumor formation. When the tumor volume reached 120mm3, the mice were randomly divided into treatment group and control group (n = 6 groups). H2-921 at 0.5 mg/kg, T-DM1 (1.5 mg/kg, positive control) and PBS (control) were administered at day 0, 7 and 14, respectively. Animal weight was monitored every 3 days and animal behavior was observed daily.Tumor volume was monitored every 3 days during treatment and calculated using the formula TV = a× B2/3, where a represents the long diameter of each tumor and b represents the short diameter of each tumor.    Click to Show/Hide
In Vivo Model	SKOV3 tumor bearing female nude mouse model
Experiment 2 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Tumor Growth lnhibition value (TGl)	≈ 83.30%	Positive HER2 expression (HER2+++/++)
Method Description	Female nude mice (5 ~ 6 weeks old, weight about 20g) were included in the experiment after 1 week of adaptive feeding. It's going to be about 5 x 10Six SKOV-3 cells were inoculated under the skin of the right hind limb of mice to observe the tumor formation. When the tumor volume reached 120mm3, the mice were randomly divided into treatment group and control group (n = 6 groups). H2-921 at 1.5 mg/kg, T-DM1 (1.5 mg/kg, positive control) and PBS (control) were administered at day 0, 7 and 14, respectively. Animal weight was monitored every 3 days and animal behavior was observed daily.Tumor volume was monitored every 3 days during treatment and calculated using the formula TV = a× B2/3, where a represents the long diameter of each tumor and b represents the short diameter of each tumor.    Click to Show/Hide
In Vivo Model	SKOV3 tumor bearing female nude mouse model
Experiment 3 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Tumor Growth lnhibition value (TGl)	≈ 99.60%	Positive HER2 expression (HER2+++/++)
Method Description	Female nude mice (5 ~ 6 weeks old, weight about 20g) were included in the experiment after 1 week of adaptive feeding. It's going to be about 5 x 10Six SKOV-3 cells were inoculated under the skin of the right hind limb of mice to observe the tumor formation. When the tumor volume reached 120mm3, the mice were randomly divided into treatment group and control group (n = 6 groups). H2-921 at 4.5 mg/kg, T-DM1 (1.5 mg/kg, positive control) and PBS (control) were administered at day 0, 7 and 14, respectively. Animal weight was monitored every 3 days and animal behavior was observed daily.Tumor volume was monitored every 3 days during treatment and calculated using the formula TV = a× B2/3, where a represents the long diameter of each tumor and b represents the short diameter of each tumor.    Click to Show/Hide
In Vivo Model	SKOV3 tumor bearing female nude mouse model

Experiment 1 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	. log10 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	BT-474 cells were inoculated in 96-well plates with 5×103 cells/wells and cultured overnight at 37°C with 5% CO2. Then trastuzumab, SB743921, linker+SB743921 or H were added at concentrations of 100ug/ml, 10ug/ml, 1ug/ml, 100ng/ml, 10ng/ml, 1ng/ml, 100pg/ml, 10pg/ml, 1pg/ml or 0mg/ml, respectively 2-921. After culture at 37°C and 5% CO2 for 48h, 10ul CCK-8 solution was added to each well. After 2 ~ 4h, the absorbance at 450nm was measured by enzymograph, and the cell survival rate was calculated.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	. log10 ng/mL	Negative HER2 expression (HER2-)
Method Description	IOSE80 cells were inoculated in 96-well plates with 5×103 cells/wells and cultured overnight at 37°C with 5% CO2. Then trastuzumab, SB743921, linker+SB743921 or H were added at concentrations of 100ug/ml, 10ug/ml, 1ug/ml, 100ng/ml, 10ng/ml, 1ng/ml, 100pg/ml, 10pg/ml, 1pg/ml or 0mg/ml, respectively 2-921. After culture at 37°C and 5% CO2 for 48h, 10ul CCK-8 solution was added to each well. After 2 ~ 4h, the absorbance at 450nm was measured by enzymograph, and the cell survival rate was calculated.    Click to Show/Hide
In Vitro Model	Normal	IOSE80 cells		CVCL_5546
Experiment 3 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	. log10 ng/mL	Negative HER2 expression (HER2-)
Method Description	GES-1 cells were inoculated in 96-well plates with 5×103 cells/Wells and cultured overnight at 37°C with 5% CO2. Then trastuzumab, SB743921, linker+SB743921 or H were added at concentrations of 100ug/ml, 10ug/ml, 1ug/ml, 100ng/ml, 10ng/ml, 1ng/ml, 100pg/ml, 10pg/ml, 1pg/ml or 0mg/ml, respectively 2-921. After culture at 37°C and 5% CO2 for 48h, 10ul CCK-8 solution was added to each well. After 2 ~ 4h, the absorbance at 450nm was measured by enzymograph, and the cell survival rate was calculated.    Click to Show/Hide
In Vitro Model	Normal	GES-1 cells		CVCL_EQ22
Experiment 4 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	. log10 ng/mL	Negative HER2 expression (HER2-)
Method Description	MDA-MB-468 cells were inoculated in 96-well plates with 5×103 cells/wells and cultured overnight at 37°C with 5% CO2. Then trastuzumab, SB743921, linker+SB743921 or H were added at concentrations of 100ug/ml, 10ug/ml, 1ug/ml, 100ng/ml, 10ng/ml, 1ng/ml, 100pg/ml, 10pg/ml, 1pg/ml or 0mg/ml, respectively 2-921. After culture at 37°C and 5% CO2 for 48h, 10ul CCK-8 solution was added to each well. After 2 ~ 4h, the absorbance at 450nm was measured by enzymograph, and the cell survival rate was calculated.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 5 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.8 log10 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	SKOV-3 cells were inoculated in 96-well plates at 5×103 cells/wells and cultured overnight at 37°C with 5% CO2. Then trastuzumab, SB743921, linker+SB743921 or H were added at concentrations of 100ug/ml, 10ug/ml, 1ug/ml, 100ng/ml, 10ng/ml, 1ng/ml, 100pg/ml, 10pg/ml, 1pg/ml or 0mg/ml, respectively 2-921. After culture at 37°C and 5% CO2 for 48h, 10ul CCK-8 solution was added to each well. After 2 ~ 4h, the absorbance at 450nm was measured by enzymograph, and the cell survival rate was calculated.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3.5 log10 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells were inoculated in 96-well plates with 5×103 cells/wells and cultured overnight at 37°C with 5% CO2. Then trastuzumab, SB743921, linker+SB743921 or H were added at concentrations of 100ug/ml, 10ug/ml, 1ug/ml, 100ng/ml, 10ng/ml, 1ng/ml, 100pg/ml, 10pg/ml, 1pg/ml or 0mg/ml, respectively 2-921. After culture at 37°C and 5% CO2 for 48h, 10ul CCK-8 solution was added to each well. After 2 ~ 4h, the absorbance at 450nm was measured by enzymograph, and the cell survival rate was calculated.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 7 Reporting the Activity Date of This ADC					[216]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5 log10 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	NCI-N87 were inoculated in 96-well plates at 5×103 cells/wells and cultured overnight at 37°C with 5% CO2. Then trastuzumab, SB743921, linker+SB743921 or H were added at concentrations of 100ug/ml, 10ug/ml, 1ug/ml, 100ng/ml, 10ng/ml, 1ng/ml, 100pg/ml, 10pg/ml, 1pg/ml or 0mg/ml, respectively 2-921. After culture at 37°C and 5% CO2 for 48h, 10ul CCK-8 solution was added to each well. After 2 ~ 4h, the absorbance at 450nm was measured by enzymograph, and the cell survival rate was calculated.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 8 Reporting the Activity Date of This ADC					[216]
Efficacy Data	apoptosis	24.05%	Positive HER2 expression (HER2+++/++)
Method Description	SKOV-3 cells were inoculated in 6-well plates at about 1×106 cells per well and incubated overnight at 37°C with 5% CO2. The cells were then treated with 1 ug/ml H2-921 for 48 hours. The cells were then collected, suspended with pre-cooled 70% alcohol and fixed overnight at 4 °C. The cells were then incubated with RNase A at 37 °C, RNase A was removed again, and the cells were suspended with propyl iodide (PI) staining solution. 30min dull staining and FACSCalibur flow cytometry. For apoptosis analysis, the cells were treated as described above, and apoptosis was detected by Annexin V-FITC/PI double staining apoptosis kit (Dojindo, Japan) after 48h. Cell cycle distribution and apoptosis were detected by FACSCalibur flow cytometry.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 9 Reporting the Activity Date of This ADC					[216]
Efficacy Data	apoptosis	38.19%	Positive HER2 expression (HER2+++/++)
Method Description	NCI-N87 cells were inoculated in 6-well plates at about 1×106 cells per well and incubated overnight at 37°C with 5% CO2. The cells were then treated with 1 ug/ml H2-921 for 48 hours. The cells were then collected, suspended with pre-cooled 70% alcohol and fixed overnight at 4 °C. The cells were then incubated with RNase A at 37 °C, RNase A was removed again, and the cells were suspended with propyl iodide (PI) staining solution. 30min dull staining and FACSCalibur flow cytometry. For apoptosis analysis, the cells were treated as described above, and apoptosis was detected by Annexin V-FITC/PI double staining apoptosis kit (Dojindo, Japan) after 48h. Cell cycle distribution and apoptosis were detected by FACSCalibur flow cytometry.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 10 Reporting the Activity Date of This ADC					[216]
Efficacy Data	apoptosis	51.63%	Positive HER2 expression (HER2+++/++)
Method Description	NCI-N87 cells were inoculated in 6-well plates at about 1×106 cells per well and incubated overnight at 37°C with 5% CO2. The cells were then treated with 10 ug/ml H2-921 for 48 hours. The cells were then collected, suspended with pre-cooled 70% alcohol and fixed overnight at 4 °C. The cells were then incubated with RNase A at 37 °C, RNase A was removed again, and the cells were suspended with propyl iodide (PI) staining solution. 30min dull staining and FACSCalibur flow cytometry. For apoptosis analysis, the cells were treated as described above, and apoptosis was detected by Annexin V-FITC/PI double staining apoptosis kit (Dojindo, Japan) after 48h. Cell cycle distribution and apoptosis were detected by FACSCalibur flow cytometry.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 11 Reporting the Activity Date of This ADC					[216]
Efficacy Data	apoptosis	58.87%	Positive HER2 expression (HER2+++/++)
Method Description	NCI-N87 cells were inoculated in 6-well plates at about 1×106 cells per well and incubated overnight at 37°C with 5% CO2. The cells were then treated with 100 ug/ml H2-921 for 48 hours. The cells were then collected, suspended with pre-cooled 70% alcohol and fixed overnight at 4 °C. The cells were then incubated with RNase A at 37 °C, RNase A was removed again, and the cells were suspended with propyl iodide (PI) staining solution. 30min dull staining and FACSCalibur flow cytometry. For apoptosis analysis, the cells were treated as described above, and apoptosis was detected by Annexin V-FITC/PI double staining apoptosis kit (Dojindo, Japan) after 48h. Cell cycle distribution and apoptosis were detected by FACSCalibur flow cytometry.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 12 Reporting the Activity Date of This ADC					[216]
Efficacy Data	apoptosis	78.59%	Positive HER2 expression (HER2+++/++)
Method Description	SKOV-3 cells were inoculated in 6-well plates at about 1×106 cells per well and incubated overnight at 37°C with 5% CO2. The cells were then treated with 10 ug/ml H2-921 for 48 hours. The cells were then collected, suspended with pre-cooled 70% alcohol and fixed overnight at 4 °C. The cells were then incubated with RNase A at 37 °C, RNase A was removed again, and the cells were suspended with propyl iodide (PI) staining solution. 30min dull staining and FACSCalibur flow cytometry. For apoptosis analysis, the cells were treated as described above, and apoptosis was detected by Annexin V-FITC/PI double staining apoptosis kit (Dojindo, Japan) after 48h. Cell cycle distribution and apoptosis were detected by FACSCalibur flow cytometry.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 13 Reporting the Activity Date of This ADC					[216]
Efficacy Data	apoptosis	82.56%	Positive HER2 expression (HER2+++/++)
Method Description	SKOV-3 cells were inoculated in 6-well plates at about 1×106 cells per well and incubated overnight at 37°C with 5% CO2. The cells were then treated with 100 ug/ml H2-921 for 48 hours. The cells were then collected, suspended with pre-cooled 70% alcohol and fixed overnight at 4 °C. The cells were then incubated with RNase A at 37 °C, RNase A was removed again, and the cells were suspended with propyl iodide (PI) staining solution. 30min dull staining and FACSCalibur flow cytometry. For apoptosis analysis, the cells were treated as described above, and apoptosis was detected by Annexin V-FITC/PI double staining apoptosis kit (Dojindo, Japan) after 48h. Cell cycle distribution and apoptosis were detected by FACSCalibur flow cytometry.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Tumor Growth lnhibition value (TGl)	79.60%	High HER2 expression (HER2+++)
Method Description	Investigated the antitumour effect of 3mg/kg ADC in a HER2high HCC-1954 xenograft NUNU mice tumour model, D21.
In Vivo Model	HER2-high HCC-1954 xenograft NUNU mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 15 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Tumor Growth lnhibition value (TGl)	80.32%	Positive her2 expression (her2+++/++)
Method Description	Cell line-derived xenograft models were established in in female BALB/c Nude mice, by subcutaneous injection of 1x106 (NCI-N87) tumor cells, and treatmen with 1.33mg/kg ADC (single dosee) after tumor volume about 198mm3. Determined tumor volume after the experiment, measured at day 36.
In Vivo Model	NCI-N87 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Tumor Growth lnhibition value (TGl)	107.47%	Positive her2 expression (her2+++/++)
Method Description	Cell line-derived xenograft models were established in in female BALB/c Nude mice, by subcutaneous injection of 1x106 (NCI-N87) tumor cells, and treatmen with 4mg/kg ADC (single dosee) after tumor volume about 198mm3. Determined tumor volume after the experiment, measured at day 36.
In Vivo Model	NCI-N87 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.008 nM	High HER2 expression (HER2 +++)
Method Description	5000cells/well for SK-BR-3 (100 uL) of cells were seeded onto 96-well plates and incubated for 24 hours before adding the ADC. After 24 hours, growth medium was replaced with ADC in growth medium. After 96 hours, viability was detected using the CellTiter-Glo® luminescence assay. Assay plates were equilibrated at room temperature for 20 minutes before addition of 100ul CellTiter-Glo® reagent per well. The plates were then mixed for 3minutes at 300 rpm to assist cell lysis and incubated for a further 20 minutes at room temperatureto stabilise the luminescence signal. Luminescence was recorded using a SpectraMax i3x platereader with a default integration time of 0.5 s/well.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.228 nM	Low HER2 expression (HER2+)
Method Description	2000cells/well for JIMT-1 (100 uL) of cells were seeded onto 96-well plates and incubated for 24 hours before adding the ADC. After 24 hours, growth medium was replaced with ADC in growth medium. After 96 hours, viability was detected using the CellTiter-Glo® luminescence assay. Assay plates were equilibrated at room temperature for 20 minutes before addition of 100ul CellTiter-Glo® reagent per well. The plates were then mixed for 3minutes at 300 rpm to assist cell lysis and incubated for a further 20 minutes at room temperatureto stabilise the luminescence signal. Luminescence was recorded using a SpectraMax i3x platereader with a default integration time of 0.5 s/well.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	2500cells/well for NCI-H520 (100 uL) of cells were seeded onto 96-well plates and incubated for 24 hours before adding the ADC. After 24 hours, growth medium was replaced with ADC in growth medium. After 96 hours, viability was detected using the CellTiter-Glo® luminescence assay. Assay plates were equilibrated at room temperature for 20 minutes before addition of 100ul CellTiter-Glo® reagent per well. The plates were then mixed for 3minutes at 300 rpm to assist cell lysis and incubated for a further 20 minutes at room temperatureto stabilise the luminescence signal. Luminescence was recorded using a SpectraMax i3x platereader with a default integration time of 0.5 s/well.    Click to Show/Hide
In Vitro Model	Lung squamous cell carcinoma	NCI-H520 cells		CVCL_1566

Experiment 1 Reporting the Activity Date of This ADC					[218]
Efficacy Data	Tumor Growth lnhibition value (TGl)	87.71%
Method Description	Compared to the PBS control group, the TZ-dSA3-12 (1 and 3mg kg-1) treatment group displayed significant and sustained suppression of tumor growth with an inhibition rate of 87.71% and 89.75%
In Vivo Model	N87 tumor-bearing BALB/c nude mice
Experiment 2 Reporting the Activity Date of This ADC					[218]
Efficacy Data	Tumor Growth lnhibition value (TGl)	89.75%
Method Description	Compared to the PBS control group, the TZ-dSA3-12 (1 and 3mg kg-1) treatment group displayed significant and sustained suppression of tumor growth with an inhibition rate of 87.71% and 89.75%
In Vivo Model	N87 tumor-bearing BALB/c nude mice

Experiment 1 Reporting the Activity Date of This ADC					[218]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	SKOV3 or MCF-7 cells were seeded into 96-well plates at a density of 8000 cells/well and treated with various concentrations of TZ-dSA3-12 for 24 h (37°C, 5% CO 2). After 10 uL of Cell Counting Kit-8 (CCK-8) reagent (C0005, TargetMol, USA) was added to each well, the cells were incubated at 37°C for another 3 h. The absorbance was measured at an optical density (OD) of 450 nm using a microplate reader (Thermo Fisher Scientific, Inc., MA, USA).    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[218]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.11- 0.28 nM	Positive HER2 expression (HER2+++/++)
Method Description	SKOV3 or MCF-7 cells were seeded into 96-well plates at a density of 8000 cells/well and treated with various concentrations of TZ-dSA3-12 for 24 h (37°C, 5% CO 2). After 10 uL of Cell Counting Kit-8 (CCK-8) reagent (C0005, TargetMol, USA) was added to each well, the cells were incubated at 37°C for another 3 h. The absorbance was measured at an optical density (OD) of 450 nm using a microplate reader (Thermo Fisher Scientific, Inc., MA, USA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[218]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.13 nM	Positive HER2 expression (HER2+++/++)
Method Description	SKOV3 or MCF-7 cells were seeded into 96-well plates at a density of 8000 cells/well and treated with various concentrations of TZ-dSA3-12 for 24 h (37°C, 5% CO 2). After 10 uL of Cell Counting Kit-8 (CCK-8) reagent (C0005, TargetMol, USA) was added to each well, the cells were incubated at 37°C for another 3 h. The absorbance was measured at an optical density (OD) of 450 nm using a microplate reader (Thermo Fisher Scientific, Inc., MA, USA).    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Tumor Growth lnhibition value (TGl)	88%	High HER2 expression (HER2+++)
Method Description	Investigated the antitumour effect of 3mg/kg ADC in a HER2high HCC-1954 xenograft NUNU mice tumour model, D21.
In Vivo Model	HER2-high HCC-1954 xenograft NUNU mice tumour model
Experiment 2 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Tumor Growth lnhibition value (TGl)	95%	Low HER2 expression (HER2+)
Method Description	Investigated the antitumour effect of 5mg/kg ADC in a HER2low JIMT-1 xenograft NUNU mice tumour model, D13.
In Vivo Model	HER2-low JIMT-1 xenograft NUNU mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.8 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to BT-474 cells
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01676 nM	Low HER2 expression (HER2+)
Method Description	Cytotoxicity of ADC to T-47D cells
In Vitro Model	Invasive breast carcinoma of no special type	T-47D cells		CVCL_0553
Experiment 4 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.4645 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to NCI-N87 cells
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Tumor Growth lnhibition value (TGl)	90.10%	Low HER2 expression (HER2+)
Method Description	Investigated the antitumour effect of 5mg/kg ADC in a HER2low JIMT-1 xenograft NUNU mice tumour model, D13.
In Vivo Model	HER2-low JIMT-1 xenograft NUNU mice tumour model

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 15 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Tumor Growth lnhibition value (TGl)	90.18%
Method Description	Cell line-derived xenograft models were established in female nude mice (BALB/C),by subcutaneous injection of 5x106 (NCI-H358) tumor cells, and treatment with 1mg/kg (QW&#423) ADC after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 29.
In Vivo Model	NCI-H358 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Tumor Growth lnhibition value (TGl)	90.99%
Method Description	Cell line-derived xenograft models were established in female nude mice (BALB/C),by subcutaneous injection of 5x106 (NCI-H358) tumor cells, and treatment with 3mg/kg (QW&#423) ADC after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 29.
In Vivo Model	NCI-H358 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Tumor Growth lnhibition value (TGl)	95.80%
Method Description	Cell line-derived xenograft models were established in female nude mice (BALB/C),by subcutaneous injection of 5x106 (NCI-H358) tumor cells, and treatment with 10mg/kg (QW&#423) ADC after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 29.
In Vivo Model	NCI-H358 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	Low her2 expression (her2+)
Method Description	MCF7, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	Positive her2 expression (her2+++/++)
Method Description	NCIN87 HABCG2, 3000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 200 nM with a 5-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 6 days exposure, 75ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04 nM	Positive her2 expression (her2+++/++)
Method Description	NCI N87 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 1000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04 nM	High her2 expression (her2 +++)
Method Description	SKBR3, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.65 nM	Low her2 expression (her2+)
Method Description	H358, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Minimally invasive lung adenocarcinoma	H358 cells		CVCL_1559
Experiment 6 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.85 nM	Positive her2 expression (her2+++/++)
Method Description	NCI N87, 2000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 300 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 6 days exposure, 75ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	54.6 nM	Positive her2 expression (her2+++/++)
Method Description	NCIN87 HABCB1, 3000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 5-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 6 days exposure, 75ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Tumor Growth lnhibition value (TGl)	95.96%	Positive HER2 expression (HER2+++/++)
Method Description	3x104 A431 cells were injected subcutaneously into the right shoulder of 4-6-week-old BALB/c nude mice, and when the average tumor size of the mice grew to 140 ~ 150mm3, they were randomly divided into 5 cells in each group. At day 0, day 7, day 14, day 21, intravenous injection of a blank control (blank buffer solution) and a dose of 10mg/kg antibody drug conjugate was administered. The tumor volume was measured at day 0, day 7, day 14, day 21, day 24, day 28, day 32, day 36 and the tumor growth inhibition rate on day 28 of d was calculated.    Click to Show/Hide
In Vivo Model	A431 tumor bearing nude mouse model

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Tumor Growth lnhibition value (TGl)	96.69%	Positive HER2 expression (HER2+++/++)
Method Description	3x104 A431 cells were injected subcutaneously into the right shoulder of 4-6-week-old BALB/c nude mice, and when the average tumor size of the mice grew to 140 ~ 150mm3, they were randomly divided into 5 cells in each group. At day 0, day 7, day 14, day 21, intravenous injection of a blank control (blank buffer solution) and a dose of 10mg/kg antibody drug conjugate was administered. The tumor volume was measured at day 0, day 7, day 14, day 21, day 24, day 28, day 32, day 36 and the tumor growth inhibition rate on day 28 of d was calculated.    Click to Show/Hide
In Vivo Model	A431 tumor bearing nude mouse model

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC62)	3.71 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	SW620 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC62)	7.81 nM	Positive HER2 expression (HER2+++/++)
Method Description	Fadu cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC62)	18.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	N87 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC62)	25.72 nM	Positive HER2 expression (HER2+++/++)
Method Description	BXPC-3 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC62)	43.16 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	A431 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Tumor Growth lnhibition value (TGl)	96.85%	Positive HER2 expression (HER2+++/++)
Method Description	3x104 A431 cells were injected subcutaneously into the right shoulder of 4-6-week-old BALB/c nude mice, and when the average tumor size of the mice grew to 140 ~ 150mm3, they were randomly divided into 5 cells in each group. At day 0, day 7, day 14, day 21, intravenous injection of a blank control (blank buffer solution) and a dose of 10mg/kg antibody drug conjugate was administered. The tumor volume was measured at day 0, day 7, day 14, day 21, day 24, day 28, day 32, day 36 and the tumor growth inhibition rate on day 28 of d was calculated.    Click to Show/Hide
In Vivo Model	A431 tumor bearing nude mouse model

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC61)	13.7 nM	Positive HER2 expression (HER2+++/++)
Method Description	N87 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC61)	15.09 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	SW620 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC61)	18.92 nM	Positive HER2 expression (HER2+++/++)
Method Description	Fadu cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC61)	49.85 nM	Positive HER2 expression (HER2+++/++)
Method Description	BXPC-3 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC61)	56.7 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	A431 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.08%	Positive HER2 expression (HER2+++/++)
Method Description	3x104 A431 cells were injected subcutaneously into the right shoulder of 4-6-week-old BALB/c nude mice, and when the average tumor size of the mice grew to 140 ~ 150mm3, they were randomly divided into 5 cells in each group. At day 0, day 7, day 14, day 21, intravenous injection of a blank control (blank buffer solution) and a dose of 10mg/kg antibody drug conjugate was administered. The tumor volume was measured at day 0, day 7, day 14, day 21, day 24, day 28, day 32, day 36 and the tumor growth inhibition rate on day 28 of d was calculated.    Click to Show/Hide
In Vivo Model	A431 tumor bearing nude mouse model

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC59)	2.46 nM	Positive HER2 expression (HER2+++/++)
Method Description	N87 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC59)	3.01 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	SW620 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC59)	3.44 nM	Positive HER2 expression (HER2+++/++)
Method Description	Fadu cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC59)	9.85 nM	Positive HER2 expression (HER2+++/++)
Method Description	BXPC-3 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC59)	27.72 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	A431 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.25%	Positive HER2 expression (HER2+++/++)
Method Description	3x104 A431 cells were injected subcutaneously into the right shoulder of 4-6-week-old BALB/c nude mice, and when the average tumor size of the mice grew to 140 ~ 150mm3, they were randomly divided into 5 cells in each group. At day 0, day 7, day 14, day 21, intravenous injection of a blank control (blank buffer solution) and a dose of 10mg/kg antibody drug conjugate was administered. The tumor volume was measured at day 0, day 7, day 14, day 21, day 24, day 28, day 32, day 36 and the tumor growth inhibition rate on day 28 of d was calculated.    Click to Show/Hide
In Vivo Model	A431 tumor bearing nude mouse model

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	6.22 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	SW620 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	7.37 nM	Positive HER2 expression (HER2+++/++)
Method Description	N87 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	8.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Fadu cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	28.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	BXPC-3 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	36.91 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	A431 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.37%	Positive HER2 expression (HER2+++/++)
Method Description	3x104 A431 cells were injected subcutaneously into the right shoulder of 4-6-week-old BALB/c nude mice, and when the average tumor size of the mice grew to 140 ~ 150mm3, they were randomly divided into 5 cells in each group. At day 0, day 7, day 14, day 21, intravenous injection of a blank control (blank buffer solution) and a dose of 10mg/kg antibody drug conjugate was administered. The tumor volume was measured at day 0, day 7, day 14, day 21, day 24, day 28, day 32, day 36 and the tumor growth inhibition rate on day 28 of d was calculated.    Click to Show/Hide
In Vivo Model	A431 tumor bearing nude mouse model

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC54)	0.008 nM	Positive HER2 expression (HER2+++/++)
Method Description	Fadu cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC54)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	N87 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC54)	0.42 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	SW620 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC54)	1.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	BXPC-3 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC54)	10.98 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	A431 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.53%	Positive HER2 expression (HER2+++/++)
Method Description	In the SKOV3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	SKOV3 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.53%	Positive HER2 expression (HER2+++/++)
Method Description	In the SKOV3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	SKOV3 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.82%	Positive HER2 expression (HER2+++/++)
Method Description	3x104 A431 cells were injected subcutaneously into the right shoulder of 4-6-week-old BALB/c nude mice, and when the average tumor size of the mice grew to 140 ~ 150mm3, they were randomly divided into 5 cells in each group. At day 0, day 7, day 14, day 21, intravenous injection of a blank control (blank buffer solution) and a dose of 10mg/kg antibody drug conjugate was administered. The tumor volume was measured at day 0, day 7, day 14, day 21, day 24, day 28, day 32, day 36 and the tumor growth inhibition rate on day 28 of d was calculated.    Click to Show/Hide
In Vivo Model	A431 tumor bearing nude mouse model

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC52)	2.97 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	SW620 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC52)	3.21 nM	Positive HER2 expression (HER2+++/++)
Method Description	Fadu cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC52)	4.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	N87 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC52)	10.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	BXPC-3 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC52)	22.24 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	A431 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 100%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 1 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	< 10%	Negative HER2 expression (HER2-)
Method Description	Growth inhibition test of HER2-negative human breast cancer cell line (MDA-MB-231). The cells were seeded at 1000 cells / 100 pL / well. The cells were cultured at 37 0 C overnight, then the medium was exchanged with new one (95 uL/well), and the cells were treated with a test compound, which was adjusted to 2 ug/mL with PBS , at 5 uL/well (treatment concentration: 100 ng/mL). The cells were cultured for 6 days, then CellTiter-Glo was added thereto at 100 uL/well, and the luminescence amount of each well was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	102%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 100%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 100%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 104%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 1 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 100%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 105%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 1 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 100%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 100%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 101%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[221]
Efficacy Data	Tumor Growth lnhibition value (TGl)	101%
Method Description	Animal experiments were conducted in accordance with protocols approved by the Institutional Animal Care and Use Committee of Seoul National University. A heterogeneous tumor model was established by subcutaneously injecting a mixture of 1 × 107 JIMT-1 cells and 2.5 × 106 MDA-MB-231 cells in 100 uL PBS into the dorsal flank of 6-week-old female NU/J mice (OrientBio) [29]. This 4:1 co-implantation reflects the diverse composition often observed in advanced HER2-positive breast cancer while ensuring enough HER2-negative cells to model intratumor heterogeneity [29]. When tumors reached approximately 150 mm3, mice were randomly assigned to different experimental groups and received intravenous injections of PBS (Control), IgG DEVD ADC, HER2 DEVD ADC, or T-Dxd (trastuzumab deruxtecan) at a dose of 5 mg/kg weekly for four weeks. This 5 mg/kg dose aligns with the range commonly used in prior preclinical trastuzumab-based ADC evaluations [7,12] and follows recent analysis [30] suggesting that efficacy in mice is most meaningful when the mg/kg dose approximates the maximum tolerated dose seen in human trials. Tumor volumes and body weights were measured every three days. Tumor volume was calculated using the ellipsoidal formula: volume = (length × width2)/2. The tumor growth inhibition (%TGI) was calculated using the formula: %TGI = [1 - (Tt/T0)/ (Ct/C0)]/[1- (C0/Ct)] × 100, where Tt and Ct are the mean tumor volumes of the treatment and control groups at the endpoint, and T0 and C0 are the initial tumor volumes. Mice were euthanized when tumors exceeded 1000 mm3 or if severe distress was observed. Tumors were harvested for histological analysis.    Click to Show/Hide
In Vivo Model	HER2-positive JIMT-1 cells and HER2-negative MDA-MB-231 cells in a 4:1 ratio Immunodeficient mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 102%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 103%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Tumor Growth lnhibition value (TGl)	105.80%	Positive HER2 expression (HER2+++/++)
Method Description	In the SKOV3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	SKOV3 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Tumor Growth lnhibition value (TGl)	105.80%	Positive HER2 expression (HER2+++/++)
Method Description	In the SKOV3 xenograft model, the ADCs were administered at 5 mg/kg (once, IV).
In Vivo Model	SKOV3 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Half Maximal Effective Concentration (EC50)	36 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	MDA-MB-453 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC1 for 120 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Half Maximal Effective Concentration (EC50)	43 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC1 for 120 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Half Maximal Effective Concentration (EC50)	62 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	BT-474 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC1 for 120 h.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Half Maximal Effective Concentration (EC50)	82 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	NCI-N87 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC1 for 120 h.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[214]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10000 ng/mL	Negative HER2 expression (HER2-)
Method Description	MDA-MB-468 cells were seeded in 96-well cell culture plates for 24 hours before treatment. Cells were treated with ADC1 for 120 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 106%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 1 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 107%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 1 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	99.30%
In Vivo Model	NCI-N87/MDA-MB-231 co-incubation model 2 mpk
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%
In Vivo Model	NCI-N87 CDX model 3 mpk
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%
In Vivo Model	NCI-N87 CDX model 1 mpk

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.071 nM
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.091 nM
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.674 nM
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[222]
Efficacy Data	stable disease (SD)	33%
Patients Enrolled	Eligibility requires adults (≥18) with incurable HER2+ (IHC≥1+/ISH/NGS-confirmed) malignancies who exhausted standard therapies, with adequate hematologic/organ function (ANC≥1500/uL, CrCl≥50mL/min, LVEF≥45%), excluding those with cardiac dysfunction (NYHA III-IV, QTc>470ms), active hepatitis/HIV, uncontrolled comorbidities, prior trastuzumab intolerance, or symptomatic brain metastases. Fertile patients must use contraception for 7 months post-treatment.    Click to Show/Hide
Administration Dosage	Six dose levels have been selected for evaluation in the Phase I part of the study: 0.3, 0.6, 1.2, 2.4, 3.6, and 4.8 mg/kg of A166
Related Clinical Trial
NCT Number	NCT03602079	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Phase I-II, FIH Study of A166 in Locally Advanced/Metastatic Solid Tumors Expressing Human Epidermal Growth Factor Receptor 2 (HER2) or Are HER2 Amplified That Did Not Respond or Stopped Responding to Approved Therapies
Primary Endpoint	The phase I primary endpoint evaluates maximum tolerated dose (MTD) and dose-limiting toxicities (DLTs) in HER2-positive advanced cancer patients over a 21-day DLT observation period, with continuous safety monitoring up to 24 months.
Other Endpoint	Secondary phase I objectives include comprehensive safety assessment (CTCAE v4.03 graded AEs, immunogenicity via anti-drug antibodies) and pharmacokinetic profiling (Cmax, CL, AUC, hale-life, Vz, Vss) through 84-day PK sampling in this dose-escalation study.
Experiment 2 Reporting the Activity Date of This ADC					[222]
Efficacy Data	progressive disease (PD)	41%
Patients Enrolled	Eligibility requires adults (≥18) with incurable HER2+ (IHC≥1+/ISH/NGS-confirmed) malignancies who exhausted standard therapies, with adequate hematologic/organ function (ANC≥1500/uL, CrCl≥50mL/min, LVEF≥45%), excluding those with cardiac dysfunction (NYHA III-IV, QTc>470ms), active hepatitis/HIV, uncontrolled comorbidities, prior trastuzumab intolerance, or symptomatic brain metastases. Fertile patients must use contraception for 7 months post-treatment.    Click to Show/Hide
Administration Dosage	Six dose levels have been selected for evaluation in the Phase I part of the study: 0.3, 0.6, 1.2, 2.4, 3.6, and 4.8 mg/kg of A166
Related Clinical Trial
NCT Number	NCT03602079	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Phase I-II, FIH Study of A166 in Locally Advanced/Metastatic Solid Tumors Expressing Human Epidermal Growth Factor Receptor 2 (HER2) or Are HER2 Amplified That Did Not Respond or Stopped Responding to Approved Therapies
Primary Endpoint	The phase I primary endpoint evaluates maximum tolerated dose (MTD) and dose-limiting toxicities (DLTs) in HER2-positive advanced cancer patients over a 21-day DLT observation period, with continuous safety monitoring up to 24 months.
Other Endpoint	Secondary phase I objectives include comprehensive safety assessment (CTCAE v4.03 graded AEs, immunogenicity via anti-drug antibodies) and pharmacokinetic profiling (Cmax, CL, AUC, hale-life, Vz, Vss) through 84-day PK sampling in this dose-escalation study.
Experiment 3 Reporting the Activity Date of This ADC					[222]
Efficacy Data	Partial Response (PR)	26%
Patients Enrolled	Eligibility requires adults (≥18) with incurable HER2+ (IHC≥1+/ISH/NGS-confirmed) malignancies who exhausted standard therapies, with adequate hematologic/organ function (ANC≥1500/uL, CrCl≥50mL/min, LVEF≥45%), excluding those with cardiac dysfunction (NYHA III-IV, QTc>470ms), active hepatitis/HIV, uncontrolled comorbidities, prior trastuzumab intolerance, or symptomatic brain metastases. Fertile patients must use contraception for 7 months post-treatment.    Click to Show/Hide
Administration Dosage	Six dose levels have been selected for evaluation in the Phase I part of the study: 0.3, 0.6, 1.2, 2.4, 3.6, and 4.8 mg/kg of A166
Related Clinical Trial
NCT Number	NCT03602079	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Phase I-II, FIH Study of A166 in Locally Advanced/Metastatic Solid Tumors Expressing Human Epidermal Growth Factor Receptor 2 (HER2) or Are HER2 Amplified That Did Not Respond or Stopped Responding to Approved Therapies
Primary Endpoint	The phase I primary endpoint evaluates maximum tolerated dose (MTD) and dose-limiting toxicities (DLTs) in HER2-positive advanced cancer patients over a 21-day DLT observation period, with continuous safety monitoring up to 24 months.
Other Endpoint	Secondary phase I objectives include comprehensive safety assessment (CTCAE v4.03 graded AEs, immunogenicity via anti-drug antibodies) and pharmacokinetic profiling (Cmax, CL, AUC, hale-life, Vz, Vss) through 84-day PK sampling in this dose-escalation study.
Experiment 4 Reporting the Activity Date of This ADC					[222]
Efficacy Data	Disease control rate (DCR)	59%
Patients Enrolled	Eligibility requires adults (≥18) with incurable HER2+ (IHC≥1+/ISH/NGS-confirmed) malignancies who exhausted standard therapies, with adequate hematologic/organ function (ANC≥1500/uL, CrCl≥50mL/min, LVEF≥45%), excluding those with cardiac dysfunction (NYHA III-IV, QTc>470ms), active hepatitis/HIV, uncontrolled comorbidities, prior trastuzumab intolerance, or symptomatic brain metastases. Fertile patients must use contraception for 7 months post-treatment.    Click to Show/Hide
Administration Dosage	Six dose levels have been selected for evaluation in the Phase I part of the study: 0.3, 0.6, 1.2, 2.4, 3.6, and 4.8 mg/kg of A166
Related Clinical Trial
NCT Number	NCT03602079	Clinical Status	PHASE1|||PHASE2
Clinical Description	A Phase I-II, FIH Study of A166 in Locally Advanced/Metastatic Solid Tumors Expressing Human Epidermal Growth Factor Receptor 2 (HER2) or Are HER2 Amplified That Did Not Respond or Stopped Responding to Approved Therapies
Primary Endpoint	The phase I primary endpoint evaluates maximum tolerated dose (MTD) and dose-limiting toxicities (DLTs) in HER2-positive advanced cancer patients over a 21-day DLT observation period, with continuous safety monitoring up to 24 months.
Other Endpoint	Secondary phase I objectives include comprehensive safety assessment (CTCAE v4.03 graded AEs, immunogenicity via anti-drug antibodies) and pharmacokinetic profiling (Cmax, CL, AUC, hale-life, Vz, Vss) through 84-day PK sampling in this dose-escalation study.
Experiment 5 Reporting the Activity Date of This ADC					[257]
Patients Enrolled	Eligibility requires adults (≥18) with incurable HER2+ (IHC≥1+/ISH/NGS-confirmed) solid tumors who have exhausted standard therapies, with adequate organ function and ECOG 0-1.
Administration Dosage	According to the initial dose, the highest dose and the modified Fibonacci method, the dose escalation of A166 for injection is designed as: 0.1 mg/kg, 0.3 mg/kg, 0.6 mg/kg, 1.2 mg/kg, 2.4 mg/kg, 3.6 mg/kg, 4.8 mg/kg (the highest dose is tentatively set at 4.8 mg/kg).
Related Clinical Trial
NCT Number	NCT05311397	Clinical Status	PHASE1
Clinical Description	A Phase I Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of A166 in Patients With Unresectable, Locally Advanced or Metastatic HER2-expressing Solid Tumors (KL166-I-01-CTP)
Primary Endpoint	Primary endpoint evaluates investigator-assessed ORR (CR+PR) per RECIST v1.1 criteria in HER2-positive advanced solid tumor patients over 24 months.
Other Endpoint	Secondary endpoints include 24-month assessments of DOR (from first response to PD/death), PFS (from randomization to PD/death), and OS (from randomization to death/loss to follow-up), all measured according to RECIST v1.1 standards.
Experiment 6 Reporting the Activity Date of This ADC					[258]
Patients Enrolled	Eligibility includes adults (18-75y) with confirmed HER2+ (IHC3+ or IHC2+/FISH+) metastatic breast cancer and prior taxane exposure, excluding those with cardiac dysfunction (NYHA III-IV/QTc prolongation), active ILD, uncontrolled CNS metastases, or trastuzumab intolerance, while requiring adequate organ function for safety evaluation.
Administration Dosage	4.8 mg/kg for each 21 day cycle
Related Clinical Trial
NCT Number	NCT05346328	Clinical Status	PHASE2
Clinical Description	An Open-clinical Trial Phase II, Injection of A166 for HER2-positive Patients With Refractory Unresectable Locally Advanced or Metastatic Breast Cancer;KL166-IIS-001
Primary Endpoint	The primary endpoint evaluates ORR (complete/partial response rates per RECIST 1.1) in HER2-positive metastatic breast cancer patients over 24 months, focusing on heavily pretreated populations who failed ≥3 prior HER2-targeted therapies including trastuzumab, TKIs, and ADCs.
Other Endpoint	Secondary objectives assess 24-month efficacy through PFS (first dose to progression/death), DCR/CRB (response+stable disease), DOR (response duration), TTR (time to progression excluding deaths), and OS (overall survival from first dose), all measured by RECIST 1.1 standards in this refractory patient population.
Experiment 7 Reporting the Activity Date of This ADC					[259]
Efficacy Data	Partial Response (PR)	25.92%
Patients Enrolled	Locally advanced/metastatic solid tumors expressing human epidermal growth factor receptor 2 (HER2) or are HER2 amplified.
Administration Dosage	0.30, 1.20, 3.60, 4.80 mg/kg, every 3 weeks from date of enrollment until the date of first documented progression or date of death from any cause, whichever came first, assessed up to 24 months.
Related Clinical Trial
NCT Number	NCT03602079	Clinical Status	Phase 1
Clinical Description	A phase 1-2, FIH Study of A166 in locally advanced/metastatic solid tumors expressing human epidermal growth factor receptor 2 (HER2) or are HER2 amplified that did not respond or stopped responding to approved therapies.
Primary Endpoint	Overall incidence of ophthalmic toxicities in the 3.60 mg/kg cohort was 80% and in the 4.80 mg/kg cohort it was 83.00%. Responses were seen only at the dose levels of 3.60 mg/kg and 4.80 mg/kg. Among the 27 patients evaluable for efficacy,best response was progression of disease in 11 patients (40.74%), stable disease in 9 patients (33.33%) and partial response in 7 patients (25.92%),for the total disease control rate of 59%.    Click to Show/Hide
Experiment 8 Reporting the Activity Date of This ADC					[260]
Efficacy Data	Objective Response Rate (ORR)	73.90 68.60 %
Patients Enrolled	Patients with HER2-expressing advanced solid tumours.
Administration Dosage	0.10, 0.30, 0.60, 1.20, 2.40, 3.60, 4.80 or 6.00 mg/kg Q3W.
Related Clinical Trial
NCT Number	NCT05311397	Clinical Status	Phase 1
Clinical Description	A phase 1 study to evaluate the safety, tolerability, pharmacokinetics and preliminary efficacy of A166 in patients with unresectable, locally advanced or metastatic HER2-expressing solid tumors (KL166-I-01-CTP).
Experiment 9 Reporting the Activity Date of This ADC					[261]
Related Clinical Trial
NCT Number	NCT05346328	Clinical Status	Phase 2
Clinical Description	An open-clinical trial phase , injection of A166 for HER2-positive patients with refractory unresectable locally advanced or metastatic breast cancer KL166-2S-001.
Experiment 10 Reporting the Activity Date of This ADC					[262]
Related Clinical Trial
NCT Number	NCT03602079	Clinical Status	Phase 1/2
Clinical Description	A phase 1-2, FIH study of A166 in locally advanced/metastatic solid tumors expressing human epidermal growth factor receptor 2 (HER2) or are HER2 amplified that did not respond or stopped responding to approved therapies.

Experiment 1 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Ninety Percent Inhibitory Concentration (IC90)	0.11- 0.28 ng/mL	Negative HER2 expression (HER2-)
Method Description	We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1937 cells		CVCL_0290
Experiment 2 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Ninety Percent Inhibitory Concentration (IC90)	0.27- 0.38 ng/mL	High HER2 expression (HER2 +++)
Method Description	We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.18 ng/mL	Negative HER2 expression (HER2-)
Method Description	We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1937 cells		CVCL_0290
Experiment 4 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.32 ng/mL	High HER2 expression (HER2 +++)
Method Description	We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Ninety Percent Inhibitory Concentration (IC90)	0.17- 0.55 ng/mL	Negative HER2 expression (HER2-)
Method Description	We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1937 cells		CVCL_0290
Experiment 2 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Ninety Percent Inhibitory Concentration (IC90)	0.19- 0.31 ng/mL	High HER2 expression (HER2 +++)
Method Description	We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.24 ng/mL	High HER2 expression (HER2 +++)
Method Description	We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.31 ng/mL	Negative HER2 expression (HER2-)
Method Description	We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1937 cells		CVCL_0290

Experiment 1 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Ninety Percent Inhibitory Concentration (IC90)	0.86- 1.28 ng/mL	High HER2 expression (HER2 +++)
Method Description	We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Ninety Percent Inhibitory Concentration (IC90)	1.46- 2.69 ng/mL	Negative HER2 expression (HER2-)
Method Description	We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1937 cells		CVCL_0290
Experiment 3 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.05 ng/mL	High HER2 expression (HER2 +++)
Method Description	We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[223]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.98 ng/mL	Negative HER2 expression (HER2-)
Method Description	We added 100 uL of media containing the drug to be tested (drug by concentration + 1 % FBS). We added PBS to surrounding wells to prevent evaporation. we cultivate in conditions of 37°C and 5 % CO2 according to the set time (Payload: initial observation and observes 48hr, 72hr, and 96hr culture conditions to select appropriate culture conditions). For Antibody and ADC, we selected appropriate culture conditions by observing culture conditions for 96hr, 120hr, and 144hr. In the case of 120hr and 144hr incubation conditions, we added additional media after 72hr incubation (The concentration of the drug is set to 3 below and 3 above based on the IC50 value used as a reference). Positive control usually uses etoposide 10 uM or 24 uM, and negative control uses DMSO with same concentration of drug and a positive control with SN38 or etoposide for validating the assay system (data not shown).    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1937 cells		CVCL_0290

Experiment 1 Reporting the Activity Date of This ADC					[224]
Efficacy Data	Max Tumor Growth lnhibition value (TGl) (d)	> 50%	Positive TLR expression (TLR+++/++)
Method Description	ADC30 was tested in mouse M38 CRC model in C57BL/6 mice, 3 mg/kg, QWx3, IV
In Vivo Model	Mouse MC38 CRC Model in C57BL/6 Mice

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC63)	13.08 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	SW620 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC63)	15.98 nM	Positive HER2 expression (HER2+++/++)
Method Description	Fadu cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC63)	21.2 nM	Positive HER2 expression (HER2+++/++)
Method Description	N87 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC63)	23.21 nM	Positive HER2 expression (HER2+++/++)
Method Description	BXPC-3 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC63)	36.49 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	A431 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC60)	9.03 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	SW620 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC60)	11.86 nM	Positive HER2 expression (HER2+++/++)
Method Description	N87 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC60)	13.57 nM	Positive HER2 expression (HER2+++/++)
Method Description	Fadu cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC60)	35.66 nM	Positive HER2 expression (HER2+++/++)
Method Description	BXPC-3 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC60)	43.81 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	A431 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC58)	13.56 nM	Positive HER2 expression (HER2+++/++)
Method Description	Fadu cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC58)	14.53 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	SW620 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC58)	26.79 nM	Positive HER2 expression (HER2+++/++)
Method Description	N87 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC58)	48.96 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	A431 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC58)	98.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	BXPC-3 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[225]
Efficacy Data	Half Maximal inhibitory Concentration (lC57)	0.144 nM	Positive HER2 expression (HER2+++/++)
Method Description	Chemiluminescence staining (Luminescent Cell Viability Assay) was carried out, and IC12owas calculated after reading the fluorescence data.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[225]
Efficacy Data	Half Maximal inhibitory Concentration (lC56)	0.312 nM	Positive HER2 expression (HER2+++/++)
Method Description	Chemiluminescence staining (Luminescent Cell Viability Assay) was carried out, and IC11owas calculated after reading the fluorescence data.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC57)	15.23 nM	Positive HER2 expression (HER2+++/++)
Method Description	Fadu cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC57)	16.55 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	SW620 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC57)	35.31 nM	Positive HER2 expression (HER2+++/++)
Method Description	N87 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC57)	62.25 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	A431 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC57)	87.78 nM	Positive HER2 expression (HER2+++/++)
Method Description	BXPC-3 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC56)	2.24 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	SW620 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC56)	4.01 nM	Positive HER2 expression (HER2+++/++)
Method Description	Fadu cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC56)	4.52 nM	Positive HER2 expression (HER2+++/++)
Method Description	N87 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC56)	11.22 nM	Positive HER2 expression (HER2+++/++)
Method Description	BXPC-3 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC56)	16.35 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	A431 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC55)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Fadu cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC55)	1.15 nM	Positive HER2 expression (HER2+++/++)
Method Description	N87 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC55)	1.23 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	SW620 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC55)	6.09 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	A431 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC55)	21.9 nM	Positive HER2 expression (HER2+++/++)
Method Description	BXPC-3 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[225]
Efficacy Data	Half Maximal inhibitory Concentration (lC55)	16.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	Chemiluminescence staining (Luminescent Cell Viability Assay) was carried out, and IC10owas calculated after reading the fluorescence data.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[225]
Efficacy Data	Half Maximal inhibitory Concentration (lC54)	0.049 nM	Positive HER2 expression (HER2+++/++)
Method Description	Chemiluminescence staining (Luminescent Cell Viability Assay) was carried out, and IC9owas calculated after reading the fluorescence data.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC53)	5.89 nM	Positive HER2 expression (HER2+++/++)
Method Description	Fadu cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC53)	6.43 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	SW620 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC53)	7.89 nM	Positive HER2 expression (HER2+++/++)
Method Description	N87 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC53)	19.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	BXPC-3 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC53)	28.77 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	A431 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[225]
Efficacy Data	Half Maximal inhibitory Concentration (lC53)	18.5 nM	Positive HER2 expression (HER2+++/++)
Method Description	Chemiluminescence staining (Luminescent Cell Viability Assay) was carried out, and IC8owas calculated after reading the fluorescence data.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[225]
Efficacy Data	Half Maximal inhibitory Concentration (lC52)	0.187 nM	Positive HER2 expression (HER2+++/++)
Method Description	Chemiluminescence staining (Luminescent Cell Viability Assay) was carried out, and IC7owas calculated after reading the fluorescence data.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[225]
Efficacy Data	Half Maximal inhibitory Concentration (lC51)	0.113 nM	Positive HER2 expression (HER2+++/++)
Method Description	Chemiluminescence staining (Luminescent Cell Viability Assay) was carried out, and IC6owas calculated after reading the fluorescence data.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC51)	9.82 nM	Positive HER2 expression (HER2+++/++)
Method Description	N87 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC51)	10.98 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	SW620 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 3 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC51)	11.31 nM	Positive HER2 expression (HER2+++/++)
Method Description	Fadu cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 4 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC51)	32.13 nM	Positive HER2 expression (HER2+++/++)
Method Description	BXPC-3 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC					[220]
Efficacy Data	Half Maximal inhibitory Concentration (lC51)	41.67 nM	Positive HER2 and EGFR expression (HER2 and EGFR+++/++)
Method Description	A431 cells were used as in vitro pharmacodynamic detection systems. An appropriate number of tumor cell lines were inoculated in 96-well plates, incubated in carbon dioxide incubators for 24 hours, and then treated with medicine. The drug was diluted in a medium (the initial concentration of ADC drug was 500nM, the dilution factor was 7 times, there were 8 concentration points, the theoretical coupling ratio (DAR) of toxin and antibody was 8:1, and the actual coupling ratio was roughly 7.5:1, so the initial concentration of toxin was 4.0 uM, 7 times concentration gradient dilution, 8 concentration points). After mixing, it was added into the corresponding cell holes and incubated at 37°C in carbon dioxide incubator for 5 days. After 5 days, 20uL MTS was added to each well (Promega, G3581) reacted for 2 hours, and the absorption value reading at 490nm was taken with an enzyme label. By detecting the activity of dehydrogenase in mitochondria, IC50 was calculated to evaluate the inhibitory effect of ADC drugs on the proliferation of tumor cells.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[226]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	. pM	High HER2 expression (HER2 +++)
Method Description	A Cell line test on SKBR-3
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[226]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	. pM	High HER2 expression (HER2 +++)
Method Description	A Cell line test on SKBR-3
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	8 pM	High HER2 expression (HER2 +++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	6 nM	Moderate HER2 expression (HER2++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0024 uM	High TROP2 expression (TROP2 +++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-468 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.018 uM	Low TROP2 expression (TROP2+)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the BxPc-3 cell.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.18 uM	High TROP2 expression (TROP2 +++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-231 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 6 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.34 uM	Low TROP2 expression (TROP2+)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the CFPAC cell.
In Vitro Model	Cystic fibrosis, Pancreatic ductal adenocarcinoma	CFPAC cells		CVCL_1119
Experiment 7 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.4 uM	Moderate Trop2 expression (Trop2++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the AsPc1 cell.
In Vitro Model	Pancreatic ductal adenocarcinoma	AsPc1 cells		CVCL_0152

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 15 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15-25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15-25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 15 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15-25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 15 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15-25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 15 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15-25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15-25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[215]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 25 pM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[226]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	35.06 pM	High HER2 expression (HER2 +++)
Method Description	A Cell line test on SKBR-3
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[226]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	36.15 pM	High HER2 expression (HER2 +++)
Method Description	A Cell line test on SKBR-3
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[226]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	44.88 pM	High HER2 expression (HER2 +++)
Method Description	A Cell line test on SKBR-3
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[226]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	47.82 pM	High HER2 expression (HER2 +++)
Method Description	A Cell line test on SKBR-3
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[226]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	109.2 pM	High HER2 expression (HER2 +++)
Method Description	A Cell line test on SKBR-3
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[226]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	790.08 pM	High HER2 expression (HER2 +++)
Method Description	A Cell line test on SKBR-3
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.002 nM	High HER2 expression (HER2 +++)
Method Description	A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 30 nM	Negative HER2 expression (HER2-)
Method Description	A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.002 nM	High HER2 expression (HER2 +++)
Method Description	A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.002829 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to BT-474 cells
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.008852 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.2212 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to NCI-N87 cells
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.449 nM	Low HER2 expression (HER2+)
Method Description	Cytotoxicity of ADC to T47D cells
In Vitro Model	Invasive breast carcinoma of no special type	T47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.003 nM	High HER2 expression (HER2 +++)
Method Description	A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.003 nM	High HER2 expression (HER2 +++)
Method Description	A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.003352 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.005559 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to BT-474 cells
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01479 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.3965 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to NCI-N87 cells
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	7.064 nM	Low HER2 expression (HER2+)
Method Description	Cytotoxicity of ADC to T47D cells
In Vitro Model	Invasive breast carcinoma of no special type	T47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.007 nM	High HER2 expression (HER2 +++)
Method Description	A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 30 nM	Negative HER2 expression (HER2-)
Method Description	A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0089 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.009 nM	High HER2 expression (HER2 +++)
Method Description	A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 30 nM	Negative HER2 expression (HER2-)
Method Description	A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01 nM	Positive her2 expression (her2+++/++)
Method Description	NCI N87 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 1000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01 nM	High her2 expression (her2 +++)
Method Description	SKBR3, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.41 nM	Low her2 expression (her2+)
Method Description	H358, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Minimally invasive lung adenocarcinoma	H358 cells		CVCL_1559

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.11 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-20 was tested in HCC1954,80ul,18&#4524h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.09 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-20 was tested in NCI-N87,80ul,18&#4524h
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.18 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-20 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 4 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Emax (TNF-a)	791.6 pg/mL	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-20 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01 nM	High HER2 expression (HER2 +++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01 nM	High HER2 expression (HER2 +++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0024 uM	High TROP2 expression (TROP2 +++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-468 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.016 uM	Low TROP2 expression (TROP2+)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the BxPc-3 cell.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.3 uM	High TROP2 expression (TROP2 +++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-231 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 5 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.33 uM	Low TROP2 expression (TROP2+)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the CFPAC cell.
In Vitro Model	Cystic fibrosis, Pancreatic ductal adenocarcinoma	CFPAC cells		CVCL_1119
Experiment 6 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.1 uM	Moderate Trop2 expression (Trop2++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the AsPc1 cell.
In Vitro Model	Pancreatic ductal adenocarcinoma	AsPc1 cells		CVCL_0152

Experiment 1 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01 nM	High HER2 expression (HER2 +++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01 nM	High HER2 expression (HER2 +++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.011 nM	High HER2 expression (HER10 +++)
Method Description	Trastuzumab-C-10 was tested in HCC1954,80ul,18&#4524h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.023 nM	High HER2 expression (HER11 +++)
Method Description	Trastuzumab-C-10 was tested in NCI-N87,80ul,18&#4524h
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	164.13 nM	High HER2 expression (HER12 +++)
Method Description	Trastuzumab-C-10 was tested in NCI-H358,80ul,18&#4524h
In Vitro Model	Minimally invasive lung adenocarcinoma	NCI-H358 cells		CVCL_1559
Experiment 4 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal Effective Concentration (EC50)	7.54 nM	High HER2 expression (HER13 +++)
Method Description	Trastuzumab-C-10 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 5 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Emax (TNF-a)	522.28 pg/mL	High HER2 expression (HER14 +++)
Method Description	Trastuzumab-C-10 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01116 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01165 nM	High HER2 expression (HER2 +++)
Method Description	On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0408 nM	High HER2 expression (HER2 +++)
Method Description	On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.    Click to Show/Hide
In Vitro Model	Breast carcinoma	ZR-75-30 cells		CVCL_1661
Experiment 3 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04618 nM	High HER2 expression (HER2 +++)
Method Description	On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma of no special type	UACC812 cells		CVCL_1781

Experiment 1 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.014 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-17 was tested in HCC1954,80ul,18&#4524h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.32 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-17 was tested in NCI-N87,80ul,18&#4524h
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.39 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-17 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 4 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Emax (TNF-a)	788.8 pg/mL	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-17 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.014 nM	High HER2 expression (HER2 +++)
Method Description	A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5 nM	Negative HER2 expression (HER2-)
Method Description	A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.015 nM	High HER2 expression (HER2 +++)
Method Description	A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.017 nM	High HER2 expression (HER15 +++)
Method Description	Trastuzumab-C-11 was tested in NCI-H358,80ul,18&#4524h
In Vitro Model	Minimally invasive lung adenocarcinoma	NCI-H358 cells		CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.026 nM	High HER2 expression (HER16 +++)
Method Description	Trastuzumab-C-11 was tested in NCI-H358,80ul,18&#4524h
In Vitro Model	Minimally invasive lung adenocarcinoma	NCI-H358 cells		CVCL_1559
Experiment 3 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	331.62 nM	High HER2 expression (HER17 +++)
Method Description	Trastuzumab-C-11 was tested in NCI-H358,80ul,18&#4524h
In Vitro Model	Minimally invasive lung adenocarcinoma	NCI-H358 cells		CVCL_1559
Experiment 4 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal Effective Concentration (EC50)	32.59 nM	High HER2 expression (HER18 +++)
Method Description	Trastuzumab-C-11 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 5 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Emax (TNF-a)	427.95 pg/mL	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-11 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.017 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-15 was tested in HCC1954,80ul,18&#4524h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.17 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-15 was tested in NCI-N87,80ul,18&#4524h
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal Effective Concentration (EC50)	74.62 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-15 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 4 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Emax (TNF-a)	817.79 pg/mL	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-15 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0179 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.018 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-16 was tested in HCC1954,80ul,18&#4524h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.15 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-16 was tested in NCI-N87,80ul,18&#4524h
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal Effective Concentration (EC50)	4.61 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-16 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 4 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Emax (TNF-a)	411.5 pg/mL	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-16 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.018 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-21 was tested in HCC1954,80ul,18&#4524h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.12 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-21 was tested in NCI-N87,80ul,18&#4524h
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.13 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-21 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 4 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Emax (TNF-a)	573.7 pg/mL	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-21 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	Positive her2 expression (her2+++/++)
Method Description	NCI N87 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 1000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	High her2 expression (her2 +++)
Method Description	SKBR3, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.32 nM	Low her2 expression (her2+)
Method Description	H358, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Minimally invasive lung adenocarcinoma	H358 cells		CVCL_1559

Experiment 1 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	Low her2 expression (her2+)
Method Description	MCF7, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.05 nM	Positive her2 expression (her2+++/++)
Method Description	NCI N87 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 1000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.05 nM	High her2 expression (her2 +++)
Method Description	SKBR3, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.96 nM	Low her2 expression (her2+)
Method Description	H358, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Minimally invasive lung adenocarcinoma	H358 cells		CVCL_1559

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	300 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	300 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	24.18 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	30.6 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	29.01 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	64.66 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.35 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.91 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.13 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.68 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.14 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.37 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	300 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	High HER2 expression (HER2 +++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0036 uM	High TROP2 expression (TROP2 +++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-468 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.013 uM	Low TROP2 expression (TROP2+)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the BxPc-3 cell.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.25 uM	High TROP2 expression (TROP2 +++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-231 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 5 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.29 uM	Low TROP2 expression (TROP2+)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the CFPAC cell.
In Vitro Model	Cystic fibrosis, Pancreatic ductal adenocarcinoma	CFPAC cells		CVCL_1119
Experiment 6 Reporting the Activity Date of This ADC					[249]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.8 uM	Moderate Trop2 expression (Trop2++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the AsPc1 cell.
In Vitro Model	Pancreatic ductal adenocarcinoma	AsPc1 cells		CVCL_0152

Experiment 1 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	High HER2 expression (HER2 +++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	High HER2 expression (HER2 +++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	High HER2 expression (HER2 +++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[233]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02&#1770.01 nM	High HER2 expression (HER2 +++)
Method Description	Cells were seeded in 96-well plates at a density of 2000 cells/well for MDA-MB-231 cells and 5 000 cells/well for all the other cell lines and allowed to grow under normal oxygen conditions (20% O2). Cells were treated with the appropriate compound 24 h after plating and maintained at 37 °C under a humidified 5% CO2 and 20% O2 atmosphere. Cell viability was measured 72 or 120 h later with the WST-1 cell proliferation assay (Takara) according to the manufacturer's instructions. To represent the relative cell proliferation rate, results were normalized against the untreated condition.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0208 nM	High HER2 expression (HER2 +++)
Method Description	On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.076 nM	High HER2 expression (HER2 +++)
Method Description	On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.    Click to Show/Hide
In Vitro Model	Breast carcinoma	ZR-75-30 cells		CVCL_1661
Experiment 3 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.09663 nM	High HER2 expression (HER2 +++)
Method Description	On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma of no special type	UACC812 cells		CVCL_1781

Experiment 1 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.021 nM	High HER2 expression (HER5 +++)
Method Description	Trastuzumab-C-9 was tested in NCI-H358,80ul,18&#4524h
In Vitro Model	Minimally invasive lung adenocarcinoma	NCI-H358 cells		CVCL_1559
Experiment 2 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.058 nM	High HER2 expression (HER6 +++)
Method Description	Trastuzumab-C-9 was tested in NCI-H358,80ul,18&#4524h
In Vitro Model	Minimally invasive lung adenocarcinoma	NCI-H358 cells		CVCL_1559
Experiment 3 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	136.77 nM	High HER2 expression (HER7 +++)
Method Description	Trastuzumab-C-9 was tested in NCI-H358,80ul,18&#4524h
In Vitro Model	Minimally invasive lung adenocarcinoma	NCI-H358 cells		CVCL_1559
Experiment 4 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal Effective Concentration (EC50)	24.41 nM	High HER2 expression (HER8 +++)
Method Description	Trastuzumab-C-9 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 5 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Emax (TNF-a)	470.23 pg/mL	High HER2 expression (HER9 +++)
Method Description	Trastuzumab-C-9 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[229]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02107 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.03 nM	Low her2 expression (her2+)
Method Description	MCF7, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.05 nM	Positive her2 expression (her2+++/++)
Method Description	NCI N87 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 1000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.05 nM	High her2 expression (her2 +++)
Method Description	SKBR3, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.68 nM	Low her2 expression (her2+)
Method Description	H358, 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 2000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Minimally invasive lung adenocarcinoma	H358 cells		CVCL_1559

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	10.74 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	300 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.18 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.89 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10 nM	Moderate HER2 expression (HER2++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10 nM	Negative HER2 expression (HER2-)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	1250cells/well for SK-BR-3 (100 uL) of cells were seeded onto 384-well plates and incubated for 24 hours before adding the ADC. After 9 hours, the limited exposure treated plates were removed from the incubator and media containing compound was removed. Cells were washed 2x with growth medium and 40 uL growth medium was then added to each well. Plates were incubated at 37 °C/5% CO, for a further 96 hours. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.68 nM	High HER2 expression (HER2 +++)
Method Description	1250cells/well for SK-BR-3 (100 uL) of cells were seeded onto 384-well plates and incubated for 24 hours before adding the ADC. After 9 hours, the limited exposure treated plates were removed from the incubator and media containing compound was removed. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	1250cells/well for SK-BR-3 (100 uL) of cells were seeded onto 384-well plates and incubated for 24 hours before adding the ADC. After 9 hours, the limited exposure treated plates were removed from the incubator and media containing compound was removed. Cells were washed 2x with growth medium and 40 uL growth medium was then added to each well. Plates were incubated at 37 °C/5% CO, for a further 96 hours. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[217]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.18 nM	High HER2 expression (HER2 +++)
Method Description	1250cells/well for SK-BR-3 (100 uL) of cells were seeded onto 384-well plates and incubated for 24 hours before adding the ADC. After 9 hours, the limited exposure treated plates were removed from the incubator and media containing compound was removed. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.11 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.45 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	300 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	300 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10 nM	Moderate HER2 expression (HER2++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10 nM	Negative HER2 expression (HER2-)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.047 nM	High HER2 expression (HER2 +++)
Method Description	Cultivate the cell line in a tissue culture incubator at 5% CO2 and 37 °C in the optimal growth medium. Separate cells at least 2 days prior to inoculation for proliferation assays to ensure optimal growth density. On the day of vaccination, cell viability and cell density were determined using a cell counter (Vi Cell XR Cell viability analyzer, Beckman Coulter). Inoculate cells with vitality above 85% into a 384 well TC treated plate (Corning catalog number 3765) with a white transparent bottom. Inoculate cells at a density of 1000 cells per well into 45 u L of standard growth medium. Incubate the plate overnight in a tissue culture incubator at 5% CO2 and 37 °C. On the second day, prepare free atorvastatin payload and targeted ADC at a 10 fold ratio in standard growth medium. Add the prepared treatment substance to the cells to obtain a final concentration of 0.005-100nM and a final volume of 50 u L/well. Each drug concentration is tested in quadruplicate. Incubate the plates in a tissue culture incubator at 5% CO2 and 37 °C for 5 days, and then evaluate cell viability by adding 25 u L of CellTiterGlo (Promega, catalog number G7573) (a reagent for cell lysis and measurement of total adenosine triphosphate (ATP) content). Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal, and then read using a luminescence reader (EnVision multi label enzyme-linked immunosorbent assay, PerkinElmer). To evaluate the effectiveness of drug treatment, luminescence counts from wells containing untreated cells (100% viability) were used to normalize the treated samples. Apply a variable slope model to fit the nonlinear regression curve to the data in GraphPad PRISM version 7.02 software. Extrapolating IC50 from the obtained curve    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.053 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-21 was tested in HCC1954,80ul,18&#4524h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.103 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-21 was tested in NCI-N87,80ul,18&#4524h
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.05 nM	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-21 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 4 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Emax (TNF-a)	1562.5 pg/mL	High HER2 expression (HER19 +++)
Method Description	Trastuzumab-C-21 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.057 nM	High HER2 expression (HER2 +++)
Method Description	Cultivate the cell line in a tissue culture incubator at 5% CO2 and 37 °C in the optimal growth medium. Separate cells at least 2 days prior to inoculation for proliferation assays to ensure optimal growth density. On the day of vaccination, cell viability and cell density were determined using a cell counter (Vi Cell XR Cell viability analyzer, Beckman Coulter). Inoculate cells with vitality above 85% into a 384 well TC treated plate (Corning catalog number 3765) with a white transparent bottom. Inoculate cells at a density of 1000 cells per well into 45 u L of standard growth medium. Incubate the plate overnight in a tissue culture incubator at 5% CO2 and 37 °C. On the second day, prepare free atorvastatin payload and targeted ADC at a 10 fold ratio in standard growth medium. Add the prepared treatment substance to the cells to obtain a final concentration of 0.005-100nM and a final volume of 50 u L/well. Each drug concentration is tested in quadruplicate. Incubate the plates in a tissue culture incubator at 5% CO2 and 37 °C for 5 days, and then evaluate cell viability by adding 25 u L of CellTiterGlo (Promega, catalog number G7573) (a reagent for cell lysis and measurement of total adenosine triphosphate (ATP) content). Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal, and then read using a luminescence reader (EnVision multi label enzyme-linked immunosorbent assay, PerkinElmer). To evaluate the effectiveness of drug treatment, luminescence counts from wells containing untreated cells (100% viability) were used to normalize the treated samples. Apply a variable slope model to fit the nonlinear regression curve to the data in GraphPad PRISM version 7.02 software. Extrapolating IC50 from the obtained curve    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.05973 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cell viability analysis of MDA-MB-453 (HER2+++) cell line, FaDu (HER2+) cell line and MDA-MB-468 (HER2-) cell line in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	51.02 nM	Low HER2 expression (HER2+)
Method Description	Cell viability analysis of MDA-MB-453 (HER2+++) cell line, FaDu (HER2+) cell line and MDA-MB-468 (HER2-) cell line in vitro.
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	174.8 nM	Negative HER2 expression (HER2-)
Method Description	Cell viability analysis of MDA-MB-453 (HER2+++) cell line, FaDu (HER2+) cell line and MDA-MB-468 (HER2-) cell line in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.49 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	6.36 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.2 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.15 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.071 nM	Low HER2 expression (HER2+)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-453 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.091 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the nci-n87 cell.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.076 nM	High HER2 expression (HER2 +++)
Method Description	Cultivate the cell line in a tissue culture incubator at 5% CO2 and 37 °C in the optimal growth medium. Separate cells at least 2 days prior to inoculation for proliferation assays to ensure optimal growth density. On the day of vaccination, cell viability and cell density were determined using a cell counter (Vi Cell XR Cell viability analyzer, Beckman Coulter). Inoculate cells with vitality above 85% into a 384 well TC treated plate (Corning catalog number 3765) with a white transparent bottom. Inoculate cells at a density of 1000 cells per well into 45 u L of standard growth medium. Incubate the plate overnight in a tissue culture incubator at 5% CO2 and 37 °C. On the second day, prepare free atorvastatin payload and targeted ADC at a 10 fold ratio in standard growth medium. Add the prepared treatment substance to the cells to obtain a final concentration of 0.005-100nM and a final volume of 50 u L/well. Each drug concentration is tested in quadruplicate. Incubate the plates in a tissue culture incubator at 5% CO2 and 37 °C for 5 days, and then evaluate cell viability by adding 25 u L of CellTiterGlo (Promega, catalog number G7573) (a reagent for cell lysis and measurement of total adenosine triphosphate (ATP) content). Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal, and then read using a luminescence reader (EnVision multi label enzyme-linked immunosorbent assay, PerkinElmer). To evaluate the effectiveness of drug treatment, luminescence counts from wells containing untreated cells (100% viability) were used to normalize the treated samples. Apply a variable slope model to fit the nonlinear regression curve to the data in GraphPad PRISM version 7.02 software. Extrapolating IC50 from the obtained curve    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.091 nM	Low HER2 expression (HER2+)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-453 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.331 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the nci-n87 cell.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[236]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	According to Vichai et al., (31) experiments were performed in 96-well plates (flat bottom, transparent plate, with lid; Corning-Falcon cat. n° 353072) using a CLARIOstar Plus plate-reader device (BMG LABTECH). Cells were seeded in a 96-well plate at a density of 2 × 103 cells in 100 uL per well, keeping a column of the plate without cells (background control), and allowed to recover for 24 h. Cells were treated live with 100 uL of various concentrations (final concentrations ranging from 0.003 to 100 nM) of trastuzumab conjugates (diluted in supplemented RPMI for HCC1954 and MDA-MB-231 cell lines and in DMEM for MCF7 cell line) or not (negative control = untreated cells; only supplemented with 100 uL of RPMI for HCC1954 and MDA-MB-231 cell lines or with 100 uL of DMEM for MCF7 cell line) in technical triplicates. Cells were incubated for 96 h at 37 °C and 5% CO2 under a humid atmosphere in an IncuCyteS3 (from Sartorius). Cells were fixed with an addition of 100 uL of cold 10% (w/v) trichloroacetic acid (TCA) to wells for 1 h at 4 °C, washed with tap water (×3), allowed to dry overnight at 25 °C, stained with 0.057% (w/v) SRB (in 1% (v/v) acetic acid) for 30 min at 25 °C, then quickly washed with 1% (v/v) acetic acid (×3) and allowed to dry overnight at 25 °C. After incubating the plate with 100 uL of cold 10 mM unbuffered Trizma base solution for 5 min at 25 °C under agitation, the Abs 530 nm was recorded. Final data were analyzed with Excel (Microsoft Corp.) and GraphPad Prism version 10.1.2 for Windows (GraphPad Software, Boston, Massachusetts USA). Mean Abs values and Normalized % cell viability (see below) were calculated. IC50 was calculated in performing a sigmoidal fit ([inhibitor] vs response-variable slope, GraphPad Prism v10.0.0). A minimum of three independent experiments (n = 3) was used. Normalized % cell viability [x] = [ (Mean Abs 530 nm conjugates [x] - Mean Abs 530 nm background control)/ (Mean Abs 530 nm negative control - Mean Abs 530 nm background control)] × 100; with [x] corresponding to the final conjugate's concentration.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[236]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	According to Vichai et al., (31) experiments were performed in 96-well plates (flat bottom, transparent plate, with lid; Corning-Falcon cat. n° 353072) using a CLARIOstar Plus plate-reader device (BMG LABTECH). Cells were seeded in a 96-well plate at a density of 2 × 103 cells in 100 uL per well, keeping a column of the plate without cells (background control), and allowed to recover for 24 h. Cells were treated live with 100 uL of various concentrations (final concentrations ranging from 0.003 to 100 nM) of trastuzumab conjugates (diluted in supplemented RPMI for HCC1954 and MDA-MB-231 cell lines and in DMEM for MCF7 cell line) or not (negative control = untreated cells; only supplemented with 100 uL of RPMI for HCC1954 and MDA-MB-231 cell lines or with 100 uL of DMEM for MCF7 cell line) in technical triplicates. Cells were incubated for 96 h at 37 °C and 5% CO2 under a humid atmosphere in an IncuCyteS3 (from Sartorius). Cells were fixed with an addition of 100 uL of cold 10% (w/v) trichloroacetic acid (TCA) to wells for 1 h at 4 °C, washed with tap water (×3), allowed to dry overnight at 25 °C, stained with 0.057% (w/v) SRB (in 1% (v/v) acetic acid) for 30 min at 25 °C, then quickly washed with 1% (v/v) acetic acid (×3) and allowed to dry overnight at 25 °C. After incubating the plate with 100 uL of cold 10 mM unbuffered Trizma base solution for 5 min at 25 °C under agitation, the Abs 530 nm was recorded. Final data were analyzed with Excel (Microsoft Corp.) and GraphPad Prism version 10.1.2 for Windows (GraphPad Software, Boston, Massachusetts USA). Mean Abs values and Normalized % cell viability (see below) were calculated. IC50 was calculated in performing a sigmoidal fit ([inhibitor] vs response-variable slope, GraphPad Prism v10.0.0). A minimum of three independent experiments (n = 3) was used. Normalized % cell viability [x] = [ (Mean Abs 530 nm conjugates [x] - Mean Abs 530 nm background control)/ (Mean Abs 530 nm negative control - Mean Abs 530 nm background control)] × 100; with [x] corresponding to the final conjugate's concentration.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[236]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	According to Vichai et al., (31) experiments were performed in 96-well plates (flat bottom, transparent plate, with lid; Corning-Falcon cat. n° 353072) using a CLARIOstar Plus plate-reader device (BMG LABTECH). Cells were seeded in a 96-well plate at a density of 2 × 103 cells in 100 uL per well, keeping a column of the plate without cells (background control), and allowed to recover for 24 h. Cells were treated live with 100 uL of various concentrations (final concentrations ranging from 0.003 to 100 nM) of trastuzumab conjugates (diluted in supplemented RPMI for HCC1954 and MDA-MB-231 cell lines and in DMEM for MCF7 cell line) or not (negative control = untreated cells; only supplemented with 100 uL of RPMI for HCC1954 and MDA-MB-231 cell lines or with 100 uL of DMEM for MCF7 cell line) in technical triplicates. Cells were incubated for 96 h at 37 °C and 5% CO2 under a humid atmosphere in an IncuCyteS3 (from Sartorius). Cells were fixed with an addition of 100 uL of cold 10% (w/v) trichloroacetic acid (TCA) to wells for 1 h at 4 °C, washed with tap water (×3), allowed to dry overnight at 25 °C, stained with 0.057% (w/v) SRB (in 1% (v/v) acetic acid) for 30 min at 25 °C, then quickly washed with 1% (v/v) acetic acid (×3) and allowed to dry overnight at 25 °C. After incubating the plate with 100 uL of cold 10 mM unbuffered Trizma base solution for 5 min at 25 °C under agitation, the Abs 530 nm was recorded. Final data were analyzed with Excel (Microsoft Corp.) and GraphPad Prism version 10.1.2 for Windows (GraphPad Software, Boston, Massachusetts USA). Mean Abs values and Normalized % cell viability (see below) were calculated. IC50 was calculated in performing a sigmoidal fit ([inhibitor] vs response-variable slope, GraphPad Prism v10.0.0). A minimum of three independent experiments (n = 3) was used. Normalized % cell viability [x] = [ (Mean Abs 530 nm conjugates [x] - Mean Abs 530 nm background control)/ (Mean Abs 530 nm negative control - Mean Abs 530 nm background control)] × 100; with [x] corresponding to the final conjugate's concentration.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.108 nM	High HER2 expression (HER2 +++)
Method Description	Trastuzumab-C-7 was tested in HCC1954,80ul,18&#4524h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.293 nM	High HER2 expression (HER2 +++)
Method Description	Trastuzumab-C-7 was tested in NCI-N87,80ul,18&#4524h
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	83.769 nM	High HER2 expression (HER2 +++)
Method Description	Trastuzumab-C-7 was tested in NCI-H358,80ul,18&#4524h
In Vitro Model	Minimally invasive lung adenocarcinoma	NCI-H358 cells		CVCL_1559
Experiment 4 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal Effective Concentration (EC50)	11.25 nM	High HER2 expression (HER2 +++)
Method Description	Trastuzumab-C-7 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 5 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Emax (TNF-a)	1791.26 pg/mL	High HER2 expression (HER2 +++)
Method Description	Trastuzumab-C-7 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.112 nM	High HER2 expression (HER2 +++)
Method Description	Trastuzumab-C-8 was tested in HCC1954,80ul,18&#4524h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.25 nM	High HER2 expression (HER2 +++)
Method Description	Trastuzumab-C-8 was tested in NCI-N87,80ul,18&#4524h
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	374.766 nM	High HER2 expression (HER2 +++)
Method Description	Trastuzumab-C-8 was tested in NCI-H358,80ul,18&#4524h
In Vitro Model	Minimally invasive lung adenocarcinoma	NCI-H358 cells		CVCL_1559
Experiment 4 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Half Maximal Effective Concentration (EC50)	17.72 nM	High HER2 expression (HER3 +++)
Method Description	Trastuzumab-C-8 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 5 Reporting the Activity Date of This ADC					[231]
Efficacy Data	Emax (TNF-a)	1836.92 pg/mL	High HER2 expression (HER4 +++)
Method Description	Trastuzumab-C-8 was tested in HCC1954 and PBMC,50ul,24h
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.117 nM	High HER2 expression (HER2 +++)
Method Description	Cultivate the cell line in a tissue culture incubator at 5% CO2 and 37 °C in the optimal growth medium. Separate cells at least 2 days prior to inoculation for proliferation assays to ensure optimal growth density. On the day of vaccination, cell viability and cell density were determined using a cell counter (Vi Cell XR Cell viability analyzer, Beckman Coulter). Inoculate cells with vitality above 85% into a 384 well TC treated plate (Corning catalog number 3765) with a white transparent bottom. Inoculate cells at a density of 1000 cells per well into 45 u L of standard growth medium. Incubate the plate overnight in a tissue culture incubator at 5% CO2 and 37 °C. On the second day, prepare free atorvastatin payload and targeted ADC at a 10 fold ratio in standard growth medium. Add the prepared treatment substance to the cells to obtain a final concentration of 0.005-100nM and a final volume of 50 u L/well. Each drug concentration is tested in quadruplicate. Incubate the plates in a tissue culture incubator at 5% CO2 and 37 °C for 5 days, and then evaluate cell viability by adding 25 u L of CellTiterGlo (Promega, catalog number G7573) (a reagent for cell lysis and measurement of total adenosine triphosphate (ATP) content). Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal, and then read using a luminescence reader (EnVision multi label enzyme-linked immunosorbent assay, PerkinElmer). To evaluate the effectiveness of drug treatment, luminescence counts from wells containing untreated cells (100% viability) were used to normalize the treated samples. Apply a variable slope model to fit the nonlinear regression curve to the data in GraphPad PRISM version 7.02 software. Extrapolating IC50 from the obtained curve    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[225]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.117 nM	Positive HER2 expression (HER2+++/++)
Method Description	Chemiluminescence staining (Luminescent Cell Viability Assay) was carried out, and IC5owas calculated after reading the fluorescence data.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1192 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cell viability analysis of MDA-MB-453 (HER2+++) cell line, FaDu (HER2+) cell line and MDA-MB-468 (HER2-) cell line in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	34.5 nM	Low HER2 expression (HER2+)
Method Description	Cell viability analysis of MDA-MB-453 (HER2+++) cell line, FaDu (HER2+) cell line and MDA-MB-468 (HER2-) cell line in vitro.
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 3 Reporting the Activity Date of This ADC					[235]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	128.8 nM	Negative HER2 expression (HER2-)
Method Description	Cell viability analysis of MDA-MB-453 (HER2+++) cell line, FaDu (HER2+) cell line and MDA-MB-468 (HER2-) cell line in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.16 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.16 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1996 nM	High HER2 expression (HER2 +++)
Method Description	On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.    Click to Show/Hide
In Vitro Model	Breast carcinoma	ZR-75-30 cells		CVCL_1661
Experiment 2 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.6574 nM	High HER2 expression (HER2 +++)
Method Description	On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma of no special type	UACC812 cells		CVCL_1781
Experiment 3 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.888 nM	High HER2 expression (HER2 +++)
Method Description	On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[237]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.2 nM	High HER2 expression (HER2 +++)
Method Description	The MTT (3- (4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assays were performed using WT ADC and positively charged ADC in three cell lines with varying HER2 expression levels: N87 (high), MCF-7 (low), and MDA-MB-468 (non-expressing). Cells were seeded at a density of 10,000 cells per well in 96-well plates and incubated for 24 h before treatment. ADCs were added at concentrations ranging from 0.01 nM to 1000 nM, and cells were incubated for an additional 96 h. Following treatment, 5 mg/mL MTT solution was added to each well and incubated for 4 h, after which 10% SDS-HCl solution was added to dissolve the formazan crystals. Absorbance was measured at 570 nm the next day. Cell viability (%) was calculated as (ODtreated/ (ODcontrol) × 100%. GraphPad Prism (version 10.4.1) was used for curve fitting of the sigmoidal dose-response curves (cell viability vs. ADC concentration) under the nonlinear regression option, and the half-maximal inhibitory concentration (IC50) values were determined.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[237]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	296 nM	Negative HER2 expression (HER2-)
Method Description	The MTT (3- (4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assays were performed using WT ADC and positively charged ADC in three cell lines with varying HER2 expression levels: N87 (high), MCF-7 (low), and MDA-MB-468 (non-expressing). Cells were seeded at a density of 10,000 cells per well in 96-well plates and incubated for 24 h before treatment. ADCs were added at concentrations ranging from 0.01 nM to 1000 nM, and cells were incubated for an additional 96 h. Following treatment, 5 mg/mL MTT solution was added to each well and incubated for 4 h, after which 10% SDS-HCl solution was added to dissolve the formazan crystals. Absorbance was measured at 570 nm the next day. Cell viability (%) was calculated as (ODtreated/ (ODcontrol) × 100%. GraphPad Prism (version 10.4.1) was used for curve fitting of the sigmoidal dose-response curves (cell viability vs. ADC concentration) under the nonlinear regression option, and the half-maximal inhibitory concentration (IC50) values were determined.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[237]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1603 nM	Low HER2 expression (HER2+)
Method Description	The MTT (3- (4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assays were performed using WT ADC and positively charged ADC in three cell lines with varying HER2 expression levels: N87 (high), MCF-7 (low), and MDA-MB-468 (non-expressing). Cells were seeded at a density of 10,000 cells per well in 96-well plates and incubated for 24 h before treatment. ADCs were added at concentrations ranging from 0.01 nM to 1000 nM, and cells were incubated for an additional 96 h. Following treatment, 5 mg/mL MTT solution was added to each well and incubated for 4 h, after which 10% SDS-HCl solution was added to dissolve the formazan crystals. Absorbance was measured at 570 nm the next day. Cell viability (%) was calculated as (ODtreated/ (ODcontrol) × 100%. GraphPad Prism (version 10.4.1) was used for curve fitting of the sigmoidal dose-response curves (cell viability vs. ADC concentration) under the nonlinear regression option, and the half-maximal inhibitory concentration (IC50) values were determined.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.21 nM
Method Description	The SK-BR-3 cells (ATCC), which are negative for CD30 antigen but positive for HER2 antigen, were cultured to reach 2×106 cells/mL. 50 uL of each was added to 96-well cell culture microplates. 50 uL of CellTiter-Glo Luminescent Cell Viability Assay (Promega) was added to each well and mixed. The mixture was incubated in the dark for 20 minutes. The luminescence was measured using a microplate illuminometer, and the cell survival rates at each ADC concentration were calculated accordingly.The IC50 value can be calculated based on the value of cell survival rate.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[238]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3.77 nM
Method Description	The Karpas-299 cells (ECACC), which express CD30 antigen and are negative for HER2 antigen, were cultured to reach 2×106 cells/mL. 50 uL of each was added to 96-well cell culture microplates. 50 uL of CellTiter-Glo Luminescent Cell Viability Assay (Promega) was added to each well and mixed. The mixture was incubated in the dark for 20 minutes. The luminescence was measured using a microplate illuminometer, and the cell survival rates at each ADC concentration were calculated accordingly.The IC50 value can be calculated based on the value of cell survival rate.    Click to Show/Hide
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.22 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.23 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.239 nM	High HER2 expression (HER2 +++)
Method Description	On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.    Click to Show/Hide
In Vitro Model	Breast carcinoma	ZR-75-30 cells		CVCL_1661
Experiment 2 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.892 nM	High HER2 expression (HER2 +++)
Method Description	On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma of no special type	UACC812 cells		CVCL_1781
Experiment 3 Reporting the Activity Date of This ADC					[232]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.991 nM	High HER2 expression (HER2 +++)
Method Description	On the day of administration, HER2 targeted ADC and HER2 were prepared at a 10 fold ratio in standard growth medium. Add the prepared targeted ADC treatment to cells to obtain a final concentration of 3.81e-5nM to 100nM and a final volume of 50uL/well. Each drug concentration is tested in quadruplicate. On the same day, the cell viability of untreated cells at the time of administration was evaluated by adding 25 u L of CellTiter (ProMag catalog number G7573), a reagent for lysing cells and measuring total adenosine triphosphate (ATP) content. Incubate the plate at room temperature for 10 minutes to stabilize the luminescence signal before reading. Use luminous readingThe PHERAstar FSX ELISA reader (BMG Labtech) was used to measure the luminescence signals of all plates. This signal represents the cell viability of untreated cells on the day of administration or day 0.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.25 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	10.1 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.26 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	300 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.26 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.35 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.73 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	≈ 0.3 nM	Positive ErbB2/HER2 expression (ErbB2/HER2+++/++)
Method Description	Cytotoxicity of ADC-2 to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[239]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	≈ 8 nM	Positive ErbB2/HER2 expression (ErbB2/HER2+++/++)
Method Description	Cytotoxicity of ADC-2 to NCI-N87 cells
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.4 nM	Positive HER2 expression (HER2+++/++)
Method Description	Calu3 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Lung adenocarcinoma	Calu3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.5 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.55 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[240]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.49 nM	Positive HER2 expression (HER2+++/++)
Method Description	Next, the dose dependent cytotoxicity of ADC1 was investigated in HER2-positive (BT474 and SK-BR3) and HER2-negative (MCF-7) breast cancer cell lines. The potency of ADC1 was compared to the FDA approved ADC Kadcyla®. ADC1 proved to be highly potent in both BT474 and SK-BR3 cell lines while having negligible toxicity in MCF-7 cells, indicating neglectable extracellular linker cleavage (Fig. 4). We also observed that ADC 1 had a higher potency against BT-474 cells (IC50 = 0.49 nM) compared to Kadcyla (IC50 =1.06 nM) suggesting efficient intracellular linker cleavage and payload release.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.51 nM	High HER2 expression (HER2 +++)
Method Description	A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 30 nM	Negative HER2 expression (HER2-)
Method Description	A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[241]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.6 nM	High HER2 expression (HER2 +++)
Method Description	HCC-1954, JIMT-1 and MDA-MB-468 cells were plated in 24-well culture plates (5000, 5000 and 10,000 cells/well, respectively) and incubated for 24 h. Cells were then exposed to serial dilutions of trastuzumab, free exatecan, or Tras-Exa (DAR4) ADC. Cell viability was evaluated following 6 days of incubation using MTT (3 ug/mL, Sigma). MTT absorbance was measured at 570 nm using SpectraMax M5e multi-detection reader.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC-1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[241]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	40 nM	Positive HER2 expression (HER2+++/++)
Method Description	HCC-1954, JIMT-1 and MDA-MB-468 cells were plated in 24-well culture plates (5000, 5000 and 10,000 cells/well, respectively) and incubated for 24 h. Cells were then exposed to serial dilutions of trastuzumab, free exatecan, or Tras-Exa (DAR4) ADC. Cell viability was evaluated following 6 days of incubation using MTT (3 ug/mL, Sigma). MTT absorbance was measured at 570 nm using SpectraMax M5e multi-detection reader.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[241]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	50 nM	Low HER2 expression (HER2+)
Method Description	HCC-1954, JIMT-1 and MDA-MB-468 cells were plated in 24-well culture plates (5000, 5000 and 10,000 cells/well, respectively) and incubated for 24 h. Cells were then exposed to serial dilutions of trastuzumab, free exatecan, or Tras-Exa (DAR4) ADC. Cell viability was evaluated following 6 days of incubation using MTT (3 ug/mL, Sigma). MTT absorbance was measured at 570 nm using SpectraMax M5e multi-detection reader.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.61 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.64 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.72 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.78 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[242]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1 nM	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.28 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.3&#1770.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tumor cell lines were maintained in RPMI1640 medium supplemented with 10% heat-inactivated fetal bovine serum, 2 mM L-glutamine and 1 mM sodium pyruvate. 1800 cells per well were seeded in a volume of 180 uL in a 96-well flat bottom polystyrene plate. The cells were allowed to adhere overnight at 37 °C in a CO2 incubator. Ligands were initially formulated in dimethyl sulphoxide, and stocks stored at -80 °C. They were then further formulated at 10× concentration in RPMI1640 medium. 20 uL of diluted samples were added into each treatment well. On each plate, blank wells with no cells, and untreated wells containing cells, were included. Plates were then cultured at 37 °C in a CO2 incubator for 96 h. Cytotoxicity was evaluated in triplicate using a tetrazolium salt-based assay, the MTT assay. After 96 h, the supernatant was removed from each well and 200 uL of a sterile filtered 500 ug mL-1 MTT solution in water added to each well. The plates were then incubated at 37 °C in a CO2 incubator for 4 h. The supernatant was then removed and the formazan crystals formed solubilized by adding 150 uL of dimethyl sulphoxide to each well. The plate was then read on a plate reader at 540 nm, and percentage cell survival calculated as follows: ((mean absorbance treated wells at concentration x - mean absorbance blank wells) ÷ (mean absorbance untreated wells at concentration x - mean absorbance blank wells)) × 100. Data were plotted as concentration in nM vs. % cell survival, and IC50 values for inhibition of cell growth were determined with the GraphPad Prism software using non-linear regression.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC					[243]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	29.7&#1771.55 nM	Negative HER2 expression (HER2-)
Method Description	Tumor cell lines were maintained in RPMI1640 medium supplemented with 10% heat-inactivated fetal bovine serum, 2 mM L-glutamine and 1 mM sodium pyruvate. 1800 cells per well were seeded in a volume of 180 uL in a 96-well flat bottom polystyrene plate. The cells were allowed to adhere overnight at 37 °C in a CO2 incubator. Ligands were initially formulated in dimethyl sulphoxide, and stocks stored at -80 °C. They were then further formulated at 10× concentration in RPMI1640 medium. 20 uL of diluted samples were added into each treatment well. On each plate, blank wells with no cells, and untreated wells containing cells, were included. Plates were then cultured at 37 °C in a CO2 incubator for 96 h. Cytotoxicity was evaluated in triplicate using a tetrazolium salt-based assay, the MTT assay. After 96 h, the supernatant was removed from each well and 200 uL of a sterile filtered 500 ug mL-1 MTT solution in water added to each well. The plates were then incubated at 37 °C in a CO2 incubator for 4 h. The supernatant was then removed and the formazan crystals formed solubilized by adding 150 uL of dimethyl sulphoxide to each well. The plate was then read on a plate reader at 540 nm, and percentage cell survival calculated as follows: ((mean absorbance treated wells at concentration x - mean absorbance blank wells) ÷ (mean absorbance untreated wells at concentration x - mean absorbance blank wells)) × 100. Data were plotted as concentration in nM vs. % cell survival, and IC50 values for inhibition of cell growth were determined with the GraphPad Prism software using non-linear regression.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.35 nM	High HER2 expression (HER2 +++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10 nM	Moderate HER2 expression (HER2++)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[227]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10 nM	Negative HER2 expression (HER2-)
Method Description	The ability of bis-intercalating peptide free drugs and ADCs to inhibit proliferation of tumor cells in vitro was evaluated using the following cell lines: OVCAR-3 (ovarian, ATCC), SKOV-3 (ovarian, ATCC), IGROV-1 (ovarian, national research council of Canada (NRC)), OV-90 (ovarian, ATCC), OVKATE (Ovarian, Japanese Collection of Research Bioresources (JCRB) (JCRB1044)), JIMT-1 (breast, NRC), SK-BR-3 (breast, ATCC), T-47D (breast, ATCC), ZR-75-1 (breast, ATCC), MDA-MB-468 (breast, AddexBio), BT-20 (breast, ATCC), BT-474 (breast, NRC), MDA-MB-175 (breast, AddexBio), A549 (lung, collaborator), NCI-H226 (lung, NRC), NCI-H661 (lung, NRC), NCI-H1573 (lung, ATCC). NCI-H1563 (lung, ATCC), H358 (lung, collaborator), EBC-1 (lung, Xenotech), H1299 (lung, NRC), NCI-H292 (lung, ATCC), HCC817 (lung, ATCC), NCI-H441 (lung, ATCC), MIA-PaCa-2 (pancreatic, ATCC), BxPC-3 (pancreatic, ATCC), Panc-1 (pancreatic, ATCC), AsPC-1 (pancreatic, ATCC), JEG-3 (placenta, AddexBio), HT-29 (colon, ATCC). Cells cultured (per vendor instructions) in log-phase growth were detached by brief incubation in 0.05% trypsin and resuspended in respective culturing media at 20,000 cells/mL (except for ZR-75 cells, which were resuspended at 10,000 cells/mL). 50 uL/well (~1000 cells/well) were transferred to sterile tissue culture (TC)-treated 384-well plates (ThermoFisher Scientific, Catalogue # 164610) and incubated overnight at 37 °C with 5% CO2 to allow the cells to adhere to the plate surface. The next day, in a sterile, V-bottom, 96-well plate, test articles were titrated 1:3 in complete growth medium, creating a 10-point dose response titration with compounds at 3.5-times the desired final concentration. A total of 20 uL from each dilution was added to the 384-well plate containing the seeded cells, and these plates were incubated at 37 °C with 5% CO2 for 5 nights. Cell viability was quantified by first incubating with 15 uL/well of CellTiter-Glo (Promega, Catalogue # G7572) for 30 min and then measuring luminescence with a microplate luminometer (BioTek Synergy H1 Microplate Reader). IC50 values were determined by GraphPad Prism (GraphPad Software, Sand Diego, CA).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.21 nM	Positive her2 expression (her2+++/++)
Method Description	NCI N87 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 1000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[242]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.3 nM	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.45 nM	Positive her2 expression (her2+++/++)
Method Description	NCI N87 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 1000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.9 nM	High HER2 expression (HER2 +++)
Method Description	A total of 30,000 SK-BR-3 (HER2-high) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[228]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 30 nM	Negative HER2 expression (HER2-)
Method Description	A total of 10,000 MDA-MB-468 (HER2-negative) cells were seeded either as monocultures or cocultures in TC-treated 48-well microtiter plates (Greiner Bio-One, catalog no. 667180) and treated with 1.0 or 0.1 nmol/L ADCs diluted in growth medium.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[234]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[219]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3.23 nM	Positive her2 expression (her2+++/++)
Method Description	NCI N87 5000cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added, the maximum concentration of the drug is 1000 nM with a 4-fold dilution across 10 points, for the various ADCs. Cell proliferation was measured after 4 days exposure, 50ul Cell titer glo to test IC50.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[244]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3.77 nM	Positive CD30 expression (CD30+++/++)
Method Description	Karpas-299 cells (ECACC), which are CD30 antigen-positiveand HER2 antigen-negative,were cultured in RPMI 1640 (GIBCO)containing 10%fetal bovine serum (MP Biomedicals) (hereinafter,referred to as "culture medium A" in this test).
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	16.9 nM	Moderate CD276 expression (CD276 ++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-468 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	18.8 nM	Moderate CD276 expression (CD276 ++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-231 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	40.8 nM	High CD276expression (CD276 +++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the 4T1 cell.
In Vitro Model	Mammary carcinoma	4T1 cells		CVCL_0125

Experiment 1 Reporting the Activity Date of This ADC					[246]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	19.33 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	MDA-MB-468, NCI-N87 and SK-BR-3 were seeded per well in a 96-well plate and grew for 24 h. Then cells were exposed to DXd, exatecan, homocamtothecins or Enhertu and further incubated for 72 h. The cell viability and proliferation behavior were assessed by the MTT assay. For each compound, inhibitory concentration values (IC50, EC50) were determined using the GraphPad Prism 6.0 Software for MDA-MB-468, NCI-N87 and SK-BR-3 cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[246]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	24.85 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	MDA-MB-468, NCI-N87 and SK-BR-3 were seeded per well in a 96-well plate and grew for 24 h. Then cells were exposed to DXd, exatecan, homocamtothecins or Enhertu and further incubated for 72 h. The cell viability and proliferation behavior were assessed by the MTT assay. For each compound, inhibitory concentration values (IC50, EC50) were determined using the GraphPad Prism 6.0 Software for MDA-MB-468, NCI-N87 and SK-BR-3 cells.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[242]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 25 nM	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	34 nM	Moderate HER2 expression (HER2++)
Method Description	JIMT1 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Breast ductal carcinoma	JIMT1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[230]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	300 nM	Low HER2 expression (HER2+)
Method Description	MCF-7 cells were plated at a density of 5000 cells per well and the next day were treated with antibody-PBD conjugate for 3 days.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	50.7 nM	Moderate CD276 expression (CD276 ++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-468 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	125.4 nM	High CD276expression (CD276 +++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the 4T1 cell.
In Vitro Model	Mammary carcinoma	4T1 cells		CVCL_0125
Experiment 3 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	175 nM	Moderate CD276 expression (CD276 ++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-231 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	73.56 nM
Method Description	The in vitro antitumor efficacy of BsADC was assessed using the SNU899 cell.
In Vitro Model	Laryngeal squamous cell carcinoma, Squamous cell carcinoma of the larynx	SNU899 cells		CVCL_5105
Experiment 2 Reporting the Activity Date of This ADC					[247]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	115.4 nM
Method Description	The in vitro antitumor efficacy of BsADC was assessed using the SNU46 cell.
In Vitro Model	Laryngeal squamous cell carcinoma, Squamous cell carcinoma of the larynx	SNU46 cells		CVCL_5063

Experiment 1 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01 nmol/L	High her2 expression (her2 +++)
Method Description	SKBR3 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04 nmol/L	High her2 expression (her2 +++)
Method Description	N87 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1 nmol/L	High her2 expression (her2 +++)
Method Description	BT474 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.15 nmol/L	Low her2 expression (her2+)
Method Description	MCF7 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	13.53 nmol/L	Moderate her2 expression (her2++)
Method Description	JIMT1 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nmol/L	High her2 expression (her2 +++)
Method Description	SKBR3 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.14 nmol/L	Low her2 expression (her2+)
Method Description	MCF7 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.18 nmol/L	High her2 expression (her2 +++)
Method Description	BT474 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.2 nmol/L	High her2 expression (her2 +++)
Method Description	N87 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15.82 nmol/L	Moderate her2 expression (her2++)
Method Description	JIMT1 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nmol/L	High her2 expression (her2 +++)
Method Description	SKBR3 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07 nmol/L	High her2 expression (her2 +++)
Method Description	N87 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1 nmol/L	High her2 expression (her2 +++)
Method Description	BT474 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.14 nmol/L	Low her2 expression (her2+)
Method Description	MCF7 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	14.56 nmol/L	Moderate her2 expression (her2++)
Method Description	JIMT1 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nmol/L	High her2 expression (her2 +++)
Method Description	SKBR3 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.09 nmol/L	High her2 expression (her2 +++)
Method Description	BT474 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1 nmol/L	High her2 expression (her2 +++)
Method Description	N87 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.14 nmol/L	Low her2 expression (her2+)
Method Description	MCF7 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	17.69 nmol/L	Moderate her2 expression (her2++)
Method Description	JIMT1 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nmol/L	High her2 expression (her2 +++)
Method Description	SKBR3 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.09 nmol/L	High her2 expression (her2 +++)
Method Description	N87 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.13 nmol/L	High her2 expression (her2 +++)
Method Description	BT474 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.17 nmol/L	Low her2 expression (her2+)
Method Description	MCF7 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	18.47 nmol/L	Moderate her2 expression (her2++)
Method Description	JIMT1 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.03 nmol/L	High her2 expression (her2 +++)
Method Description	SKBR3 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.11 nmol/L	High her2 expression (her2 +++)
Method Description	BT474 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.11 nmol/L	High her2 expression (her2 +++)
Method Description	N87 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.13 nmol/L	Low her2 expression (her2+)
Method Description	MCF7 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	100 nmol/L	Moderate her2 expression (her2++)
Method Description	JIMT1 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	9.962 nmol/L	High her2 expression (her2 +++)
Method Description	SKBR3 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	11.73 nmol/L	High her2 expression (her2 +++)
Method Description	BT474 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	17.97 nmol/L	Moderate her2 expression (her2++)
Method Description	JIMT1 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	20.99 nmol/L	Low her2 expression (her2+)
Method Description	MCF7 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	29.39 nmol/L	High her2 expression (her2 +++)
Method Description	N87 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	11.06 nmol/L	High her2 expression (her2 +++)
Method Description	SKBR3 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	21.91 nmol/L	Low her2 expression (her2+)
Method Description	MCF7 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	22.07 nmol/L	High her2 expression (her2 +++)
Method Description	N87 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	27.7 nmol/L	Moderate her2 expression (her2++)
Method Description	JIMT1 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	29.14 nmol/L	High her2 expression (her2 +++)
Method Description	BT474 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 100 nmol/L	High her2 expression (her2 +++)
Method Description	BT474 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 100 nmol/L	High her2 expression (her2 +++)
Method Description	SKBR3 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 100 nmol/L	High her2 expression (her2 +++)
Method Description	N87 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 100 nmol/L	Moderate her2 expression (her2++)
Method Description	JIMT1 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 100 nmol/L	Low her2 expression (her2+)
Method Description	MCF7 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 100 nmol/L	High her2 expression (her2 +++)
Method Description	BT474 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 100 nmol/L	High her2 expression (her2 +++)
Method Description	SKBR3 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 100 nmol/L	High her2 expression (her2 +++)
Method Description	N87 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 100 nmol/L	Moderate her2 expression (her2++)
Method Description	JIMT1 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 100 nmol/L	Low her2 expression (her2+)
Method Description	MCF7 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 300 nmol/L	High her2 expression (her2 +++)
Method Description	BT474 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 300 nmol/L	High her2 expression (her2 +++)
Method Description	SKBR3 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 300 nmol/L	High her2 expression (her2 +++)
Method Description	N87 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 300 nmol/L	Moderate her2 expression (her2++)
Method Description	JIMT1 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 300 nmol/L	Low her2 expression (her2+)
Method Description	MCF7 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 300 nmol/L	High her2 expression (her2 +++)
Method Description	BT474 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 300 nmol/L	High her2 expression (her2 +++)
Method Description	SKBR3 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 300 nmol/L	High her2 expression (her2 +++)
Method Description	N87 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 300 nmol/L	Moderate her2 expression (her2++)
Method Description	JIMT1 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[248]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 300 nmol/L	Low her2 expression (her2+)
Method Description	MCF7 cell line was plated at 5,000cell/well in black walled 96-well plate and allowed to adhere overnight. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measured after 10 min using a SpectraMax M5 plate reader (Molecular Devices). Dose response curves were generated using SoftMax Pro software. IC50 values were determined from four-parameter curve fitting    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.18 uM
Method Description	ZR-75-30 Cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.    Click to Show/Hide
In Vitro Model	Breast carcinoma	ZR-75-30 cells		CVCL_1661
Experiment 2 Reporting the Activity Date of This ADC					[212]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.712 uM	Positive her2 expression (her2+++/++)
Method Description	BT-474 cells were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added at serial dilutions of each test compound spanning a concentration range of either 50 nM to 0.005 nM for the various ADCs. Cell proliferation was measured after 144 hours exposure, by CellTiter-Glo 2.0 Solution Cell Viability Assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	6.9 uM	Moderate CD276 expression (CD276 ++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-468 cell.
In Vitro Model	Mammary carcinoma	4T1 cells		CVCL_0125
Experiment 2 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	7.7 uM	Moderate CD276 expression (CD276 ++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-231 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[245]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	13.1 uM	High CD276expression (CD276 +++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the 4T1 cell.
In Vitro Model	Mammary carcinoma	4T1 cells		CVCL_0125

Experiment 1 Reporting the Activity Date of This ADC					[250]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.594 ug/ml	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the effect of the masked ADC - S423 on cell viability after demasking with MMP2 protease, the cytotoxicity of the masked and demasked (MMP2 - treated) ADC - S423 and ADC - S426 was tested on HER2 - positive SK - BR - 3 cells, and compared with that of the naked (unmasked) trastuzumab - based ADC - TRA41C and the isotype - control ADC - RIT41C. After 6 days of treatment, cell viability was measured using the CellTiter - GloTM (CTG) luminescent assay kit.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[250]
Efficacy Data	Half Maximal Effective Concentration (EC50)	82.01 ug/ml	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the effect of the masked ADC - S423 on cell viability after demasking with MMP2 protease, the cytotoxicity of the masked and demasked (MMP2 - treated) ADC - S423 and ADC - S426 was tested on HER2 - positive SK - BR - 3 cells, and compared with that of the naked (unmasked) trastuzumab - based ADC - TRA41C and the isotype - control ADC - RIT41C. After 6 days of treatment, cell viability was measured using the CellTiter - GloTM (CTG) luminescent assay kit.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[250]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.728 ug/ml	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the effect of the masked ADC - S423 on cell viability after demasking with MMP2 protease, the cytotoxicity of the masked and demasked (MMP2 - treated) ADC - S423 and ADC - S426 was tested on HER2 - positive SK - BR - 3 cells, and compared with that of the naked (unmasked) trastuzumab - based ADC - TRA41C and the isotype - control ADC - RIT41C. After 6 days of treatment, cell viability was measured using the CellTiter - GloTM (CTG) luminescent assay kit.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[250]
Efficacy Data	Half Maximal Effective Concentration (EC50)	324 ug/ml	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the effect of the masked ADC - S423 on cell viability after demasking with MMP2 protease, the cytotoxicity of the masked and demasked (MMP2 - treated) ADC - S423 and ADC - S426 was tested on HER2 - positive SK - BR - 3 cells, and compared with that of the naked (unmasked) trastuzumab - based ADC - TRA41C and the isotype - control ADC - RIT41C. After 6 days of treatment, cell viability was measured using the CellTiter - GloTM (CTG) luminescent assay kit.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.00122 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.00784 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.01013 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0126 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.014 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	1.6137 nM	Negative HER2 expression (HER2-)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0131 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0131 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0823 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	1.211 nM	Negative HER2 expression (HER2-)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0147 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0182 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.1263 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	4.0737 nM	Negative HER2 expression (HER2-)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0147 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0153 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.1007 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	2.766 nM	Negative HER2 expression (HER2-)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0157 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0174 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.1027 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	2.2807 nM	Negative HER2 expression (HER2-)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0172 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0207 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.1341 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	7.6951 nM	Negative HER2 expression (HER2-)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0181 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0184 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.151 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	1.6273 nM	Negative HER2 expression (HER2-)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1 nM	Low B7H3 expression (B7H3+)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 6 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.9 nM	High B7H3 expression (B7H3 +++)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0221 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0221 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.1377 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	27.2295 nM	Negative HER2 expression (HER2-)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0484 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.051 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0512 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.1022 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.6 nM	Low B7H3 expression (B7H3+)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 4 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.5 nM	High B7H3 expression (B7H3 +++)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0571 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0641 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0751 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0771 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0825 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0865 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.4945 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	9.9322 nM	Negative HER2 expression (HER2-)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	100 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0915 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0937 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0953 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0954 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.104 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.107 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.1088 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.5115 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	14.9972 nM	Negative HER2 expression (HER2-)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	100 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.113 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.144 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.152 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.6929 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	20.4961 nM	Negative HER2 expression (HER2-)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	34.0772 nM	Positive HER2 expression (HER2 +++/++)
Method Description	After sample addition, culture for 6 days. Thaw the CellTiter-Glo® reagent and place the cell culture plate at room temperature to equilibrate for 30 minutes. Then add 50 to each well. Shake and lyse the cell plate in a shaker for 2 minutes, then incubate at room temperature for 10 minutes to stabilize the luminescence signal.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.187 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.193 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.212 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.234 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.234 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.375 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.389 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.403 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.441 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.481 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.513 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.517 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	2.91 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	3.11 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	4.42 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[251]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	7.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Breast inflammatory carcinoma	KPL4 cells		CVCL_5310

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.091 nM
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.331 nM
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[252]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.029 nM	High HER2 expression (HER2+++)
Method Description	IC50 (in nM) cell-based assays of tested entities on breast cancer cell lines MDA-MB-231 (HER2-low)
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells (HER2 low)		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[252]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Low HER2 expression (HER2+)
Method Description	IC50 (in nM) cell-based assays of tested entities on breast cancer cell lines MDA-MB-231 (HER2-low)
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells (HER2 low)		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.038 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 0.1 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.1 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to BT474-HDR cells under 0.1 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	21.32 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 toBT474-HDR cells under 20 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	42.79 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 20 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.063 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 0.1 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.19 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to BT474-HDR cells under 0.1 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	66.8 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 20 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	109.1 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 toBT474-HDR cells under 20 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.12 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 0.1 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.34 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to BT474-HDR cells under 0.1 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	6.15 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 toBT474-HDR cells under 20 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	26.65 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 20 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.14 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 0.1 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.39 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to BT474-HDR cells under 0.1 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	16.25 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 toBT474-HDR cells under 20 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[213]
Efficacy Data	Half Maximal Effective Concentration (EC50)	43.77 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 20 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.4 nM	Low B7H3 expression (B7H3+)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.3 nM	High B7H3 expression (B7H3 +++)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483

Experiment 1 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.5 nM	Low B7H3 expression (B7H3+)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.6 nM	High B7H3 expression (B7H3 +++)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483

Experiment 1 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.6 nM	Low B7H3 expression (B7H3+)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.7 nM	High B7H3 expression (B7H3 +++)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483

Experiment 1 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.7 nM	Low B7H3 expression (B7H3+)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.3 nM	High B7H3 expression (B7H3 +++)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483

Experiment 1 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.8 nM	Low B7H3 expression (B7H3+)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.8 nM	High B7H3 expression (B7H3 +++)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483

Experiment 1 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1 nM	Low B7H3 expression (B7H3+)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237
Experiment 2 Reporting the Activity Date of This ADC					[253]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2.1 nM	High B7H3 expression (B7H3 +++)
Method Description	Cells were seeded (NCI-1650 or MDA-MB-453 (2E3/well) or Capan-1 (4E3/well)) into 3D 96-well plates (Corning: 4520), 80 ul/well, and incubated at 37 °C, 5% CO2, overnight.
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483

Experiment 1 Reporting the Activity Date of This ADC					[210]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	NCI-N87 (HER2+++)
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14.8 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	17.2 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	62 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	68 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	71 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	78 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	97 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	133 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	233.7 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	459 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	464 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	788 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[254]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM
Method Description	Mycloid TNFa Secretion
In Vitro Model	Mycloid	Mycloid cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Effective Concentration (EC50)	12.5 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Effective Concentration (EC50)	97.6 ng/mL	Negative HER2 expression (HER2-)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC-78 cells		CVCL_2061

Experiment 1 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Effective Concentration (EC50)	15.5 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Effective Concentration (EC50)	144.1 ng/mL	Negative HER2 expression (HER2-)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC-78 cells		CVCL_2061

Experiment 1 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Effective Concentration (EC50)	18 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Effective Concentration (EC50)	121.2 ng/mL	Negative HER2 expression (HER2-)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC-78 cells		CVCL_2061

Experiment 1 Reporting the Activity Date of This ADC					[256]
Efficacy Data	Half Maximal Effective Concentration (EC50)	67.94&#17713.53 ng/mL	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	Cells were distributed into 96-well white round-bottom plates, with each well receiving 1000 cells in RPMI-1640 medium supplemented with 10% FBS. Following a 24-hour incubation period, diluted compounds were introduced to the wells. After 144 hours, a CellTiter-Glo luminescent cell viability assay (Promega, Madison, WI, USA) was performed to assess cell viability. The luminescent readings were normalized as percentages relative to untreated cells, and the IC50 values for each compound were determined.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Effective Concentration (EC50)	114.7 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 3000 ng/mL	Negative HER2 expression (HER2-)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC-78 cells		CVCL_2061

Experiment 1 Reporting the Activity Date of This ADC					[256]
Efficacy Data	Half Maximal Effective Concentration (EC50)	142.21&#17726.91 ng/mL	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	Cells were distributed into 96-well white round-bottom plates, with each well receiving 1000 cells in RPMI-1640 medium supplemented with 10% FBS. Following a 24-hour incubation period, diluted compounds were introduced to the wells. After 144 hours, a CellTiter-Glo luminescent cell viability assay (Promega, Madison, WI, USA) was performed to assess cell viability. The luminescent readings were normalized as percentages relative to untreated cells, and the IC50 values for each compound were determined.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[256]
Efficacy Data	Half Maximal Effective Concentration (EC50)	145.43&#17727.69 ng/mL	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	Cells were distributed into 96-well white round-bottom plates, with each well receiving 1000 cells in RPMI-1640 medium supplemented with 10% FBS. Following a 24-hour incubation period, diluted compounds were introduced to the wells. After 144 hours, a CellTiter-Glo luminescent cell viability assay (Promega, Madison, WI, USA) was performed to assess cell viability. The luminescent readings were normalized as percentages relative to untreated cells, and the IC50 values for each compound were determined.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[256]
Efficacy Data	Half Maximal Effective Concentration (EC50)	166.41&#17739.34 ng/mL	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	Cells were distributed into 96-well white round-bottom plates, with each well receiving 1000 cells in RPMI-1640 medium supplemented with 10% FBS. Following a 24-hour incubation period, diluted compounds were introduced to the wells. After 144 hours, a CellTiter-Glo luminescent cell viability assay (Promega, Madison, WI, USA) was performed to assess cell viability. The luminescent readings were normalized as percentages relative to untreated cells, and the IC50 values for each compound were determined.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Effective Concentration (EC50)	182.4 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 3000 ng/mL	Negative HER2 expression (HER2-)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC-78 cells		CVCL_2061

Experiment 1 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Effective Concentration (EC50)	251 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 3000 ng/mL	Negative HER2 expression (HER2-)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC-78 cells		CVCL_2061

Experiment 1 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Effective Concentration (EC50)	265 ng/mL	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[255]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 3000 ng/mL	Negative HER2 expression (HER2-)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC-78 cells		CVCL_2061

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	< 10%	Negative HER2 expression (HER2-)
Method Description	Growth inhibition test of HER2-negative human breast cancer cell line (MDA-MB-231). The cells were seeded at 1000 cells / 100 pL / well. The cells were cultured at 37 0 C overnight, then the medium was exchanged with new one (95 uL/well), and the cells were treated with a test compound, which was adjusted to 2 ug/mL with PBS , at 5 uL/well (treatment concentration: 100 ng/mL). The cells were cultured for 6 days, then CellTiter-Glo was added thereto at 100 uL/well, and the luminescence amount of each well was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	95%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	< 10%	Negative HER2 expression (HER2-)
Method Description	Growth inhibition test of HER2-negative human breast cancer cell line (MDA-MB-231). The cells were seeded at 1000 cells / 100 pL / well. The cells were cultured at 37 0 C overnight, then the medium was exchanged with new one (95 uL/well), and the cells were treated with a test compound, which was adjusted to 2 ug/mL with PBS , at 5 uL/well (treatment concentration: 100 ng/mL). The cells were cultured for 6 days, then CellTiter-Glo was added thereto at 100 uL/well, and the luminescence amount of each well was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	107%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[211]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603