Payload ID	PAY0JCIBW
Name	Mertansine DM1
Synonyms	Mertansine; Maytansinoid DM 1; 139504-50-0; maytansinoid DM1; Mertansine (DM1); N2'-deacetyl-N2'-(3-mercapto-1-oxopropyl)-maytansine; DDZ29HGH0E; DM 1; [(1S,2R,3S,5S,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[methyl(3-sulfanylpropanoyl)amino]propanoate; DM1; Maytansine, N2'-deacetyl-N2'-(3-mercapto-1-oxopropyl)-; N2'-Deacetyl-N2'-(3-mercapto-1-oxopropyl)-maytansine, L-; DM1 [Maytansinoid]; DM 1 [Maytansinoid]; UNII-DDZ29HGH0E; Mertasine; DM1;Maytansinoid; Maytansinoid DM1; MAYTANSINOID DM1 [MI]; CHEMBL4802230; SCHEMBL13558634; CHEBI:82755; MFCD28398157; s6773; CS-5804; DA-48536; HY-19792; J3.653.420F; Q4515649; (1S,2R,3S,5S,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.1(10,14).0(3,5)]hexacosa-10(26),11,13,16,18-pentaen-6-yl (2S)-2-[methyl(3-sulfanylpropanoyl)amino]propanoate; (3S)-3-O-De[2-(acetylmethylamino)-1-oxopropyl]-3-O-[(2S)-2-(methyl 3-mercaptopropanoylamino)propanoyl]maytansine    Click to Show/Hide
Target	Microtubule (MT)					Target Info
Structure
	3D MOL			2D MOL
Formula	C35H48ClN3O10S
Isosmiles	C[C@@H]1[C@@H]2C[C@]([C@@H](/C=C/C=C(/CC3=CC(=C(C(=C3)OC)Cl)N(C(=O)C[C@@H]([C@]4([C@H]1O4)C)OC(=O)[C@H](C)N(C)C(=O)CCS)C)\C)OC)(NC(=O)O2)O
PubChem CID	11343137
InChI	InChI=1S/C35H48ClN3O10S/c1-19-10-9-11-26(46-8)35(44)18-25(47-33(43)37-35)20(2)31-34(4,49-31)27(48-32(42)21(3)38(5)28(40)12-13-50)17-29(41)39(6)23-15-22(14-19)16-24(45-7)30(23)36/h9-11,15-16,20-21,25-27,31,44,50H,12-14,17-18H2,1-8H3,(H,37,43)/b11-9+,19-10+/t20-,21+,25+,26-,27+,31+,34+,35+/m1/s1
InChIKey	ANZJBCHSOXCCRQ-FKUXLPTCSA-N
IUPAC Name	[(1S,2R,3S,5S,6S,16E,18E,20R,21S)-11-chloro-21-hydroxy-12,20-dimethoxy-2,5,9,16-tetramethyl-8,23-dioxo-4,24-dioxa-9,22-diazatetracyclo[19.3.1.110,14.03,5]hexacosa-10,12,14(26),16,18-pentaen-6-yl] (2S)-2-[methyl(3-sulfanylpropanoyl)amino]propanoate
Pharmaceutical Properties	Molecule Weight		738.3	Polar area		158
	Complexity		1340	xlogp Value		2.2
	Heavy Count		50	Rot Bonds		8
	Hbond acc		11	Hbond Donor		3

Experiment 1 Reporting the Activity Date of This ADC					[1]
Patients Enrolled	Key eligibility: Adults (≥18) with progressive advanced sarcoma/prostate/breast/ovarian/pancreatic cancers (ECOG ≤2, life expectancy ≥6 months) post ≥1 prior therapy. Requires ACT Tumor Board recommendation, adequate organ function (ANC ≥1,500/uL, platelets ≥100,000/uL, bilirubin ≤1.5×ULN), and measurable disease. Major exclusions: active secondary malignancies, untreated CNS metastases, uncontrolled comorbidities (NYHA III-IV heart failure, severe infections), pregnancy/breastfeeding, or conditions jeopardizing protocol compliance.    Click to Show/Hide
Administration Dosage	Administered in monotherapy or in combination with other targeted agents or immunotherapies, chemotherapies, or radiation. Combination treatment plans may include a two-week monotherapy lead-in, followed by a combination treatment regimen. Each ACT study intervention must have an established RP2D determined in a prior clinical trial. Participants undergo a Pre-Treatment Biopsy, plus an On-Treatment Biopsy after two weeks on first dose of study drug (s) and prior to starting Cycle 2, regardless of regimen. Participants continue to receive study agent (s) after the On-Treatment Biopsy, according to the biopsy results and the results of ongoing safety and clinical assessments. Treatment cycles repeat every 21 to 28 days in the absence of disease progression or unacceptable toxicity. Cycles are determined based on the study agent (s). Upon disease progression, participants are given the option to undergo an additional biopsy.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05238831	Phase Status	EARLY_PHASE1
Clinical Description	Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART) Trial: Adaptive Clinical Treatment (ACT)
Primary Endpoint	Primary endpoint evaluates feasibility of ACT therapy implementation, requiring ≥11/15 participants (80%) to initiate recommended regimen within 2 years, with protocol-specified analysis of barriers if threshold unmet.
Other Endpoint	Secondary objectives assess safety (CTCAE v5.0-graded AEs, discontinuation rates), efficacy (6-month ORR by RECIST 1.1/pseudoprogression criteria), and survival outcomes (PFS, disease-specific survival, OS) through 5-year follow-up using Kaplan-Meier/cumulative incidence methods.
Experiment 2 Reporting the Activity Date of This ADC					[2]
Patients Enrolled	Key eligibility: Adults (≥18) with HER2+ (IHC3+/FISH+) metastatic breast cancer (1-3 prior lines, ECOG 0-1). Exclusions: prior HER2-ADC use, active CNS metastases (except stable treated lesions), uncontrolled effusions/ILD, significant cardiac disease, QTc risks, active infections (HBV/HCV/HIV), or pregnancy. Requires adequate organ function (ANC ≥1.0×109/L, LVEF >50%) and measurable disease (RECIST 1.1).    Click to Show/Hide
Administration Dosage	FS-1502 Dosage form: lyophilized powder Specification: 30 mg/vial Dose: 2.3 mg/kg, once every 3 weeks, 21 days as a cycle; Method of administration: intravenous drip.
Related Clinical Trial
NCT Number	NCT05755048	Phase Status	PHASE3
Clinical Description	A Multicenter, Open-label, Randomized Controlled Phase III Clinical Study to Compare the Efficacy and Safety of FS-1502 Versus T-DM1 in Patients With HER2-positive Unresectable Locally Advanced or Metastatic Breast Cancer
Primary Endpoint	Primary endpoint evaluates PFS by independent central review (up to 28 months) in HER2+ metastatic breast cancer patients post-trastuzumab/taxane treatment, defined as time from enrollment to disease progression (≥20% target lesion increase per RECIST 1.1) or death.
Other Endpoint	Secondary objectives assess OS (time to death), ORR (confirmed CR+PR rates), DCR (CR+PR+SD), CBR (response lasting ≥24 weeks), DOR (response duration), and treatment-emergent AEs (NCI-CTCAE v5.0 graded) over 28 months.
Experiment 3 Reporting the Activity Date of This ADC					[3]
Patients Enrolled	Key eligibility: Adults (≥18) with untreated HER2+ (IHC3+) metastatic breast cancer (ECOG 0-1, LVEF ≥50%), no prior systemic therapy except THP within 6 weeks. Exclusions: prior invasive breast cancer treatment, uncontrolled cardiac/ILD conditions, active infections (unless controlled HIV/HBV/HCV), CYP2C8/3A4 modifiers use, or pregnancy. Requires adequate organ function and stable brain metastases if present.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06439693	Phase Status	PHASE2
Clinical Description	A Single-Arm, Phase II Study of Sequential Therapy With Curative Intent in de Novo HER2+ Metastatic Breast Cancer: The SAPPHO Study:
Primary Endpoint	Primary endpoint evaluates 4-year Disease-Free Survival (DFS4) using Kaplan-Meier method in HER2+ metastatic breast cancer patients, measuring time from registration to disease progression/death/anti-cancer therapy resumption (excluding endocrine therapy), with censoring at last evaluation for progression-free survivors.
Other Endpoint	Secondary objectives assess median Overall Survival (OS), Objective Response Rate (ORR by RECIST 1.1), Grade 3-5 treatment-related toxicity (CTCAE v5.0), completion rates of sequential therapy parts (A: taxane/trastuzumab/pertuzumab; B: trastuzumab deruxtecan; C: T-DM1/tucatinib; D: trastuzumab/pertuzumab/tucatinib), and DFS4 by Minimal Residual Disease status over 54 months.    Click to Show/Hide
Experiment 4 Reporting the Activity Date of This ADC					[2]
Patients Enrolled	Eligible patients (≥18 years) must have HER2+ disease (IHC3+ or IHC2+/FISH+), 1-3 prior lines (including adjuvant trastuzumab/taxane), ECOG 0-1, LVEF>50%, and adequate organ function. Key exclusions: prior HER2-ADC use, uncontrolled CNS metastases (unless stable ≥6 months post-treatment), QTc prolongation risks, active HBV/HCV/HIV, or unresolved toxicity >CTCAE G1 (except alopecia/stable G2 neuropathy).    Click to Show/Hide
Administration Dosage	Experimental: FS-1502 Dosage form: lyophilized powder Specification: 30 mg/vial Dose: 2.3 mg/kg, once every 3 weeks, 21 days as a cycle; Method of administration: intravenous drip.
Related Clinical Trial
NCT Number	NCT05755048	Phase Status	PHASE3
Clinical Description	A Multicenter, Open-label, Randomized Controlled Phase III Clinical Study to Compare the Efficacy and Safety of FS-1502 Versus T-DM1 in Patients With HER2-positive Unresectable Locally Advanced or Metastatic Breast Cancer
Primary Endpoint	The study evaluates PFS by ICR in HER2+ unresectable/metastatic breast cancer patients previously treated with trastuzumab/taxanes over 28 months, with PD defined as ≥20% target lesion increase per RECIST v1.1.
Other Endpoint	Key efficacy endpoints (OS, ORR, DCR, CBR, DOR) and safety (TEAEs per NCI-CTCAE v5.0) are assessed via ICR/investigator over 28 months, with ORR requiring confirmed CR/PR (CR=target lesion disappearance; PR=≥30% decrease).
Experiment 5 Reporting the Activity Date of This ADC					[4]
Patients Enrolled	Eligible patients (≥18 years) have HER2+ advanced cancers (IHC3+ or IHC2+/FISH+), ECOG 0-1, LVEF>50%, with ≥2 prior anti-HER2 lines. Key exclusions: CNS metastases, recent major surgery/RT (<4 weeks), QTc >470ms, active HBV/HCV/HIV, or unresolved toxicity >CTCAE G1 (except stable G2 alopecia/neuropathy). Tissue confirmation is mandatory for pivotal study participants.    Click to Show/Hide
Administration Dosage	Phase Ia: Patients enrolled on the 1.2 and 2.0 regimens: FS-1502 monotherapy every 4 weeks with intravenous drip, 28 days as a cycle; Patients enrolled on the 3.0 regimens: starting from the 1.0mg/kg dose group, FS-1502 monotherapy every 3 weeks with intravenous drip, 21 days as a cycle; Phase Ib: FS-1502 monotherapy, the dose and frequency of administration for Stage Ib will be obtained according to Phase Ia (RP2D).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT03944499	Phase Status	PHASE1
Clinical Description	A Phase I,Multicenter,Open-label,Single-arm Study:A Dose-escalation Phase Evaluating FS1502 in Patients With HER2 Expressed Advanced Solid Tumors,and a Dose-expanded Phase in Patients With Local Advanced or Metastatic,HER2+ Breast Cancer
Primary Endpoint	The Phase Ia study evaluates DLT (NCI-CTCAE v5.0) and determines MTD/RP2D for FS-1502. ORR (CR/PR per RECIST v1.1) is assessed by IRC in Phase Ib over ~2 years in HER2+ solid tumors with confirmed HER2 expression criteria.
Other Endpoint	Safety analyses include TEAEs (CTCAE v5.0), SAEs, and treatment discontinuations over ~3 years. Efficacy is measured by PFS (time to progression/death), OS (1-year rate), DOR (CR/PR to progression), and CBR (CR/PR/SD >6 mo). PK parameters (AUC, Cmax, tmax, T1/2, clearance) and anti-drug antibodies are also assessed.

Experiment 1 Reporting the Activity Date of This ADC					[5]
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 <1.5×109/L, platelets <100×109/L, ALT/AST >2.5×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.
Related Clinical Trial
NCT Number	NCT03953833	Phase 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					[6]
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.
Related Clinical Trial
NCT Number	NCT06042894	Phase 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					[7]
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.
Related Clinical Trial
NCT Number	NCT05990803	Phase 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					[8]
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.
Related Clinical Trial
NCT Number	NCT06008054	Phase 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					[9]
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 ≤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 ≥3 immune-related adverse events from immunotherapy.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05668858	Phase 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					[10]
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.
Related Clinical Trial
NCT Number	NCT06006169	Phase 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					[11]
Patients Enrolled	Eligible patients (18-75 years) must have recurrent/metastatic HNSCC (excluding nasopharyngeal origin) with measurable lesions (RECIST 1.1), ECOG ≤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 ≥3 immune-related adverse events from immunotherapy.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06668961	Phase 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					[12]
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, ≥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	Phase 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					[13]
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: ≥3 lines; Cohort_B: standard therapy failure or treatment-naïve).    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05924841	Phase 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					[14]
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 ≥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	Phase 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&plusmn; 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					[15]
Patients Enrolled	Eligible patients (Phase Ia: ≥18-75 years; Phase Ib: ≥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	Phase 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					[16]
Patients Enrolled	Eligible patients (≥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 ≥90g/L, ANC ≥1.5×109/L, platelets ≥100×109/L, Cr ≤1.5 ULN (Ccr ≥40 mL/min), LVEF ≥50%. HIV/HBV/HCV active infections disqualify.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05965856	Phase 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					[17]
Related Clinical Trial
NCT Number	NCT03953833	Phase 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					[18]
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	Phase Status	PHASE1
Clinical Description	.
Experiment 2 Reporting the Activity Date of This ADC					[19]
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					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 9.18%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 208.4 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 5 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	Breast cancer PDX model
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 60.63%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 208.4 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 10 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX model (PDX: CHGA-010)
Experiment 3 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 73.73%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 208.4 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 10 mg/kg intravenous (i.v, q3w x2) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	Gastric cancer PDX model (PDX: CHGA-010)
Experiment 4 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.30%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 208.4 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 15 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	Breast cancer PDX model

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 52.51%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 208.4 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 10 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	MFM223 CDX model
In Vitro Model	Breast carcinoma	MFM-223 cells		CVCL_1408
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.93%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 171.7 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 5 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	NCI-H716 CDX model
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 3 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 66.08%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 171.7 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 15 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	NCI-H716 CDX model
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 4 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.41%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1-0.7 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Down syndrome	KATO III cells		CVCL_0371
Experiment 3 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive FGFR2 expression (FGFR2+++/++)
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 carcinoma	SUM52PE cells		CVCL_3425
Experiment 4 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.2 nM	Positive FGFR2 expression (FGFR2+++/++)
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 adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 5 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1 nM	Positive FGFR2 expression (FGFR2+++/++)
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 carcinoma	MFM-223 cells		CVCL_1408
Experiment 6 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30 nM	Negative FGFR2 expression (FGFR2-)
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 carcinoma	NUGC-3 cells		CVCL_1612

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 36.75%	Positive ASPH expression (ASPH +++/++)
Method Description	Mice bearing an approximately 100 mm3 tumor xenograft were intravenously injected weekly with 2.5 mg/kg of SNS-622 or SNS-622-DM1, and tumor growth was monitored.
In Vivo Model	Pancreatic ductal adenocarcinoma PDX model

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55.56%	Positive ASPH expression (ASPH +++/++)
Method Description	MIA PaCa2-empty vector and MIA-PaCa2-ASPH cell lines generated sc tumors in the NSG mice were treated with SNS-622-DM1 (5 mg/kg. every 7 day) and a non-relevant IgG mAb also conjugated with DM1.
In Vivo Model	MIA PaCa2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.90%	Positive CD138 expression (CD138+++/++)
Method Description	The in vivo antitumor activity of B-B4-DM1 was evaluated in a CD138 positive OPM1 and OPM2 MM cells xenograft models. CB-17 SCID mice were inoculated subcutaneously in the interscapular area with 5x106 OPM1 (A-B) or OPM2 (C-D) MM cells. Animals were treated daily intravenously for 3 consecutive days with either vehicle alone (PBS; n = 5), unconjugated B-B4 (13.3 ug/kg; n = 5), B-B4DM1 (150 ug DM1/kg; n = 5), or control huC242-DM1 (150 ug DM1/kg; n = 5).    Click to Show/Hide
In Vivo Model	Multiple myeloma PDX model (PDX: OPM2)
In Vitro Model	Multiple myeloma	Multiple myeloma cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 27.30%	Positive CD138 expression (CD138+++/++)
Method Description	The in vivo antitumor activity of B-B4-DM1 was evaluated in a CD138 positive OPM1 and OPM2 MM cells xenograft models. CB-17 SCID mice were inoculated subcutaneously in the interscapular area with 5x106 OPM1 (A-B) or OPM2 (C-D) MM cells. Animals were treated daily intravenously for 3 consecutive days with either vehicle alone (PBS; n = 5), unconjugated B-B4 (13.3 ug/kg; n = 5), B-B4DM1 (150 ug DM1/kg; n = 5), or control huC242-DM1 (150 ug DM1/kg; n = 5).    Click to Show/Hide
In Vivo Model	CD138-expressing OPM1 MM cells xenograft model
In Vitro Model	Multiple myeloma	Multiple myeloma cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	25 nM	Positive CD138 expression (CD138+++/++)
Method Description	The inhibitory activity of B-B4-DM1 against cancer cell growth was compared with B-B4 and DM1 against cancer cell growth in vitro. The cells were treated with B-B4-DM1, B-B4 and DM1 for 96 hours.
In Vitro Model	Plasma cell myeloma	MM1.R cells		CVCL_8794

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 5 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 1 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 10.40%	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 3 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 11.50%	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 1 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian cancer	Ovarian cancer cells		Homo sapiens
Experiment 5 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 19.60%	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 5 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian cancer	Ovarian cancer cells		Homo sapiens
Experiment 6 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 32.90%	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 1 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian adenocarcinoma	OV-90 cells		CVCL_3768
Experiment 7 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46.40%	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 3 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian cancer	Ovarian cancer cells		Homo sapiens
Experiment 8 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.40%	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 3 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian adenocarcinoma	OV-90 cells		CVCL_3768
Experiment 9 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.90%	High NECTIN2 expression (NECTIN2+++)
Method Description	Treatments c12G1-DM1 at 5 mg/kg every 4th day by intraperitoneal injection.
In Vivo Model	Ovarian cancer CDX model
In Vitro Model	Ovarian adenocarcinoma	OV-90 cells		CVCL_3768

Experiment 1 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 2.01%	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,2 mg/kg.    Click to Show/Hide
In Vivo Model	GIST xenograft model
In Vitro Model	Mast cell leukemia	HMC-1.2 cells		CVCL_H205
Experiment 2 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 12.30%	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,1 mg/kg.    Click to Show/Hide
In Vivo Model	GIST xenograft model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 3 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 20.50%	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,3 mg/kg.    Click to Show/Hide
In Vivo Model	SCLC xenograft model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 4 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50.40%	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,1 mg/kg.    Click to Show/Hide
In Vivo Model	GIST xenograft model
In Vitro Model	Adult hepatocellular carcinoma	Huh-7 cells		CVCL_0336
Experiment 5 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.30%	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,5 mg/kg.    Click to Show/Hide
In Vivo Model	GIST xenograft model
In Vitro Model	Mast cell leukemia	HMC-1.2 cells		CVCL_H205
Experiment 6 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.30%	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,3.5 mg/kg.    Click to Show/Hide
In Vivo Model	GIST xenograft model
In Vitro Model	Mast cell leukemia	HMC-1.2 cells		CVCL_H205
Experiment 7 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.90%	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,3 mg/kg.    Click to Show/Hide
In Vivo Model	GIST xenograft model
In Vitro Model	Adult hepatocellular carcinoma	Huh-7 cells		CVCL_0336
Experiment 8 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.10%	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,3 mg/kg. The mice were intraperitoneally administered Etoposide was prepared in dimethyl sulfoxide, and the solution was diluted in PBS just before administration. The mice were intraperitoneally administered etoposide for 2 cycles (3 mg/kg per day;days 15 and days 1115).    Click to Show/Hide
In Vivo Model	GIST xenograft model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 9 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.30%	Positive KIT expression (KIT+++/++)
Method Description	The animal room had a controlled 12/12-h light/dark cycle (lights on at 06:00 AM), temperature (20±26 °C), and relativehumidity (50±10%). For xenograft assays, mice were anesthetized with isoflurane. Then, cells in 50% Matrigel were subcutaneously transplanted into 5-week-old female C.B-17 severe combined immunodeficiency (SCID) mice. In vivo efficacy studies were initiated when the volume of the tumors reached ~ 200 mm3. Imatinib was formulated in distilled water for oral administration. The mice were intravenously administered NN2101-DM1 three times at the indicated concentrations,3 mg/kg. The mice were intraperitoneally administered Etoposide was prepared in dimethyl sulfoxide, and the solution was diluted in PBS just before administration. The mice were intraperitoneally administered etoposide for 2 cycles (3 mg/kg per day;days 15 and days 1115).    Click to Show/Hide
In Vivo Model	SCLC xenograft model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569

Experiment 1 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 ng/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 2 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 ng/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Gastrointestinal stromal tumor	GIST-430/654 cells		CVCL_7040
Experiment 3 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.02 ng/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 4 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.07 ng/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 5 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.77 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Mast cell leukemia	HMC-1.2 cells		CVCL_H205
Experiment 6 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.18 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 7 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.52 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Ovarian serous adenocarcinoma	Caov-3 cells		CVCL_0201
Experiment 8 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.54 ug/mL	Negative KIT expression (KIT-)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 9 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.99 ug/mL	Negative KIT expression (KIT-)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 10 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.71 ug/mL	Negative KIT expression (KIT-)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Lung squamous cell carcinoma	NCI-H2170 cells		CVCL_1535
Experiment 11 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.03 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 12 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.3 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 13 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.47 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 14 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.38 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Esophageal squamous cell carcinoma	TF-1 cells		CVCL_1759
Experiment 15 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.84 ug/mL	Negative KIT expression (KIT-)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Normal	COS-7 cells		CVCL_0224
Experiment 16 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.95 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Normal	HUVEC-C cells		CVCL_2959
Experiment 17 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.47 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Lung small cell carcinoma	NCI-H889 cells		CVCL_1598
Experiment 18 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.49 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Gastrointestinal stromal tumor	GIST48 cells		CVCL_7041
Experiment 19 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.63 ug/mL	Positive KIT expression (KIT+++/++)
Method Description	For apoptosis assays, the cells were seeded into 96-well plates and incubated in a humidified CO2 chamber for 16 h. The cells were incubated with vehicle, NN2101-DM1 (1g/mL) for 72 h.
In Vitro Model	Lung small cell carcinoma	Ms-1 cells		CVCL_IQ55

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 2.05%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 171.7 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 5 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	NCI-H716 CDX model
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 57.22%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 171.7 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 15 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	NCI-H716 CDX model
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 3 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.68%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 208.4 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 10 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	MFM223 CDX model
In Vitro Model	Breast carcinoma	MFM-223 cells		CVCL_1408
Experiment 4 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.61%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive FGFR2 expression (FGFR2+++/++)
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 carcinoma	SUM52PE cells		CVCL_3425
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.5 nM	Positive FGFR2 expression (FGFR2+++/++)
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 adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 3 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.6 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Down syndrome	KATO III cells		CVCL_0371
Experiment 4 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.7 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 5 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.5 nM	Positive FGFR2 expression (FGFR2+++/++)
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 carcinoma	MFM-223 cells		CVCL_1408
Experiment 6 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30 nM	Negative FGFR2 expression (FGFR2-)
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 carcinoma	NUGC-3 cells		CVCL_1612

Experiment 1 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 2.75%	Positive PLAUR expression (PLAUR +++/++)
Method Description	To compare the in vivo anti-tumor efficacy of the various ADC constructs, we used MDA-MB-231 xenografts in mice. Animals with tumors of approximately 100 mm3 were treated once a week for four weeks with a 10 mg/kg dose of a variety of DAR 4 ADCs or 2G10 antibody.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Positive PLAUR expression (PLAUR +++/++)
Method Description	MDA-MB-231 cells (0.5x104 cells/well) were seeded in 96-well plates at the density and incubated for 120 h (5 days) with of ADCs or IgG. After 5 days of drug treatment at 37°C with 5% CO2.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 17.58%	Positive ITGAV expression (ITGAV +++/++)
Method Description	The rear flank region of female athymic rats were implanted with 5x106 cells subcutaneously (0.2 ml of25 x106 cells/ml) on the rear flank area. When mean tumor volumes reached to 250 mm3, dosed intravenously (15 mg/kg) on days 17 and 29 after tumor cell injection.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 20.88%	Positive ITGAV expression (ITGAV +++/++)
Method Description	Female athymic rats were inoculated with 5x106 HT29 cells subcutancously on the rear flank area. The animals were stratified into 13 groups, 6 animals per group based on a mean tumor volume for each group of approximately 250 mm3. On the day of grouping (day 7) each group received its initial dosing (175 ug/kg).
In Vivo Model	HT-29 CDX model
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ

Experiment 1 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 17.58%	Positive ITGAV expression (ITGAV +++/++)
Method Description	The rear flank region of female athymic rats were implanted with 5x106 cells subcutaneously (0.2 ml of25 x106 cells/ml) on the rear flank area. When mean tumor volumes reached to 250 mm3, dosed intravenously (15 mg/kg) on days 17 and 29 after tumor cell injection.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 20.12%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (1.25 mg/kg).    Click to Show/Hide
In Vivo Model	GIST430 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 32.28%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (1.25 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 39.65%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST430 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.09%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST430 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 5 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 72%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (0.625 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 6 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 75.90%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 7 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.25%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 8 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 79.31%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (1.25 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H526 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 9 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.81%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.0 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 10 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.44%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H526 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 11 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.51%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H526 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	59%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	71%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	76%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	80%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 5 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	90%	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 6 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	98%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 7 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	99%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 8 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	99%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 9 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 10 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 11 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 12 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.47 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 13 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.55 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 14 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.64 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 15 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.82 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 16 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	46.83 nM	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 23.23%	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (1 mg/kg, twice a week for 4 weeks) induces efficient tumor cell killing in cell line-derived models of A549 cells with CD147 expression with high expression.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 23.23%	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (2 mg/kg, twice a week for 4 weeks) induces efficient tumor cell killing in cell line-derived models of A549 cells with CD147 expression with high expression.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 38.63%	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (4 mg/kg, twice a week for 4 weeks) induces efficient tumor cell killing in cell line-derived models of A549 cells with CD147 expression with high expression.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.95%	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (8 mg/kg, twice a week for 4 weeks) induces efficient tumor cell killing in cell line-derived models of A549 cells with CD147 expression with high expression.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.22%	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (16 mg/kg, twice a week for 4 weeks) induces efficient tumor cell killing in cell line-derived models of A549 cells with CD147 expression with high expression.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 6 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.20%	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (30 mg/kg, i.v. injection weekly in a total 4 doses) induces efficient tumor cell killing in cell line-derived models of NCI-H226 cells with CD147 expression with high expression.
In Vivo Model	NCI-H226 CDX model
In Vitro Model	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544
Experiment 7 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.84%	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (32 mg/kg, twice a week for 4 weeks) induces efficient tumor cell killing in cell line-derived models of A549 cells with CD147 expression with high expression.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 8 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.40%	Positive CD147 expression (CD147 +++/++)
Method Description	HcHAb18-DM1 (18 mg/kg, twice a week for 4 weeks) induces efficient tumor cell killing in cell line-derived models of NCI-H460 cells with CD147 expression with high expression.
In Vivo Model	NCI-H460 CDX model
In Vitro Model	Lung large cell carcinoma	NCI-H460 cells		CVCL_0459

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.46 ug/mL	Positive CD147 expression (CD147 +++/++)
Method Description	In vitro efficacy of HcHAb18-DM1 versus HcHAb18 and IgG1-DM1 on six cell lines treated for 72 h.
In Vitro Model	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.77 ug/mL	Positive CD147 expression (CD147 +++/++)
Method Description	In vitro efficacy of HcHAb18-DM1 versus HcHAb18 and IgG1-DM1 on six cell lines treated for 72 h.
In Vitro Model	Lung large cell carcinoma	NCI-H460 cells		CVCL_0459
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.96 ug/mL	Positive CD147 expression (CD147 +++/++)
Method Description	In vitro efficacy of HcHAb18-DM1 versus HcHAb18 and IgG1-DM1 on six cell lines treated for 72 h.
In Vitro Model	Lung squamous cell carcinoma	NCI-H520 cells		CVCL_1566
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.26 ug/mL	Positive CD147 expression (CD147 +++/++)
Method Description	In vitro efficacy of HcHAb18-DM1 versus HcHAb18 and IgG1-DM1 on six cell lines treated for 72 h.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.74%	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 3 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 2 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.54%	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 6 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 3 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.81%	Positive ITGAV expression (ITGAV +++/++)
Method Description	Female athymic rats were inoculated with 5x106 HT29 cells subcutancously on the rear flank area. The animals were stratified into 13 groups, 6 animals per group based on a mean tumor volume for each group of approximately 250 mm3. On the day of grouping (day 7) each group received its initial dosing (175 ug/kg).
In Vivo Model	HT-29 CDX model
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 4 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 71.21%	Positive ITGAV expression (ITGAV +++/++)
Method Description	Nine-week-old athymic nude rats were subcutaneously inoculated with A375.S2human melanoma cells. ADC (5 mg/kg) andappropriate control compounds were intravenously injected (three injection every other day inthe first week followed by one injection per week for two weeks.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 5 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.15%	Positive ITGAV expression (ITGAV +++/++)
Method Description	Nine-week-old athymic nude rats were subcutaneously inoculated with A375.S2human melanoma cells. ADC (10 mg/kg) andappropriate control compounds were intravenously injected (three injection every other day inthe first week followed by one injection per week for two weeks.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 6 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.23%	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 10 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 7 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.10%	Positive ITGAV expression (ITGAV +++/++)
Method Description	The rear flank region of female athymic rats were implanted with 5x106 cells subcutaneously (0.2 ml of25 x106 cells/ml) on the rear flank area. When mean tumor volumes reached to 250 mm3, dosed intravenously (15 mg/kg) on days 17 and 29 after tumor cell injection.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 8 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.81%	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 15 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136

Experiment 1 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1 ug/mL	Positive ITGAV expression (ITGAV +++/++)
Method Description	Cells were seeded into white 96-well tissue culture plates (5000 cells/well)in culture medium and incubated for 16 hrs. Serial dilutions of immunoconjugates were added toeach appropraite wells (0-20 ug/ml). Tissue culture plates were incubated at 37°C for 96 hrs.
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 2 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.2 ug/mL	Positive ITGAV expression (ITGAV +++/++)
Method Description	Cells were seeded into white 96-well tissue culture plates (5000 cells/well)in culture medium and incubated for 16 hrs. Serial dilutions of immunoconjugates were added toeach appropraite wells (0-20 ug/ml). Tissue culture plates were incubated at 37°C for 96 hrs.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.19 mg/mL	Positive ITGAV expression (ITGAV +++/++)
Method Description	Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 4 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.27 mg/mL	Positive ITGAV expression (ITGAV +++/++)
Method Description	Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
In Vitro Model	Ovarian endometrioid adenocarcinoma	A2780 cells		CVCL_0134
Experiment 5 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.27 mg/mL	Positive ITGAV expression (ITGAV +++/++)
Method Description	Cells were harvested, rinsedsuspended in serum free DMEM, and sequentially incubated for 60 minutes on ice with serialdiluted CNTO 95,CNTO 364, CNTO 365 and CNTO 366 and FITC-labeled anti-humanantibody (10 mg/ml).
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.74%	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 3 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 2 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.54%	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 6 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 3 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.23%	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 10 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 4 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.81%	Positive ITGAV expression (ITGAV +++/++)
Method Description	On the day of grouping (Day 0), animals were weighed and intravenously injectedwith control ADC at 25 mg/kg. All testand control articles were given in a volume of 1ml/100 gm of body weight. CNTO 364 at 15 mg/kg groups was administered i.v. on a q7dx5 schedule.
In Vivo Model	A375.S2 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136

Experiment 1 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.42%	Positive PLAUR expression (PLAUR +++/++)
Method Description	To compare the in vivo anti-tumor efficacy of the various ADC constructs, we used MDA-MB-231 xenografts in mice. Animals with tumors of approximately 100 mm3 were treated once a week for four weeks with a 10 mg/kg dose of a variety of DAR 4 ADCs or 2G10 antibody.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Positive PLAUR expression (PLAUR +++/++)
Method Description	MDA-MB-231 cells (0.5x104 cells/well) were seeded in 96-well plates at the density and incubated for 120 h (5 days) with of ADCs or IgG. After 5 days of drug treatment at 37°C with 5% CO2.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.85%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 171.7 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 5 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	NCI-H716 CDX model
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 35.79%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 171.7 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 15 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	NCI-H716 CDX model
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581
Experiment 3 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.52%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Down syndrome	KATO III cells		CVCL_0371
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3 nM	Positive FGFR2 expression (FGFR2+++/++)
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 adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	32.17%	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Animals with established tumors of about 130 mm3 were treated with intravenous single injection of the M9346A-DM conjugates at 25 02 mg/kg, equivalent to 51 3 g conjugated maytansinoid per kg The conjugates were injected on day 20 after cell inoculation.
In Vivo Model	FRalpha-positive KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	50%	High FOLR1 expression (FOLR1+++; 1,300,000 FOLR1 molecules/cell)
Method Description	Animals with established tumors of about 130 mm3 were treated with intravenous single injection of the M9346A-DM conjugates at 25 02 mg/kg, equivalent to 51 3 g conjugated maytansinoid per kg The conjugates were injected on day 7 after cell inoculation.
In Vivo Model	Ovarian carcinoma Igrov-1 CDX model
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11±0.04 nM	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13±0.08 nM	Moderate FOLR1 expression (FOLR1++; 290,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Gestational choriocarcinoma	JEG-3 cells		CVCL_0363
Experiment 3 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14±0.05 nM	High FOLR1 expression (FOLR1+++; 1,300,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304

Experiment 1 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 38.75%	Positive PLAUR expression (PLAUR +++/++)
Method Description	To compare the in vivo anti-tumor efficacy of the various ADC constructs, we used MDA-MB-231 xenografts in mice. Animals with tumors of approximately 100 mm3 were treated once a week for four weeks with a 10 mg/kg dose of a variety of DAR 4 ADCs or 2G10 antibody.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	500 nM	Positive PLAUR expression (PLAUR +++/++)
Method Description	MDA-MB-231 cells (0.5x104 cells/well) were seeded in 96-well plates at the density and incubated for 120 h (5 days) with of ADCs or IgG. After 5 days of drug treatment at 37°C with 5% CO2.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 40%	Positive KIT expression (KIT+++/++)
Method Description	In vivo efficacy of 4C9-DM1 was examined using mouse models xenotransplanted with NCI-H526, mice with established tumors were randomized into different treatment groups when the tumor volume reached ~200 mm 3. The dose of 4C9-DM1 was 1 mg/kg twice at day 0 and day 7.
In Vivo Model	Small cell lung cancer CDX model
In Vitro Model	Small cell lung cancer	Small cell lung cancer cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45%	Positive KIT expression (KIT+++/++)
Method Description	In vivo efficacy of 4C9-DM1 was examined using mouse models xenotransplanted with NCI-H526, mice with established tumors were randomized into different treatment groups when the tumor volume reached ~200 mm 3. The dose of 4C9-DM1 was 3 mg/kg twice at day 0 and day 7.
In Vivo Model	Small cell lung cancer CDX model
In Vitro Model	Small cell lung cancer	Small cell lung cancer cells		Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59%	Positive KIT expression (KIT+++/++)
Method Description	In vivo efficacy of 4C9-DM1 was examined using mouse models xenotransplanted with NCI-H526, mice with established tumors were randomized into different treatment groups when the tumor volume reached ~200 mm 3. The dose of 4C9-DM1 was 5 mg/kg twice at day 0 and day 7.
In Vivo Model	Small cell lung cancer CDX model
In Vitro Model	Small cell lung cancer	Small cell lung cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Positive KIT expression (KIT+++/++)
Method Description	C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 2 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive KIT expression (KIT+++/++)
Method Description	C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
In Vitro Model	Lung small cell carcinoma	NCI-H889 cells		CVCL_1598
Experiment 3 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.08 nM	Positive KIT expression (KIT+++/++)
Method Description	C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 4 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.58 nM	Negative KIT expression (KIT-)
Method Description	C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
In Vitro Model	Lung small cell carcinoma	NCI-H446 cells		CVCL_1562
Experiment 5 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	35.5 nM	Negative KIT expression (KIT-)
Method Description	C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
In Vitro Model	Lung squamous cell carcinoma	NCI-H2170 cells		CVCL_1535
Experiment 6 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	47.63 nM	Negative KIT expression (KIT-)
Method Description	C-Kit positive or negative SCLC cell lines were seeded into 96-well plates and incubated with 4C9 or 4C9-DM1 in a dose-dependent manner for 35 days.
In Vitro Model	Amelanotic melanoma	MDA-MB-435 cells		CVCL_0417

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 41.22%	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	M9346A-4a-Cxxx-Mal-CX-DM1 (200 ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of KB cells with HER2 expression with high expression.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.58%	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	M9346A-4a-Cxxx-Mal-CX-DM1 (100 ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of KB cells with HER2 expression with high expression.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Cytotoxic IC50 Values (as a Function of [ADC] and [DM1]) for Various M9346A-CX-DM1 ADCs against FR-Expressing KB Cells in the absence of 1 M unconjugated M9346A antibody.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Cytotoxic IC50 Values (as a Function of [ADC] and [DM1]) for Various M9346A-CX-DM1 ADCs against FOLR1-Expressing KB Cells in the presence of 1 M unconjugated M9346A antibody.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 41.55%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.55%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.32%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 43%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 49%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (0.625 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 5 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	54%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	69%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	69%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	79%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 5 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	95%	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 6 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	97%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 7 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	99%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 8 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	100%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 9 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 10 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 11 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 12 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 13 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.33 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 14 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.34 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 15 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.51 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 16 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.69 nM	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (0.625 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	57%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	70%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	78%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	80%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 5 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	90%	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 6 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	98%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 7 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	99%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 8 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	99%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 9 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 10 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 11 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 12 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 13 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.5 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 14 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.24 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 15 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.07 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 16 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	45.43 nM	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.97%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 208.4 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 10 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	MFM223 CDX model
In Vitro Model	Breast carcinoma	MFM-223 cells		CVCL_1408
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.03%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 3 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.69%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 4 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 233 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 15 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	Positive FGFR2 expression (FGFR2+++/++)
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 carcinoma	SUM52PE cells		CVCL_3425
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Down syndrome	KATO III cells		CVCL_0371
Experiment 3 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3 nM	Positive FGFR2 expression (FGFR2+++/++)
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 adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 4 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24 nM	Positive FGFR2 expression (FGFR2+++/++)
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 carcinoma	MFM-223 cells		CVCL_1408
Experiment 5 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30 nM	Negative FGFR2 expression (FGFR2-)
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 carcinoma	NUGC-3 cells		CVCL_1612
Experiment 6 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (0.625 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 48%	Positive TF expression (TF +++)
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 3.75 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	HCC1806 CDX model
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive TF expression (TF +++)
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 15 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	HCC1806 CDX model
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive TF expression (TF +++)
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 squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive TF expression (TF +++)
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	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive TF expression (TF +++)
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	Hs 578T cells		CVCL_0332
Experiment 4 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive TF expression (TF +++)
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-231 cells		CVCL_0062
Experiment 5 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.2 nM	Positive TF expression (TF +++)
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	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 6 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	25.4 nM	Positive TF expression (TF +++)
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	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 7 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
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	T-47D cells		CVCL_0553
Experiment 8 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100 nM	Positive TF expression (TF +++)
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	MCF-7 cells		CVCL_0031
Experiment 9 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
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	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 10 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive TF expression (TF +++)
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-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 51.61%	Positive DLL4 expression (DLL4 +++/++)
Method Description	Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 1.5 mg/kg HLmD4 was intravenously administered once every three days for three weeks.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 57.73%	Positive DLL4 expression (DLL4 +++/++)
Method Description	Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 1.5 mg/kg HLmD4 was intravenously administered once every three days for three weeks.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.25%	Positive DLL4 expression (DLL4 +++/++)
Method Description	Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 5 mg/kg HLmD4 was intravenously administered once every three days for three weeks.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 4 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.11%	Positive DLL4 expression (DLL4 +++/++)
Method Description	Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 5 mg/kg HLmD4 was intravenously administered once every three days for three weeks.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	37.45 nM	Positive DLL4 expression (DLL4 +++/++)
Method Description	In vitro cytotoxicity and mechanism of anti-DLL4 ADCs. The cytotoxicity of ADCs was assessed by MTT assay. The percentage of cell inhibition relative to untreated control HUVEC cells was calculated for each drug concentration.
In Vitro Model	Normal	HUVEC-C cells		CVCL_2959

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	55.86%	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Animals with established tumors of about 130 mm3 were treated with intravenous single injection of the M9346A-DM conjugates at 25 02 mg/kg, equivalent to 51 3 g conjugated maytansinoid per kg The conjugates were injected on day 7 after cell inoculation.
In Vivo Model	FRalpha-positive KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	99.17%	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Five-week-old female CB-17 severe combined immunodeficient (SCID) mice were obtained and quarantined for 7 days prior to study initiation Mice were inoculated subcutaneously with KB cells (1 x107 cells per mouse) resuspended in serum-free culture mediaMice with established KB xenografts were dosed with a single intravenous injection of 200 g of conjugated maytansinoid per kg, equivalent to 102 mg/kg antibody on day 6 after cell inoculationTumor dimensions were measured twice weekly and volume was calculated as (A B2) 05, where A represents the largest and B the perpendicular tumor diameter.    Click to Show/Hide
In Vivo Model	FRalpha-positive KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08±0.01 nM	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.10±0.02 nM	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 3 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.00±2.00 nM	Moderate FOLR1 expression (FOLR1++; 290,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure) Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Gestational choriocarcinoma	JEG-3 cells		CVCL_0363
Experiment 4 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.00±0.70 nM	High FOLR1 expression (FOLR1+++; 1,300,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304

Experiment 1 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.67%	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 6 post cell inoculation with 2.5 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.15%	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 6 post cell inoculation with 5 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 3 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.52%	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 6 post cell inoculation with 10 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 4 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 5 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304
Experiment 6 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 7 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20 nM	Moderate FOLR1 expression (FOLR1 ++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Gestational choriocarcinoma	JEG-3 cells		CVCL_0363

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 57%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (0.625 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.61%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.0 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	54%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	69%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	74%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	80%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 5 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	91%	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 6 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	98%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 7 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	99%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 8 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	99%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 9 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 10 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 11 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 12 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 13 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.52 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 14 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.83 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 15 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.22 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 16 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.92 nM	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.12%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.2 nM	Positive FGFR2 expression (FGFR2+++/++)
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 adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.61 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 61.76%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.2 nM	Positive FGFR2 expression (FGFR2+++/++)
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 adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.59 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.10%	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	M9346A-4b-Cxxx-Mal-CX-DM1 (100 ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of KB cells with HER2 expression with high expression.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 73.36%	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	M9346A-4b-Cxxx-Mal-CX-DM1 (200 ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of KB cells with HER2 expression with high expression.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Cytotoxic IC50 Values (as a Function of [ADC] and [DM1]) for Various M9346A-CX-DM1 ADCs against FR-Expressing KB Cells in the absence of 1 M unconjugated M9346A antibody.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Cytotoxic IC50 Values (as a Function of [ADC] and [DM1]) for Various M9346A-CX-DM1 ADCs against FOLR1-Expressing KB Cells in the presence of 1 M unconjugated M9346A antibody.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.65%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (0.625 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.95%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (1.25 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.25%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	65%	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Five-week-old female CB-17 severe combined immunodeficient (SCID) mice were obtained and quarantined for 7 days prior to study initiation Mice were inoculated subcutaneously with KB cells (1 x107 cells per mouse) resuspended in serum-free culture mediaMice with established KB xenografts were dosed with a single intravenous injection of 200 g of conjugated maytansinoid per kg, equivalent to 102 mg/kg antibody on day 6 after cell inoculationTumor dimensions were measured twice weekly and volume was calculated as (A B2) 05, where A represents the largest and B the perpendicular tumor diameter.    Click to Show/Hide
In Vivo Model	FRalpha-positive KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08±0.02 nM	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	65%	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Five-week-old female CB-17 severe combined immunodeficient (SCID) mice were obtained and quarantined for 7 days prior to study initiation Mice were inoculated subcutaneously with KB cells (1 x107 cells per mouse) resuspended in serum-free culture mediaMice with established KB xenografts were dosed with a single intravenous injection of 200 g of conjugated maytansinoid per kg, equivalent to 102 mg/kg antibody on day 6 after cell inoculationTumor dimensions were measured twice weekly and volume was calculated as (A B2) 05, where A represents the largest and B the perpendicular tumor diameter.    Click to Show/Hide
In Vivo Model	FRalpha-positive KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07±0.02 nM	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.73%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Down syndrome	KATO III cells		CVCL_0371
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3 nM	Positive FGFR2 expression (FGFR2+++/++)
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 adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 71.12%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.2 nM	Positive FGFR2 expression (FGFR2+++/++)
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 adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 71.79%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.2 nM	Positive FGFR2 expression (FGFR2+++/++)
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 adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.45 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 74.86%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.2 nM	Positive FGFR2 expression (FGFR2+++/++)
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 adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.91 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 75%	Positive PDPN expression (PDPN +++/++)
Method Description	One day after cell inoculation, 100 mg of antibodies (P38B-DM1, P38B, or normal canine IgG) in 100 mL of PBS were injected into the peritoneal cavity of each mouse. On days 8 and 14, 5 mg/kg P38B-DM1 was injected into each mouse.
In Vivo Model	CHO/dPDPN CDX model
In Vitro Model	Melanoma	CHO cells (PDPN expression)		CVCL_0213

Experiment 1 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 48 ug/mL	Positive PDPN expression (PDPN +++/++)
Method Description	0.01-10 mg/mL for 30 minutes, followed by treatment with fluorescein isothiocyanate-conjugated.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[44]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	High HER2 expression (HER2+++)
Method Description	0.01-10 mg/mL for 30 minutes, followed by treatment with fluorescein isothiocyanate-conjugated.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[44]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	High HER2 expression (HER2+++)
Method Description	0.01-10 mg/mL for 30 minutes, followed by treatment with fluorescein isothiocyanate-conjugated.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[44]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.78 nM	High HER2 expression (HER2+++)
Method Description	0.01-10 mg/mL for 30 minutes, followed by treatment with fluorescein isothiocyanate-conjugated.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[44]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	35 nM	High HER2 expression (HER2+++)
Method Description	0.01-10 mg/mL for 30 minutes, followed by treatment with fluorescein isothiocyanate-conjugated.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 6 Reporting the Activity Date of This ADC					[44]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	97.62 nM	Low HER2 expression (HER2+)
Method Description	0.01-10 mg/mL for 30 minutes, followed by treatment with fluorescein isothiocyanate-conjugated.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 7 Reporting the Activity Date of This ADC					[44]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	110.54 nM	Low HER2 expression (HER2+)
Method Description	0.01-10 mg/mL for 30 minutes, followed by treatment with fluorescein isothiocyanate-conjugated.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 76.72%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.2 nM	Positive FGFR2 expression (FGFR2+++/++)
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 adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.33 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (0.625 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.01%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.0 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (2.5 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 5 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 NCI-H1048 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).    Click to Show/Hide
In Vivo Model	NCI-H1048 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	53%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	66%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	72%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	78%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 5 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	92%	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 6 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	98%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 7 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	99%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 8 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	99%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 9 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 10 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 11 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 12 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.72 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST882 cells		CVCL_7044
Experiment 13 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.74 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 14 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.26 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 15 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.49 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 16 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.77 nM	Negative KIT expression (KIT-)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.45%	Positive CD138 expression (CD138 +++/++)
Method Description	MOLP-8 cells (1.5x107 cells per mouse) suspended in a 50:50 mixture of serum free media and matrigel were injected subcutaneously in the area under the right shoulder in 100 ul. Nine groups (n=6) were treated with a single intravenous injection of ADCs, each at doses of 250 ug/kg.
In Vivo Model	MOLP-8 CDX model
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124

Experiment 1 Reporting the Activity Date of This ADC					[37]
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					[37]
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					[37]
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					[37]
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					[37]
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					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.61%	Positive CD138 expression (CD138 +++/++)
Method Description	MOLP-8 cells (1.5x107 cells per mouse) suspended in a 50:50 mixture of serum free media and matrigel were injected subcutaneously in the area under the right shoulder in 100 ul. Nine groups (n=6) were treated with a single intravenous injection of ADCs, each at doses of 250 ug/kg.
In Vivo Model	MOLP-8 CDX model
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124
Experiment 2 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.27%	Positive CD138 expression (CD138 +++/++)
Method Description	MOLP-8 cells (1.5x107 cells per mouse) suspended in a 50:50 mixture of serum free media and matrigel were injected subcutaneously in the area under the right shoulder in 100 ul. Nine groups (n=6) were treated with a single intravenous injection of ADCs, each at doses of 250 ug/kg.
In Vivo Model	MOLP-8 CDX model
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124
Experiment 3 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.11%	Positive CD138 expression (CD138 +++/++)
Method Description	MOLP-8 cells (1.5x107 cells per mouse) suspended in a 50:50 mixture of serum free media and matrigel were injected subcutaneously in the area under the right shoulder in 100 ul. Nine groups (n=6) were treated with a single intravenous injection of ADCs, each at doses of 450 ug/kg.
In Vivo Model	MOLP-8 CDX model
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00-10.00 nM	Positive CD138 expression (CD138 +++/++)
Method Description	CD138+ MOLP-8 cells were seeded in flat bottom plates at 3000 cells/well. CD138- BJAB control cells were seeded at 1000 cells/weli. The cells were treated with nBT062-SPDB-DM4nBT062-SPP-DM1 or nBT062-SMCC-DM1 at different concentrations for five days.
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124
Experiment 2 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative CD138 expression (CD138 -)
Method Description	CD138+ MOLP-8 cells were seeded in flat bottom plates at 3000 cells/well. CD138- BJAB control cells were seeded at 1000 cells/weli. The cells were treated with nBT062-SPDB-DM4nBT062-SPP-DM1 or nBT062-SMCC-DM1 at different concentrations for five days.
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.87%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	Positive FGFR2 expression (FGFR2+++/++)
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 adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.2 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.02%	Positive CD138 expression (CD138 +++/++)
Method Description	MOLP-8 cells (1.5x107 cells per mouse) suspended in a 50:50 mixture of serum free media and matrigel were injected subcutaneously in the area under the right shoulder in 100 ul. Nine groups (n=6) were treated with a single intravenous injection of ADCs, each at doses of 250 ug/kg.
In Vivo Model	MOLP-8 CDX model
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124
Experiment 2 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.32%	Positive CD138 expression (CD138 +++/++)
Method Description	MOLP-8 cells (1.5x107 cells per mouse) suspended in a 50:50 mixture of serum free media and matrigel were injected subcutaneously in the area under the right shoulder in 100 ul. Nine groups (n=6) were treated with a single intravenous injection of ADCs, each at doses of 250 ug/kg per week (five weeks).
In Vivo Model	MOLP-8 CDX model
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124
Experiment 3 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.27%	Positive CD138 expression (CD138 +++/++)
Method Description	MOLP-8 cells (1.5x107 cells per mouse) suspended in a 50:50 mixture of serum free media and matrigel were injected subcutaneously in the area under the right shoulder in 100 ul. Nine groups (n=6) were treated with a single intravenous injection of ADCs, each at doses of 450 ug/kg.
In Vivo Model	MOLP-8 CDX model
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive CD138 expression (CD138 +++/++)
Method Description	CD138+ MOLP-8 cells were seeded in flat bottom plates at 3000 cells/well. CD138- BJAB control cells were seeded at 1000 cells/weli. The cells were treated with nBT062-SPDB-DM4nBT062-SPP-DM1 or nBT062-SMCC-DM1 at different concentrations for five days.
In Vitro Model	Plasma cell myeloma	MOLP-8 cells		CVCL_2124
Experiment 2 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative CD138 expression (CD138 -)
Method Description	CD138+ MOLP-8 cells were seeded in flat bottom plates at 3000 cells/well. CD138- BJAB control cells were seeded at 1000 cells/weli. The cells were treated with nBT062-SPDB-DM4nBT062-SPP-DM1 or nBT062-SMCC-DM1 at different concentrations for five days.
In Vitro Model	Burkitt lymphoma	BJAB cells		CVCL_5711

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.93%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with Kasumi-1 cells. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	Kasumi-1 CDX model
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.35%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with Kasumi-1 cells. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of 2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	HMC-1 CDX model
In Vitro Model	Mast cell leukemia	HMC-1 cells		CVCL_0003
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	GIST430 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (10 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 5 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive KIT expression (KIT+++/++)
Method Description	Female SCID-beige mice were implanted subcutaneously with 10,000,000 cells. The total injection volume containingcells in suspension was 200 ul. Mice were enrolled in the study 15 days post implantation withaverage tumor volume of about 120 mm3. All treated groups received a single intravenous dose of2 mg/kg. After being randomly assigned to groups (n = 8/group), mice were administered a single i.v.dose of TBS (5 ml/kg) or ADC (5 mg/kg).    Click to Show/Hide
In Vivo Model	GIST-T1 CDX model
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	60%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	75%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	86%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H889 cells		CVCL_1598
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	87%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1930 cells		CVCL_1507
Experiment 5 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	91%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute megakaryoblastic leukemia	CMK-11-5 cells		CVCL_0217
Experiment 6 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	92%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 7 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	95%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells		CVCL_2481
Experiment 8 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	98%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 9 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	99%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 10 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	99%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Essential thrombocythemia	UKE-1 cells		CVCL_0104
Experiment 11 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	99%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	SKNO-1 cells		CVCL_2196
Experiment 12 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	99%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	OCI-M1 cells		CVCL_2149
Experiment 13 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	100%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute megakaryoblastic leukemia	M-07e cells		CVCL_2106
Experiment 14 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	100%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 15 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.02 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST-T1 cells		CVCL_4976
Experiment 16 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.05 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 17 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.05 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute megakaryoblastic leukemia	CMK-11-5 cells		CVCL_0217
Experiment 18 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.08 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 19 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.08 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute megakaryoblastic leukemia	M-07e cells		CVCL_2106
Experiment 20 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.09 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1930 cells		CVCL_1507
Experiment 21 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.11 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	OCI-M1 cells		CVCL_2149
Experiment 22 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.15 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H889 cells		CVCL_1598
Experiment 23 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.61 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells		CVCL_2481
Experiment 24 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	1.29 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Acute myeloid leukemia	Kasumi-6 cells		CVCL_0614
Experiment 25 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	1.8 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Essential thrombocythemia	UKE-1 cells		CVCL_0104
Experiment 26 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	3.6 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	SKNO-1 cells		CVCL_2196
Experiment 27 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	4 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 28 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	4.3 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.60%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Down syndrome	KATO III cells		CVCL_0371
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3 nM	Positive FGFR2 expression (FGFR2+++/++)
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 adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[38]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.30%	High HER2 expression (HER2+++)
Method Description	The SKOV3 xenografts were established in female BALB/c nu/nu mice by subcutaneous implantation of 1 x107 SKOV3 cells in 100 uL of medium in the abdominal region. The therapy started one week after the implantation. The mice were randomized in three groups (n = 910). One group of mice received intravenous (i.v.) injections of 13.3 mg/kg of ADAPT6-ABD-mcDM1 in 100 uL of PBS, the second group of mice received i.v. injections of the same dose of ADAPTNeg-ABD-mcDM1 in 100 uL of PBS, and the third group of mice received i.v. injections of 100 uL of PBS.    Click to Show/Hide
In Vivo Model	ER2-expressing SKOV3 ovarian cancer xenograft model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[49]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	High HER2 expression (HER2+++)
Method Description	The cytotoxic potential of ADAPT6-ABD-mcDM1 was investigated by incubation of dilution series of the conjugate with cell lines having different HER2-expression levels.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[49]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 nM	High HER2 expression (HER2+++)
Method Description	The cytotoxic potential of ADAPT6-ABD-mcDM1 was investigated by incubation of dilution series of the conjugate with cell lines having different HER2-expression levels.
In Vitro Model	Breast adenocarcinoma	AU565 cells		CVCL_1074
Experiment 3 Reporting the Activity Date of This ADC					[49]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80 nM	High HER2 expression (HER2+++)
Method Description	The cytotoxic potential of ADAPT6-ABD-mcDM1 was investigated by incubation of dilution series of the conjugate with cell lines having different HER2-expression levels.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.38%	Positive DLL4 expression (DLL4 +++/++)
Method Description	Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 5 mg/kg JmD4 was intravenously administered once every three days for three weeks.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 2 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.43%	Positive DLL4 expression (DLL4 +++/++)
Method Description	Drugs were intravenously (i.v.) administered in total three times on days 1, 4 and 7. 5 mg/kg JmD4 was intravenously administered once every three days for three weeks.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	36.12 nM	Positive DLL4 expression (DLL4 +++/++)
Method Description	In vitro cytotoxicity and mechanism of anti-DLL4 ADCs. The cytotoxicity of ADCs was assessed by MTT assay. The percentage of cell inhibition relative to untreated control HUVEC cells was calculated for each drug concentration.
In Vitro Model	Normal	HUVEC-C cells		CVCL_2959

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	85%	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Five-week-old female CB-17 severe combined immunodeficient (SCID) mice were obtained and quarantined for 7 days prior to study initiation Mice were inoculated subcutaneously with KB cells (1 x107 cells per mouse) resuspended in serum-free culture mediaMice with established KB xenografts were dosed with a single intravenous injection of 200 g of conjugated maytansinoid per kg, equivalent to 102 mg/kg antibody on day 6 after cell inoculationTumor dimensions were measured twice weekly and volume was calculated as (A B2) 05, where A represents the largest and B the perpendicular tumor diameter.    Click to Show/Hide
In Vivo Model	FRalpha-positive KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07±0.01 nM	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.56%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Down syndrome	KATO III cells		CVCL_0371
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3 nM	Positive FGFR2 expression (FGFR2+++/++)
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 adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	86.67%	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Five-week-old female CB-17 severe combined immunodeficient (SCID) mice were obtained and quarantined for 7 days prior to study initiation Mice were inoculated subcutaneously with KB cells (1 x107 cells per mouse) resuspended in serum-free culture mediaMice with established KB xenografts were dosed with a single intravenous injection of 200 g of conjugated maytansinoid per kg, equivalent to 102 mg/kg antibody on day 6 after cell inoculationTumor dimensions were measured twice weekly and volume was calculated as (A B2) 05, where A represents the largest and B the perpendicular tumor diameter.    Click to Show/Hide
In Vivo Model	FRalpha-positive KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15±0.02 nM	High FOLR1 expression (FOLR1+++; 4,500,000 FOLR1 molecules/cell)
Method Description	Dilutions of conjugates or unconjugated maytansinoid in the appropriate culture medium were added to wells of 96-well flat-bottomed plates containing 1 x103 cells per well The plates were incubated at 37°C, 6% CO2 for either 5 days (continuos exposure) or for 4 hours followed by 5-day incubation in conjugate-free medium (short exposure). Cell viability was determined by the WST-8 assay in accordance with the manufacturer's protocol, and IC50 were generated using a sigmoidal dose-response (variable slope) nonlinear regression curve fit.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.77%	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	M9436A-CX-DM1 (200 ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of KB cells with HER2 expression with high expression.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.30%	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	M9436A-CX-DM1 (100 ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of KB cells with HER2 expression with high expression.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Cytotoxic IC50 Values (as a Function of [ADC] and [DM1]) for Various M9346A-CX-DM1 ADCs against FR-Expressing KB Cells in the absence of 1 M unconjugated M9346A antibody.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Cytotoxic IC50 Values (as a Function of [ADC] and [DM1]) for Various M9346A-CX-DM1 ADCs against FOLR1-Expressing KB Cells in the presence of 1 M unconjugated M9346A antibody.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.66%	Positive FGFR2 expression (FGFR2+++/++)
Method Description	The total injection volume containing cells in suspension was 200 ul. Mice were enrolled in the first study eight days post implantation with average tumor volume of 192.9 mm3. After being randomly assigned to one of nine groups (n =8/group), mice were administered PBS or a single 3 mg/kg intravenous (i.v,) injection of one antibody drug conjugates.    Click to Show/Hide
In Vivo Model	SNU-16 CDX model
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3 nM	Positive FGFR2 expression (FGFR2+++/++)
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	Down syndrome	KATO III cells		CVCL_0371
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 3 nM	Positive FGFR2 expression (FGFR2+++/++)
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 adenocarcinoma	SNU-16 cells		CVCL_0076

Experiment 1 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.72%	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 6 post cell inoculation with 2.5 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.09%	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of KB cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once on day 6 post cell inoculation with 5 mg/kg of one of the conjugates listed above or with PBS only.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 3 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304
Experiment 4 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 5 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	Moderate FOLR1 expression (FOLR1 ++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Gestational choriocarcinoma	JEG-3 cells		CVCL_0363

Experiment 1 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.98%	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of OVCAR-3 cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 5 mg/kg of one of the conjugates listed above or with PBS only.
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					[39]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.50%	Positive CA6 expression (CA6 +++/++)
Method Description	To demonstrate the in vivo activity of the muDS6-DM1 conjugate,human tumor xenografts were established in SCID mice.A subcutaneous model of the human pancreatic cancer cell-line HPAC was developed. The dose was 27.7 mg/kg qw x2.
In Vivo Model	HPAC CDX model
In Vitro Model	Pancreatic adenocarcinoma	HPAC cells		CVCL_3517
Experiment 2 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive CA6 expression (CA6 +++/++)
Method Description	To demonstrate the in vivo activity of the muDS6-DM1 conjugate,human tumor xenografts were established in SCID mice.A subcutaneous model of the human cervical cancer cell-line HeLa was developed. The dose was 27.7 mg/kg qw x2.
In Vivo Model	HeLa CDX model
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030
Experiment 3 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive CA6 expression (CA6 +++/++)
Method Description	To demonstrate the in vivo activity of the muDS6-DM1 conjugate,human tumor xenografts were established in SCID mice.A subcutaneous model of the human ovarian cancer cell-line TOV-21G was developed. The dose was 27.7 mg/kg qw x2.
In Vivo Model	TOV-21G CDX model
In Vitro Model	Ovarian clear cell adenocarcinoma	TOV-21G cells		CVCL_3613
Experiment 4 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive CA6 expression (CA6 +++/++)
Method Description	To demonstrate the in vivo activity of the muDS6-DM1 conjugate,human tumor xenografts were established inSCID mice.A subcutaneous model of the human cervicalcarcinoma cell-line KB was developed. The dose was 27.7 mg/kg qw x2.
In Vivo Model	OVCAR-5 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-5 cells		CVCL_1628
Experiment 5 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive CA6 expression (CA6 +++/++)
Method Description	To demonstrate the in vivo activity of the muDS6-DM1 conjugate,human tumor xenografts were established inSCID mice.A subcutaneous model of the human cervicalcarcinoma cell-line KB was developed. The dose was 250 ug/kg every day for 5 days.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 6 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive CA6 expression (CA6 +++/++)
Method Description	To demonstrate the in vivo activity of the muDS6-DM1 conjugate,human tumor xenografts were established inSCID mice.A subcutaneous model of the human cervicalcarcinoma cell-line KB was developed. The dose was 150 ug/kg every day for 5 days.
In Vivo Model	KB CDX model
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Ductal carcinoma	BT-483 cells		CVCL_2319
Experiment 2 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.45 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Invasive breast carcinoma	ZR-75-1 cells		CVCL_0588
Experiment 3 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.46 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Endocervical adenocarcinoma	WISH cells		CVCL_1909
Experiment 4 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.67 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Endocervical adenocarcinoma	WISH cells		CVCL_1909
Experiment 5 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.8 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	Caov-3 cells		CVCL_0201
Experiment 6 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.4 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 7 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.61 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Ovarian serous adenocarcinoma	Caov-3 cells		CVCL_0201
Experiment 8 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.8 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Pancreatic adenocarcinoma	HPAC cells		CVCL_3517
Experiment 9 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.8 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030
Experiment 10 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.84 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Pancreatic adenocarcinoma	HPAC cells		CVCL_3517
Experiment 11 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Ovarian clear cell adenocarcinoma	TOV-21G cells		CVCL_3613
Experiment 12 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	ZR-75-1 cells		CVCL_0588
Experiment 13 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 14 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-5 cells		CVCL_1628
Experiment 15 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Pancreatic adenocarcinoma	Hs 766T cells		CVCL_0334
Experiment 16 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 17 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	High grade ovarian serous adenocarcinoma	Caov-4 cells		CVCL_0202
Experiment 18 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3 nM	Positive CA6 expression (CA6 +++/++)
Method Description	Clonogenic assays were conducted where cells (1000-2500 cells/well) were plated on6-well plates in 2 ml of conjugate diluted in culture media.The cells were continuously exposed to the conjugate at concentrations,generally between 3x10-11M toseveral 3x10-9 M,and were incubated in a 37°C,6% CO2, humidified chamber for 5-9 days.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma of no special type	BT-20 cells		CVCL_0178
Experiment 19 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.01 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 20 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.88 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Ovarian clear cell adenocarcinoma	TOV-21G cells		CVCL_3613
Experiment 21 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 22 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.4 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Invasive breast carcinoma of no special type	BT-20 cells		CVCL_0178
Experiment 23 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 24 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030
Experiment 25 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	High grade ovarian serous adenocarcinoma	Caov-4 cells		CVCL_0202
Experiment 26 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Ductal carcinoma	BT-483 cells		CVCL_2319
Experiment 27 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	32 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Pancreatic adenocarcinoma	Hs 766T cells		CVCL_0334
Experiment 28 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	846 nM	Positive CA6 expression (CA6 +++/++)
Method Description	In the MTT assay, cells were seeded in 96-well plates ata density of 1000-5000 cells/well. The cells were plated with serial dilutions of either naked muDS6 or muDS6-DM1 immunoconjugate in 200 pl of culture media. The cells and antibody/conjugate mixtures were then incubated for 2-7 d, at which time cellviability was assessed by an MTT assay.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-5 cells		CVCL_1628

Experiment 1 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugates of the exemplary anti-FOLR1 antibodies were tested using an established xenograft model of OVCAR-3 cells implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 10 mg/kg of one of the conjugates listed above or with PBS only.
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					[40]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High CD30 expression (CD30+++)
Method Description	CD30 Karpas-299 cells were either transplanted subcutaneously into NSG, or into CB17.SCID mice. Mice were treated intravenously 3 times weekly with 1 mg/kg preparations, beginning one day post randomization, when the tumors had reached a size ranging between 100 and 150 mm3.
In Vivo Model	Non-Hodgkin's lymphoma CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High CD30 expression (CD30+++)
Method Description	CD30 Karpas-299 cells were either transplanted subcutaneously into NSG, or into CB17.SCID mice. Mice were treated intravenously 3 times weekly with 10 mg/kg ADC preparations, beginning one day post randomization, when the tumors had reached a size ranging between 100 and 150 mm3.
In Vivo Model	Non-Hodgkin's lymphoma CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.7 ng/mL	High CD30 expression (CD30+++)
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	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[41]
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					[41]
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					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Conjugate in various concentrations was added to FOLR1-expressing cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	95 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells		CVCL_2481
Experiment 2 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	55%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 3 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	100%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 4 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	100%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	SKNO-1 cells		CVCL_2196
Experiment 5 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Max inhibition rate (MIR)	100%	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 6 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.02 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Myeloid leukemia with maturation	Kasumi-1 cells		CVCL_0589
Experiment 7 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	0.04 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Gastrointestinal stromal tumor	GIST430 cells		CVCL_7040
Experiment 8 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	1.45 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H1048 cells		CVCL_1453
Experiment 9 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	5.2 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Adult acute myeloid leukemia	SKNO-1 cells		CVCL_2196
Experiment 10 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximum Growth Inhibitory Concentration (GI50)	7.6 nM	Positive KIT expression (KIT+++/++)
Method Description	Cells were cultured in a tissue culture incubator at 37°C with 5% CO2 in culture medium. On the day of the assay, cells were washed twice with PBS, prior to being treated with 0.1% trypsin-EDTA for 5 min and resuspended in the recommended culture medium. Cells were then counted and seeded in 96 well plates at densities of 2,000-10,000 cells/well in 100 ul of cell culture medium.    Click to Show/Hide
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells		CVCL_2481

Experiment 1 Reporting the Activity Date of This ADC					[42]
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					[42]
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					[42]
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					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 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 2 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.54 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 3 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.76 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 1 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 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 2 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.65 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 3 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.65 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 1 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 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 2 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.75 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 3 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.79 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 1 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 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 2 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.77 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 3 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.84 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 1 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	A PEG4-mal-DM4 conjugate in various concentrations was added to FOLR1-expressing KB cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	A PEG4-mal-DM4 conjugate in various concentrations was added to FOLR1-expressing KB cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Cytotoxic IC50 Values (as a Function of [ADC] and [DM1]) for Various M9346A-CX-DM1 ADCs against FR-Expressing KB Cells in the absence of 1 M unconjugated M9346A antibody.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Cytotoxic IC50 Values (as a Function of [ADC] and [DM1]) for Various M9346A-CX-DM1 ADCs against FOLR1-Expressing KB Cells in the presence of 1 M unconjugated M9346A antibody.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Cytotoxic IC50 Values (as a Function of [ADC] and [DM1]) for Various M9346A-CX-DM1 ADCs against FR-Expressing KB Cells in the absence of 1 M unconjugated M9346A antibody.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	Cytotoxic IC50 Values (as a Function of [ADC] and [DM1]) for Various M9346A-CX-DM1 ADCs against FOLR1-Expressing KB Cells in the presence of 1 M unconjugated M9346A antibody.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.21 nM	Positive SEMA4A expression (SEMA4A +++/++)
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	Plasma cell myeloma	MM1.S cells		CVCL_8792
Experiment 2 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.42 nM	Positive SEMA4A expression (SEMA4A +++/++)
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	Plasma cell myeloma	NCI-H929 cells		CVCL_1600
Experiment 3 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.3 nM	Positive SEMA4A expression (SEMA4A +++/++)
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	Plasma cell myeloma	INA-6 cells		CVCL_5209
Experiment 4 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.8 nM	Positive SEMA4A expression (SEMA4A +++/++)
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	Plasma cell myeloma	OCI-My7 cells		CVCL_E333
Experiment 5 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.9 nM	Positive SEMA4A expression (SEMA4A +++/++)
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	Plasma cell myeloma	OCI-My5 cells		CVCL_E332
Experiment 6 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.9 nM	Positive SEMA4A expression (SEMA4A +++/++)
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	Plasma cell myeloma	KMS-12-BM cells		CVCL_1334
Experiment 7 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16.9 nM	Positive SEMA4A expression (SEMA4A +++/++)
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	Multiple myeloma	SK-MM-1 cells		CVCL_A478
Experiment 8 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	35.3 nM	Positive SEMA4A expression (SEMA4A +++/++)
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	Plasma cell myeloma	OPM-2 cells		CVCL_1625
Experiment 9 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	37 nM	Positive SEMA4A expression (SEMA4A +++/++)
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	Plasma cell myeloma	JIM3 cells		CVCL_2533
Experiment 10 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	39.6 nM	Positive SEMA4A expression (SEMA4A +++/++)
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	Plasma cell myeloma	LP-1 cells		CVCL_0012

Experiment 1 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	Cells were seeded in PDL-coated 96 well plates at 375 for MMT/hEGFRvIII, 1500 for U251/hEGFRvIII, 2000 for HEK293/hEGFRvIII, or 3000 for C4-2, PC3, and T47D cells per well in complete growth media and grown overnight.
In Vitro Model	Normal	HEK293 cells		CVCL_0045
Experiment 2 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 nM	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	Cells were seeded in PDL-coated 96 well plates at 375 for MMT/hEGFRvIII, 1500 for U251/hEGFRvIII, 2000 for HEK293/hEGFRvIII, or 3000 for C4-2, PC3, and T47D cells per well in complete growth media and grown overnight.
In Vitro Model	Astrocytoma	U-251MG cells		CVCL_0021
Experiment 3 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10 nM	Positive EGFR vIII expression (EGFR vIII+++/++)
Method Description	Cells were seeded in PDL-coated 96 well plates at 375 for MMT/hEGFRvIII, 1500 for U251/hEGFRvIII, 2000 for HEK293/hEGFRvIII, or 3000 for C4-2, PC3, and T47D cells per well in complete growth media and grown overnight.
In Vitro Model	Malignant neoplasms of the mouse mammary gland	MMT-060562 cells		CVCL_4241

Experiment 1 Reporting the Activity Date of This ADC					[47]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.85 nM	High EGFR expression (EGFR+++/++)
Method Description	HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model	HCC1954/TDR CDX model (CDX: C#19)
In Vitro Model	Breast ductal carcinoma	HCC1954 T-DM1R (T-DM1 resistance) cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[47]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.85 nM	High EGFR expression (EGFR+++/++)
Method Description	HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model	HCC1954/TDR CDX model (CDX: C#10)
In Vitro Model	Breast ductal carcinoma	HCC1954 T-DM1R (T-DM1 resistance) cells		CVCL_1259
Experiment 3 Reporting the Activity Date of This ADC					[47]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.41 nM	High EGFR expression (EGFR+++/++)
Method Description	HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 4 Reporting the Activity Date of This ADC					[47]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.52 nM	High EGFR expression (EGFR+++/++)
Method Description	HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model	HCC1954/TDR CDX model (CDX: C#20)
In Vitro Model	Breast ductal carcinoma	HCC1954 T-DM1R (T-DM1 resistance) cells		CVCL_1259
Experiment 5 Reporting the Activity Date of This ADC					[47]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.68 nM	High EGFR expression (EGFR+++/++)
Method Description	HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model	HCC1954/TDR CDX model (CDX: C#29)
In Vitro Model	Breast ductal carcinoma	HCC1954 T-DM1R (T-DM1 resistance) cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00-10.00 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	A PEG4-mal-DM4 conjugate in various concentrations was added to FOLR1-expressing KB cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium. Antibodies and conjugates were diluted into complete RPMI medium using 3-fold dilution seriesand 100 pL were added per well.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 2 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00-10.00 nM	Positive FOLR1 expression (FOLR1 +++/++)
Method Description	A PEG4-mal-DM4 conjugate in various concentrations was added to FOLR1-expressing KB cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium. Antibodies and conjugates were diluted into complete RPMI medium using 3-fold dilution seriesand 100 pL were added per well.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[48]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 nM	Positive ICAM1 expression (ICAM1+++/++)
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	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC					[48]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.8 nM	Positive ICAM1 expression (ICAM1+++/++)
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	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 3 Reporting the Activity Date of This ADC					[48]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Positive ICAM1 expression (ICAM1+++/++)
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	Normal	hTERT-HPNE cells		CVCL_C466

Experiment 1 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.65 nM	High EGFR expression (EGFR+++)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	89.6 nM	High EGFR expression (EGFR+++)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative EGFR expression (EGFR-)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Moderate EGFR expression (EGFR++)
Method Description	1 x104 cells per well in a volume of 100 ul were plated in 96-well tissue culture plates. After 24 h, ADCs were added at the indicated concentrations. After 72 h, the medium was removed and the viability was determined using the CellTiter-Glo luminescent cell viability assay kit.
In Vitro Model	Invasive breast carcinoma of no special type	BT-20 cells		CVCL_0178

Experiment 1 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	50 nM	Positive polySia expression (polySia +++/++)
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					[51]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative polySia expression (polySia -)
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	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[51]
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					[51]
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					[25]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Positive PLAUR expression (PLAUR +++/++)
Method Description	MDA-MB-231 cells (0.5x104 cells/well) were seeded in 96-well plates at the density and incubated for 120 h (5 days) with of ADCs or IgG. After 5 days of drug treatment at 37°C with 5% CO2.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[40]
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					[40]
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					[52]
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					[52]
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					[53]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100 - 500 ng/mL	Positive GABRP expression (GABRP+++/++)
Method Description	Cells were plated at 2000 cells/well in triplicate in 96-well plates and exposed to GABRP Ab-DM1 ADC and control IgG-DM1 for 3 days.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[53]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100 - 500 ng/mL	Positive GABRP expression (GABRP+++/++)
Method Description	Cells were plated at 2000 cells/well in triplicate in 96-well plates and exposed to GABRP Ab-DM1 ADC and control IgG-DM1 for 3 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[53]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 ng/mL	Positive GABRP expression (GABRP+++/++)
Method Description	Cells were plated at 2000 cells/well in triplicate in 96-well plates and exposed to GABRP Ab-DM1 ADC and control IgG-DM1 for 3 days.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[53]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 ng/mL	Positive GABRP expression (GABRP+++/++)
Method Description	Cells were plated at 2000 cells/well in triplicate in 96-well plates and exposed to GABRP Ab-DM1 ADC and control IgG-DM1 for 3 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 5 Reporting the Activity Date of This ADC					[53]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 ng/mL	Positive GABRP expression (GABRP+++/++)
Method Description	Cells were plated at 2000 cells/well in triplicate in 96-well plates and exposed to GABRP Ab-DM1 ADC and control IgG-DM1 for 3 days.
In Vitro Model	Breast ductal carcinoma	HCC1143 cells		CVCL_1245

Experiment 1 Reporting the Activity Date of This ADC					[54]
Efficacy Data	Tumor Growth lnhibition value (TGl)	< 20%	Positive CD37 expression (CD37+++/++)
Method Description	CD37-positive human diffuse large B-cell lymphoma cell line OCI-LY7 (DSMZ) was subcutaneously inoculated at a dose of 1x107 cells to the right flank region of each five or six-week-old female SCID mouse (Day 0). On Day 10, the mice were randomly grouped. On the day of grouping, the antibodydrug conjugates IMGN529 was intravenously administered at a dose of 3 mg/kg to the tail of each mouse. An antibody-drug conjugate (hmAb-IgG1-DXd) produced using human IgG was administered as a negative control at a dose of 3 mg/kg in the same manner as above. The long diameter and short diameter of the inoculated tumor were measured twice a week using electronic digital calipers, and the volume of the tumor was then calculated.    Click to Show/Hide
In Vivo Model	OCI-LY7 (DSMZ) female SCID mouse model
Experiment 2 Reporting the Activity Date of This ADC					[54]
Efficacy Data	Tumor Growth lnhibition value (TGl)	< 20%	Positive CD37 expression (CD37+++/++)
Method Description	CD37-positive human diffuse large B-cell lymphoma cell line WSU-DLCL2 (DSMZ) was subcutaneously inoculated at a dose of 1x107 cells to the right flank region of each five or six-week-old female SCID mouse (Day 0). On Day 8, the mice were randomly grouped. On the day of grouping, the antibodydrug conjugates IMGN529 was intravenously administered at a dose of 3 mg/kg to the tail of each mouse. An antibody-drug conjugate (hmAb-IgG1-DXd) produced using human IgG was administered as a negative control at a dose of 3 mg/kg in the same manner as above. The long diameter and short diameter of the inoculated tumor were measured twice a week using electronic digital calipers, and the volume of the tumor was then calculated.    Click to Show/Hide
In Vivo Model	WSU-DLCL2 (DSMZ) female SCID mouse model
Experiment 3 Reporting the Activity Date of This ADC					[54]
Efficacy Data	Tumor Growth lnhibition value (TGl)	< 20%	Positive CD37 expression (CD37+++/++)
Method Description	CD37-positive human diffuse large B-cell lymphoma cell line NU-DUL-1 (DSMZ) was subcutaneously inoculated at a dose of 1x107 cells to the right flank region of each five or six-week-old female SCID mouse (Day 0). On Day 14, the mice were randomly grouped. On the day of grouping, the antibodydrug conjugates IMGN529 was intravenously administered at a dose of 3 mg/kg to the tail of each mouse. An antibody-drug conjugate (hmAb-IgG1-DXd) produced using human IgG was administered as a negative control at a dose of 3 mg/kg in the same manner as above. The long diameter and short diameter of the inoculated tumor were measured twice a week using electronic digital calipers, and the volume of the tumor was then calculated.    Click to Show/Hide
In Vivo Model	NU-DUL-1 (DSMZ) female SCID mouse model
Experiment 4 Reporting the Activity Date of This ADC					[54]
Efficacy Data	Tumor Growth lnhibition value (TGl)	≈ 20%	Positive CD37 expression (CD37+++/++)
Method Description	CD37- positive human follicular lymphoma cell line DOHH-2 (DSMZ) was subcutaneously inoculated at a dose of 1x106 cells to the right flank region of each female SCID mouse (Day 0). On Day 21, the mice were randomly grouped. On the day of grouping, IMGN529 was intravenously administered to the tail of each mouse at 3 mg/kg.
In Vivo Model	DOHH-2 (DSMZ) female SCID mouse model
Experiment 5 Reporting the Activity Date of This ADC					[54]
Efficacy Data	Tumor Growth lnhibition value (TGl)	< 30%	Positive CD37 expression (CD37+++/++)
Method Description	CD37-positive human diffuse large B-cell lymphoma cell line SU-DHL-8 (ATCC) was subcutaneously inoculated at a dose of 5x106 cells to the right flank region of each five or six-week-old female SCID mouse (Day 0). On Day 16, the mice were randomly grouped. On the day of grouping, the antibodydrug conjugates IMGN529 was intravenously administered at a dose of 10 mg/kg to the tail of each mouse. An antibody-drug conjugate (hmAb-IgG1-DXd) produced using human IgG was administered as a negative control at a dose of 3 mg/kg in the same manner as above. The long diameter and short diameter of the inoculated tumor were measured twice a week using electronic digital calipers, and the volume of the tumor was then calculated.    Click to Show/Hide
In Vivo Model	SU-DHL-8 (ATCC) female SCID mouse model
Experiment 6 Reporting the Activity Date of This ADC					[54]
Efficacy Data	Tumor Growth lnhibition value (TGl)	< 30%	Positive CD37 expression (CD37+++/++)
Method Description	CD37- positive human chronic lymphocytic leukemia cell line JVM-3 (DSMZ) was subcutaneously inoculated at a dose of 3x106 cells to the right flank region of each female SCID mouse (Day 0). On Day 13, the mice were randomly grouped. On the day of grouping, each antibody-drug conjugate was intravenously administered to the tail of each mouse.
In Vivo Model	JVM-3 (DSMZ) female SCID mouse model

Experiment 1 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Tumor Growth lnhibition value (TGl)	40.91%
Method Description	Cell line-derived xenograft models were established in SCID-17B female mice, by subcutaneous injection of 1x107 (HCC-70) tumor cells, and treatmen with 1mg/kg ADC (single dosee) after tumor volume about 230mm3. Determined tumor volume after the experiment, measured at day 34.
In Vivo Model	HCC70 breast tumor model
Experiment 2 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Tumor Growth Inhibition value (TGI)	42.69%
Method Description	Cell line-derived xenograft models were established in SCID-17B female mice, by subcutaneous injection of 1x107 (HCC-70) tumor cells, and treatmen with 0.5mg/kg ADC (single dosee) after tumor volume about 242mm3. Determined tumor volume after the experiment, measured at day 36.
In Vivo Model	HCC70 breast tumor model

Experiment 1 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.15 nM
Method Description	4000cells/well for HCC-1954 (50 uL) of cells from each cell line were seeded onto 96-well clear bottom black plates. The cells were cultured overnight at 37°C in a humidified 5% CO2 incubator before adding the ADC, The plates were returned to the incubator for 5 days . 50 uL of CellTiter Glo solution was added to each well and incubated atroom temperature with gentle shaking for 10 minutes.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC-1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.8 nM
Method Description	6000 cells/well for HCC-70 (50 uL) of cells from each cell line were seeded onto 96-well clear bottom black plates. The cells were cultured overnight at 37°C in a humidified 5% CO2 incubator before adding the ADC, The plates were returned to the incubator for 5 days . 50 uL of CellTiter Glo solution was added to each well and incubated atroom temperature with gentle shaking for 10 minutes.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC-70 cells		CVCL_1270
Experiment 3 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.14 nM
Method Description	2000 cells/well for NCI-H1650 (50 uL) of cells from each cell line were seeded onto 96-well clear bottom black plates. The cells were cultured overnight at 37°C in a humidified 5% CO2 incubator before adding the ADC, The plates were returned to the incubator for 5 days . 50 uL of CellTiter Glo solution was added to each well and incubated atroom temperature with gentle shaking for 10 minutes.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 4 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10 nM
Method Description	5000cells/well for HT-29 (50 uL) of cells from each cell line were seeded onto 96-well clear bottom black plates. The cells were cultured overnight at 37°C in a humidified 5% CO2 incubator before adding the ADC, The plates were returned to the incubator for 5 days . 50 uL of CellTiter Glo solution was added to each well and incubated atroom temperature with gentle shaking for 10 minutes.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 5 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10 nM
Method Description	800 cells/well for A549 (50 uL) of cells from each cell line were seeded onto 96-well clear bottom black plates. The cells were cultured overnight at 37°C in a humidified 5% CO2 incubator before adding the ADC, The plates were returned to the incubator for 5 days . 50 uL of CellTiter Glo solution was added to each well and incubated atroom temperature with gentle shaking for 10 minutes.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	A549 cells		CVCL_0023
Experiment 6 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10 nM
Method Description	5000 cells/well for MDA-MB-453 (50 uL) of cells from each cell line were seeded onto 96-well clear bottom black plates. The cells were cultured overnight at 37°C in a humidified 5% CO2 incubator before adding the ADC, The plates were returned to the incubator for 5 days . 50 uL of CellTiter Glo solution was added to each well and incubated atroom temperature with gentle shaking for 10 minutes.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 7 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.019 nM
Method Description	For HCC-1954 cells,cells were washed with 100uL,1% BSA1xPBS resuspended in PE conjugated Goatanti-human IgG Fc 1:150 dilutedin 1% BSA1xPBS for 1 hour at 4°C in thedark. Cells were then washed one time as described aboveand resuspended in 1% BSA/1xPBS for 2 hours at 37°C. Supernatants were discarded and 100 uL/wellquench buffer (0.1 M glycine, 0.15 M NaCl, adjust pH to2.5) were added and incubated at 4°C. for 5 min. Cells werethen washed one time as described above and resuspended in Hoechst 33342 1:5000 diluted in DPBS for 15 min at room tem-perature.Afer washed with DPBS one time as described above, cells were resuspended in 4%%PFA and stored at 4°C.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC-1954 cells		CVCL_1259
Experiment 8 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.57 nM
Method Description	For NCI-H1650 cells,cells were washed with 100uL,1% BSA/1xPBS resuspended in Alexa647 conjugatedGoat anti-human IgG Fc 1:500 diluted in 1% BSA/1xPBS for 1 hour at 4°C. inthe dark.Cells were then washed one time as describedabove and resuspended in 1% BSA/1xPBS for 2hours at 37°C. Supernatants were discarded and cells wereresuspended in Hoechst 33342 1:5000diluted in DPBS for 15 min atroom temperature.After washed with DPBS one time as described above,100 uL/well quench buffer (0.1 M glycine, 0.15 M NaCl, adjust pH to2.5)were added and incubated at 4°C.for 5 min. Afterwashing for once with 1% BSA/1xPBS, cellswere resuspended in 4% PFA and stored at 4°C    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483

Experiment 1 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Tumor Growth lnhibition value (TGl)	87.39%
Method Description	When the tumor diameter reached 1.00 cm, qualified cynomolgus monkey liver cancer models were selected and randomly divided into an ADC intravenous injection 0.2 mg kg-1 group (n = 3), an ADC intravenous injection 1.0 mg kg-1 group (n = 3), and a physiological saline control group (n = 2). The ADC was administered once a week for 8 weeks. Tumor volumes were observed by ultrasound scans, and Figure 3C shows representative photos of ultrasound scans before and after the 8-week ADC treatment,0.2 mg/kg.    Click to Show/Hide
In Vivo Model	CRISPR-Mediated Cynomolgus Monkey Liver Cancer Model
Experiment 2 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Tumor Growth lnhibition value (TGl)	91.11%
Method Description	When the tumor diameter reached 1.00 cm, qualified cynomolgus monkey liver cancer models were selected and randomly divided into an ADC intravenous injection 0.2 mg kg-1 group (n = 3), an ADC intravenous injection 1.0 mg kg-1 group (n = 3), and a physiological saline control group (n = 2). The ADC was administered once a week for 8 weeks. Tumor volumes were observed by ultrasound scans, and Figure 3C shows representative photos of ultrasound scans before and after the 8-week ADC treatment,1 mg/kg.    Click to Show/Hide
In Vivo Model	CRISPR-Mediated Cynomolgus Monkey Liver Cancer Model

Experiment 1 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	35.97 nM	High CD147 expression (CD147 +++)
Method Description	Human HCC cell lines HCC-LM3, MHCC97-H, and Huh-7 were seeded in 96-well plates (3000 cells per well). After the cells had adhered to the walls, different concentration gradients of Mehozumab-DM1 diluent, Mehozumab diluent, and IgG were added, and the cells were cultured in a 37 °C incubator under 5% CO2 for 72 h. ThenCCK8 (cat#: C005; Topscience Biology) was used to determine cell viability. Per the manufacturer's instructions, 10 uL of CCK8 reagent was added to each well followed by incubation for 1 h. The absorbance was measured at 450 nm, and used to calculate the corresponding IC50 value using GraphPad Prism v8.0 software (GraphPad Software Inc., San Diego, CA).    Click to Show/Hide
In Vitro Model	Adult hepatocellular carcinoma	HCC-LM3 cells		CVCL_6832
Experiment 2 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	83.07 nM	High CD147 expression (CD147 +++)
Method Description	Human HCC cell lines HCC-LM3, MHCC97-H, and Huh-7 were seeded in 96-well plates (3000 cells per well). After the cells had adhered to the walls, different concentration gradients of Mehozumab-DM1 diluent, Mehozumab diluent, and IgG were added, and the cells were cultured in a 37 °C incubator under 5% CO2 for 72 h. ThenCCK8 (cat#: C005; Topscience Biology) was used to determine cell viability. Per the manufacturer's instructions, 10 uL of CCK8 reagent was added to each well followed by incubation for 1 h. The absorbance was measured at 450 nm, and used to calculate the corresponding IC50 value using GraphPad Prism v8.0 software (GraphPad Software Inc., San Diego, CA).    Click to Show/Hide
In Vitro Model	Adult hepatocellular carcinoma	MHCC97-H cells		CVCL_E3I0
Experiment 3 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	367.1 nM	Moderate CD147 expression (CD147++)
Method Description	Human HCC cell lines HCC-LM3, MHCC97-H, and Huh-7 were seeded in 96-well plates (3000 cells per well). After the cells had adhered to the walls, different concentration gradients of Mehozumab-DM1 diluent, Mehozumab diluent, and IgG were added, and the cells were cultured in a 37 °C incubator under 5% CO2 for 72 h. ThenCCK8 (cat#: C005; Topscience Biology) was used to determine cell viability. Per the manufacturer's instructions, 10 uL of CCK8 reagent was added to each well followed by incubation for 1 h. The absorbance was measured at 450 nm, and used to calculate the corresponding IC50 value using GraphPad Prism v8.0 software (GraphPad Software Inc., San Diego, CA).    Click to Show/Hide
In Vitro Model	Adult hepatocellular carcinoma	Huh-7 cells		CVCL_0336

Experiment 1 Reporting the Activity Date of This ADC					[57]
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					[57]
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					[57]
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					[57]
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					[57]
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					[57]
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					[57]
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					[57]
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					[57]
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					[57]
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					[57]
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					[57]
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					[58]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.163&#1770.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	In vitro cytotoxicity of CovADC-DM1 and CovADC-MMAE was compared to T-DM1 (Kadcyla, Roche, France) on BT-474 and SKBR3 Her2-positive breast cancer cell lines, MDA-MB-231 Her2-negative cell line was included in the assay to confirm target selectivity. All cell lines were obtained from ATCC and cultured in DMEM supplemented with 10% FBS, 100 U/ml penicillin/streptomycin and 2 mM l-glutamine (Life technologies, France). Cells were maintained at 37 °C with 5% CO2 atmosphere. Optimal cell density of each cell lines was determined by IncuCyte S3 live-cell analysis system (Essence BioScience, UK). Cells were plated (SKBR3 and BT-474: 5000 cells per well, MDA-MB-231: 1,250 cells per well) on 96-well plates. Following the incubation for 24 h, cell culture medium was removed and serial dilutions of ADCs and free unconjugated drugs were added in triplicates. After 3 days incubation cytotoxicity was evaluated by sulforhodamine B assay (SRB assay kit, Sigma, France) based on the measurement of cellular protein content according to the manufacturer's instructions. Briefly, cells were fixed with 50% (wt/vol) TriChloroacetic Acid (TCA) at 4 °C (30 ul/well, final concentration 11.5%) for 1 h. After washing with dH2O cells were stained with 100 ul of 0.04% (wt/vol) SRB solution for 30 min and subsequently washed with 1% (vol/vol) acetic acid to remove unbound stain. Cellular protein bound dye was solubilized in 200 ul of 10 mM Tris base solution (pH 10.5) and the absorption was measured at 510 nm (Microplate reader, Tecan, Switzerland). The raw data was processed using GraphPad Prism 7.0 (GraphPad Software, San Diego, USA). Error bars in graphs represent SEM of two measurements.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[58]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.65&#17710.21 nM	Positive HER2 expression (HER2+++/++)
Method Description	In vitro cytotoxicity of CovADC-DM1 and CovADC-MMAE was compared to T-DM1 (Kadcyla, Roche, France) on BT-474 and SKBR3 Her2-positive breast cancer cell lines, MDA-MB-231 Her2-negative cell line was included in the assay to confirm target selectivity. All cell lines were obtained from ATCC and cultured in DMEM supplemented with 10% FBS, 100 U/ml penicillin/streptomycin and 2 mM l-glutamine (Life technologies, France). Cells were maintained at 37 °C with 5% CO2 atmosphere. Optimal cell density of each cell lines was determined by IncuCyte S3 live-cell analysis system (Essence BioScience, UK). Cells were plated (SKBR3 and BT-474: 5000 cells per well, MDA-MB-231: 1,250 cells per well) on 96-well plates. Following the incubation for 24 h, cell culture medium was removed and serial dilutions of ADCs and free unconjugated drugs were added in triplicates. After 3 days incubation cytotoxicity was evaluated by sulforhodamine B assay (SRB assay kit, Sigma, France) based on the measurement of cellular protein content according to the manufacturer's instructions. Briefly, cells were fixed with 50% (wt/vol) TriChloroacetic Acid (TCA) at 4 °C (30 ul/well, final concentration 11.5%) for 1 h. After washing with dH2O cells were stained with 100 ul of 0.04% (wt/vol) SRB solution for 30 min and subsequently washed with 1% (vol/vol) acetic acid to remove unbound stain. Cellular protein bound dye was solubilized in 200 ul of 10 mM Tris base solution (pH 10.5) and the absorption was measured at 510 nm (Microplate reader, Tecan, Switzerland). The raw data was processed using GraphPad Prism 7.0 (GraphPad Software, San Diego, USA). Error bars in graphs represent SEM of two measurements.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[58]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10 nM	Negative HER2 expression (HER2-)
Method Description	In vitro cytotoxicity of CovADC-DM1 and CovADC-MMAE was compared to T-DM1 (Kadcyla, Roche, France) on BT-474 and SKBR3 Her2-positive breast cancer cell lines, MDA-MB-231 Her2-negative cell line was included in the assay to confirm target selectivity. All cell lines were obtained from ATCC and cultured in DMEM supplemented with 10% FBS, 100 U/ml penicillin/streptomycin and 2 mM l-glutamine (Life technologies, France). Cells were maintained at 37 °C with 5% CO2 atmosphere. Optimal cell density of each cell lines was determined by IncuCyte S3 live-cell analysis system (Essence BioScience, UK). Cells were plated (SKBR3 and BT-474: 5000 cells per well, MDA-MB-231: 1,250 cells per well) on 96-well plates. Following the incubation for 24 h, cell culture medium was removed and serial dilutions of ADCs and free unconjugated drugs were added in triplicates. After 3 days incubation cytotoxicity was evaluated by sulforhodamine B assay (SRB assay kit, Sigma, France) based on the measurement of cellular protein content according to the manufacturer's instructions. Briefly, cells were fixed with 50% (wt/vol) TriChloroacetic Acid (TCA) at 4 °C (30 ul/well, final concentration 11.5%) for 1 h. After washing with dH2O cells were stained with 100 ul of 0.04% (wt/vol) SRB solution for 30 min and subsequently washed with 1% (vol/vol) acetic acid to remove unbound stain. Cellular protein bound dye was solubilized in 200 ul of 10 mM Tris base solution (pH 10.5) and the absorption was measured at 510 nm (Microplate reader, Tecan, Switzerland). The raw data was processed using GraphPad Prism 7.0 (GraphPad Software, San Diego, USA). Error bars in graphs represent SEM of two measurements.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.49 nM	Positive TROP2 expression (TROP2+++/++)
Method Description	Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.51 nM	High TROP2 expression (TROP2 +++)
Method Description	Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.54 nM	Moderate TROP2 expression (TROP2++)
Method Description	Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.68 nM	Low TROP2 expression (TROP2+)
Method Description	Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model	Colon adenocarcinoma	Colo205 cells		CVCL_0218
Experiment 5 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.01 nM	High TROP2 expression (TROP2 +++)
Method Description	Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 6 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.88 nM	Positive TROP2 expression (TROP2+++/++)
Method Description	Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.88 nM	Moderate TROP2 expression (TROP2++)
Method Description	Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 8 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	56.42 nM	Low TROP2 expression (TROP2+)
Method Description	Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model	Colon adenocarcinoma	Colo205 cells		CVCL_0218
Experiment 9 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model	Lung adenocarcinoma	A549 cells		CVCL_0023
Experiment 10 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 11 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model	Lung adenocarcinoma	A549 cells		CVCL_0023
Experiment 12 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	Table 3 summarizes the results from in vitro cytotoxicity assays in which ADCs containing various DM1 derivative payload at different DARs were tested.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[60]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	High FRA expression (FRA +++)
Method Description	Use crystal violet analysis to evaluate the in vitro efficacy of the prepared ADCs. Initially screen all MORAb003 ADCs on IGROV1 (FRi (+++)) and SJSA - 1 (FReg (-)) cells.
In Vitro Model	Osteosarcoma	SJSA-1 cells		CVCL_1697

Experiment 1 Reporting the Activity Date of This ADC					[60]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	132 nM	High FRA expression (FRA +++)
Method Description	Use crystal violet analysis to evaluate the in vitro efficacy of the prepared ADCs. Initially screen all MORAb003 ADCs on IGROV1 (FRi (+++)) and SJSA - 1 (FReg (-)) cells.
In Vitro Model	Osteosarcoma	SJSA-1 cells		CVCL_1697

Experiment 1 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	30 ng/ml
Method Description	The cytotoxicity of ADC against cell lines was evaluated by cell viability test with CellTiter-Glo 2.0 luminescence method.

Experiment 1 Reporting the Activity Date of This ADC					[62]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	237 ng/mL	Negative EDB expression (EDB-)
Method Description	Calculated using four-parameter logistic model #203 with XLfit v4.2 (IDBS)
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 2 Reporting the Activity Date of This ADC					[62]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	268 ng/mL	Positive EDB expression (EDB+++/++)
Method Description	Calculated using four-parameter logistic model #203 with XLfit v4.2 (IDBS)
In Vitro Model	Normal	WI38-VA13 cells		CVCL_2759

Experiment 1 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	240 ng/ml
Method Description	The cytotoxicity of ADC against cell lines was evaluated by cell viability test with CellTiter-Glo 2.0 luminescence method.

Experiment 1 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	311 ng/ml
Method Description	The cytotoxicity of ADC against cell lines was evaluated by cell viability test with CellTiter-Glo 2.0 luminescence method.

Experiment 1 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2378 ng/ml
Method Description	The cytotoxicity of ADC against cell lines was evaluated by cell viability test with CellTiter-Glo 2.0 luminescence method.
Experiment 2 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4928 ng/ml
Method Description	The cytotoxicity of ADC against cell lines was evaluated by cell viability test with CellTiter-Glo 2.0 luminescence method.

Experiment 1 Reporting the Activity Date of This ADC					[63]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	7996 ng/mL	Negative CD138 expression (CD138-)
Method Description	1000 cells/well of Jurkat in 96 well, 37 °C for 5 days.
In Vitro Model	T acute lymphoblastic leukemia	Jurkat cells		CVCL_0065
Experiment 2 Reporting the Activity Date of This ADC					[63]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	8385 ng/mL	Positive CD138 expression (CD138+++/++)
Method Description	1000 cells/well of Capan-1 in 96 well, 37 °C for 5 days.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237

Experiment 1 Reporting the Activity Date of This ADC					[64]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.90%	High CD205 expression (CD205+++; IHC 3+)
Method Description	The antitumor activity of the ADCs was then evaluated in solid and hematologic mouse xenograft models. A total of 5x106-2x107 cells with or without Matrigel, were injected subcutaneously into the flanks of mice. The treatments were started when average tumor volume reached 88-300 mm3. Animals were randomly assigned into groups (6 mice/group), and treated with MEN1309/OBT076 intravenously once weekly for 2 consecutive weeks, 10 mg/kg.    Click to Show/Hide
In Vivo Model	Diffuse Large B-Cell Lymphoma CDX model
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511
Experiment 2 Reporting the Activity Date of This ADC					[64]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.10%	High CD205 expression (CD205+++; IHC 3+)
Method Description	The antitumor activity of the ADCs was then evaluated in solid and hematologic mouse xenograft models. A total of 5x106-2x107 cells with or without Matrigel, were injected subcutaneously into the flanks of mice. The treatments were started when average tumor volume reached 88-300 mm3. Animals were randomly assigned into groups (6 mice/group), and treated with MEN1309/OBT076 intravenously with a single dose, 10 mg/kg.    Click to Show/Hide
In Vivo Model	Pancreas cancer CDX model
In Vitro Model	Pancreatic cancer	Pancreatic cancer cells		Homo sapiens