Antibody ID	ANI0XJJLY
Antibody Name	Pertuzumab
Brand Name	PERJETA
Organization	Genentech, Inc.; Roche Holding AG
Indication	Ovarian cancer; Gastric cancer; Breast cancer; Prostate cancer
Approval Date	Jun. 2012
Synonyms	rhuMAB 2C4; PERTUZUMAB-ZZXF; RG-1273; RHUMAB 2C4; RHUMAB-2C4    Click to Show/Hide
Antibody Type	Monoclonal antibody (mAb)
Antibody Subtype	Humanized IgG1-kappa
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)					Antigen Info
ChEMBI ID	CHEMBL2007641
PDB ID	1l7i , 1s78 , 4llu , 4llw , 4lly
DrugBank ID	DB06366
Drug Central ID	4957
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence	EVQLVESGGGLVQPGGSLRLSCAASGFTFTDYTMDWVRQAPGKGLEWVADVNPNSGGSIY NQRFKGRFTLSVDRSKNTLYLQMNSLRAEDTAVYYCARNLGPSFYFDYWGQGTLVTVSSA STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTHTCPPCPAPELLGGP SVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNS TYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSREEM TKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQ QGNVFSCSVMHEALHNHYTQKSLSLSPGK     Click to Show/Hide
Heavy Chain Varible Domain	EVQLVESGGGLVQPGGSLRLSCAASGFTFTDYTMDWVRQAPGKGLEWVADVNPNSGGSIY NQRFKGRFTLSVDRSKNTLYLQMNSLRAEDTAVYYCARNLGPSFYFDYWGQGTLVTVSS     Click to Show/Hide
Heavy Chain Constant Domain 1	ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKKVEPKSCDKTH     Click to Show/Hide
Heavy Chain CDR 1	GFTFTDYT     Click to Show/Hide
Heavy Chain CDR 2	VNPNSGGS     Click to Show/Hide
Heavy Chain CDR 3	ARNLGPSFYFDY     Click to Show/Hide
Light Chain Sequence	DIQMTQSPSSLSASVGDRVTITCKASQDVSIGVAWYQQKPGKAPKLLIYSASYRYTGVPS RFSGSGSGTDFTLTISSLQPEDFATYYCQQYYIYPYTFGQGTKVEIKRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC     Click to Show/Hide
Light Chain Varible Domain	DIQMTQSPSSLSASVGDRVTITCKASQDVSIGVAWYQQKPGKAPKLLIYSASYRYTGVPS RFSGSGSGTDFTLTISSLQPEDFATYYCQQYYIYPYTFGQGTKVEIK     Click to Show/Hide
Light Chain Constant Domain	RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQD SKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC     Click to Show/Hide
Light Chain CDR 1	QDVSIG     Click to Show/Hide
Light Chain CDR 2	SAS     Click to Show/Hide
Light Chain CDR 3	QQYYIYPYT     Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[1]
Patients Enrolled	Eligible participants must have HER2+ advanced solid tumors refractory to standard therapy, ≥1 measurable lesion (RECIST v1.1), ECOG PS 0-1, adequate organ function, and contraceptive use. Key exclusions: CNS metastases, active lung/autoimmune diseases, severe allergies, uncontrolled cardiac conditions, concurrent malignancies (5-year window), or bleeding disorders.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT05819684	Clinical Status	PHASE1
Clinical Description	A Phase I Multi-Center, Open-Label Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Efficacy of SHR-4602 in HER2 Expressing or Mutated Advanced Malignant Solid Tumor Subjects
Primary Endpoint	The primary safety endpoints include adverse event (AE) incidence/severity (monitored until 90 days post-treatment), maximum tolerated dose (MTD), dose-limiting toxicities (DLTs) within 21 days post-dose, and recommended Phase 2 dose (RP2D) determination.
Other Endpoint	Pharmacokinetic analysis (Cmax, AUC0-t, Tmax, T1/2) and immunogenicity (anti-drug antibodies, ADAs) will be assessed up to 30-90 days post-treatment. Efficacy endpoints (per RECIST v1.1) include objective response rate (ORR), disease control rate (DCR), duration of response (DOR), and progression-free survival (PFS).
Experiment 2 Reporting the Activity Date of This ADC					[2]
Patients Enrolled	Eligible participants (age 18-75, ECOG PS 0-1) must have HER2-positive disease confirmed via tissue testing, ≥1 measurable lesion (RECIST v1.1), and adequate organ function, with stringent contraception requirements. Exclusions include active brain/CNS metastases, untreated interstitial lung disease, uncontrolled infections/cardiovascular conditions, prior therapies within 4 weeks, unresolved toxicities (>Grade 1), concurrent malignancies (5-year window), and severe allergies to SHR-4602 components.    Click to Show/Hide
Administration Dosage	Intravenous infusion, cycle every 21 days;
Related Clinical Trial
NCT Number	NCT06516926	Clinical Status	PHASE2
Clinical Description	An Open-label, Randomized, Multi-center Phase II Clinical Study of SHR-4602 for Injection in Subjects With HER2-expressing or -Mutated Unresectable or Metastatic Solid Tumors
Primary Endpoint	The primary endpoint is the objective response rate (ORR) assessed over a two-year period, evaluating treatment efficacy based on tumor response criteria.
Other Endpoint	Secondary endpoints include duration of response (DoR), progression-free survival (PFS), best overall response (BOR), disease control rate (DCR), incidence and severity of adverse events (AEs/SAEs) graded per CTCAE v5.0, and pharmacokinetic parameters (blood concentrations of conjugated/total antibodies and free toxin), all monitored over two years.    Click to Show/Hide
Experiment 3 Reporting the Activity Date of This ADC					[3]
Patients Enrolled	Eligible participants (ECOG PS 0-1, HER2+ advanced solid tumors, life expectancy ≥12 weeks) must have adequate organ function and provide consent. Key exclusions: active brain metastases, recent anticancer therapies (4 weeks), unresolved toxicities (Grade>1), uncontrolled infections, bleeding disorders, active hepatitis B/C, other malignancies (5-year window), or SHR-4602 hypersensitivity.    Click to Show/Hide
Administration Dosage	Experimental: SHR-4602 Dose level 1 : 2.0 mg/kg, Dose level 2 : 2.5mg/kg
Related Clinical Trial
NCT Number	NCT06560138	Clinical Status	PHASE1
Clinical Description	An Open-label, Multi-center Phase I Dose-expansion Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Efficacy of SHR-4602 in Subjects With HER2-expressing or HER2-mutated Locally Advanced or Metastatic Solid Tumors
Primary Endpoint	The recommended Phase II dose (RP2D) of SHR-4602 will be determined based on observed clinical responses and tolerability, assessed from informed consent until 45 (±3) days post-treatment or new anti-tumor therapy initiation (up to 1 year).
Other Endpoint	PK parameters (Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, CL, Vss, Rac) and immunogenicity (ADA) will be evaluated over 1 year post-treatment. Efficacy endpoints (ORR, DOR, DCR, PFS) will be assessed per RECIST v1.1 for up to 3 years, with responses confirmed ≥4 weeks later and Kaplan-Meier analysis for time-to-event outcomes.
Experiment 4 Reporting the Activity Date of This ADC					[4]
Patients Enrolled	Additional exclusion criteria involve untreated hepatitis, recent live vaccines (28 days), known allergies to study drug components, uncontrolled mental illness, substance abuse, other malignancies within 5 years, active tuberculosis, or any condition deemed to compromise study integrity by investigators. Requirements include consent provision and commitment to contraception until 8 months post-treatment.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT06704828	Clinical Status	PHASE2
Clinical Description	An Open-label, Multi-center Phase II Study to Evaluate the Safety, Tolerablity, Pharmacokinetics, and Efficacy of SHR-4602 as Montherapy or in Combination With Other Anti-tumor Therapies in Sujbects With Advanced Solid Tumors
Primary Endpoint	The primary endpoint is ORR by investigator assessment, defined as the percentage of participants achieving confirmed CR or PR per RECIST v1.1, evaluated over approximately 5 years. Secondary endpoints include DCR (CR+PR+SD), DoR (time from first response to PD/death), PFS (time from treatment start to PD/death), OS (time to death from any cause), and incidence of AEs.    Click to Show/Hide
Other Endpoint	Eligible participants aged 18-80 with ECOG 0-1 must have confirmed advanced/metastatic solid tumors after ≥1 line of prior therapy, measurable lesions per RECIST v1.1, expected survival ≥12 weeks, adequate organ function, and HER2 expression (Stage I). Key exclusions include active CNS metastases, recent anticancer therapy (within 4 weeks), unresolved toxicities > Grade 1, significant lung/cardiac diseases, active infections/autoimmune disorders, pregnancy/lactation, and prior severe immune-related AEs from checkpoint inhibitors.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[5]
Patients Enrolled	Eligible participants had HER2-positive (IHC 2+/3+ or amplified) advanced/metastatic tumors (breast, CRC, gastric, NSCLC) with measurable disease per RECIST v1.1, plus archived/fresh biopsy and adequate organ function. Exclusions included active brain metastases, uncontrolled ILD/pneumonitis, certain autoimmune diseases, strong CYP2C/CYP3A-interacting medications, or untreated hepatitis/HIV.    Click to Show/Hide
Administration Dosage	Dose range of 0.45 to 0.6 mg/kg by subcutaneous (SC) injection in 21-day cycles
Related Clinical Trial
NCT Number	NCT05091528	Clinical Status	PHASE1|||PHASE2
Clinical Description	An Open-label, Phase 1/2, Dose-escalation and Expansion Study of SBT6050 Combined With Other HER2-directed Therapies in Subjects With Pretreated Unresectable Locally Advanced and/or Metastatic HER2-expressing or HER2-amplified Cancers
Primary Endpoint	The study evaluated dose-limiting toxicities (DLTs) within 21 days in escalation cohorts, along with treatment-emergent adverse events (TEAEs) and lab abnormalities graded by NCI CTCAE v5.0 over 18 weeks. Objective response rate (ORR) by RECIST v1.1 was assessed in expansion cohorts at baseline.
Other Endpoint	Safety data (TEAEs severity) were collected in expansion cohorts at baseline, while ORR was tracked in escalation cohorts over 18 weeks. Duration of response (DoR) and clinical benefit rate (CBR) were monitored for all participants using RECIST v1.1 criteria, with CBR specifically applied to expansion cohorts.
Experiment 2 Reporting the Activity Date of This ADC					[6]
Patients Enrolled	Eligible patients had HER2+ advanced tumors, prior treatment exposure, measurable disease per RECIST 1.1, and adequate organ function; exclusions included active infections, autoimmune diseases, untreated CNS metastases, or hypersensitivity to drug components.
Administration Dosage	Escalating doses of SBT6050 in Part 1 and recommended dose in Part 2
Related Clinical Trial
NCT Number	NCT04460456	Clinical Status	PHASE1
Clinical Description	A Phase 1/1B, Open-Label, Dose Escalation and Expansion Study of SBT6050 Alone and in Combination With PD-1 Inhibitors in Subjects With Advanced Solid Tumors Expressing HER2
Primary Endpoint	The study evaluated dose-limiting toxicities within 28 days (Parts 1/3), adverse event incidence/severity (all parts) over 2 years, and objective response/duration (Parts 2/4/5) across the 2-year timeframe.
Other Endpoint	Assessments included response rates/duration (Parts 1/3), disease control (all parts), pharmacokinetic parameters (Cmax, AUC), immunogenicity (Parts 1/2), and progression-free survival (Parts 2/4/5) with 2-year follow-up.
Experiment 3 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Objective Response Rate (ORR)	7.10%
Patients Enrolled	Patients have HER2-expressing or amplified solid tumors.
Administration Dosage	0.60 mg/kg administered Q2 weeks.
Related Clinical Trial
NCT Number	NCT04460456	Clinical Status	Phase 1
Clinical Description	A phase 1/1b, open-label, dose escalation and expansion study of SBT6050 alone and in combination with PD-1 inhibitors in subjects with advanced solid tumors expressing HER2.
Experiment 4 Reporting the Activity Date of This ADC					[8]
Related Clinical Trial
NCT Number	NCT05091528	Clinical Status	Phase 1
Clinical Description	An open-label, phase 1/2, dose-escalation and expansion study of SBT6050 combined with other HER2-directed therapies in subjects with pretreated unresectable locally advanced and/or metastatic HER2-expressing or HER2-amplified cancers.

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	High HER2 expression (HER2+++)
Method Description	BT474 human breast carcinomas fragments were implanted subcutaneously in theright flank of the mice. Mice were divided into 4 treatment groups (N=8/group), as follows: trastuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); rituximab-Compound (la) conjugate (5 mg/kg, iv, qd x 1); pertuzumab-Compound (la) conjugate (5 mg/kg, iv, qd x 1).
In Vivo Model	BT-474 CDX model
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 67%	Positive HER2 expression (HER2 +++/++)
Method Description	Mice were orthotopically implanted with 1x107 HCC1569 human breast cancer cells suspended in amixture of Matrigel and culture media in the inguinal fat pad. Following group allocation, mice were treated with a single 10 ml/kg lateral tail vein injection of a Pertuzumab-Compound (la) conjugate at 3 mg/kg.
In Vivo Model	HCC1569 CDX model
In Vitro Model	Breast ductal carcinoma	HCC1569 cells		CVCL_1255
Experiment 3 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95%	Positive HER2 expression (HER2 +++/++)
Method Description	Mice were orthotopically implanted with 1x107 HCC1569 human breast cancer cells suspended in amixture of Matrigel and culture media in the inguinal fat pad. Following group allocation, mice were treated with a single 10 ml/kg lateral tail vein injection of a Pertuzumab-Compound (la) conjugate at 10 mg/kg.
In Vivo Model	HCC1569 CDX model
In Vitro Model	Breast ductal carcinoma	HCC1569 cells		CVCL_1255

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.19 pM	High HER2 expression (HER2+++)
Method Description	The cells, at a predetermined concentration, were plated into 96 well plates, and, after overnight incubation at 37°C/5% CO2, serial dilutions of each test article (TA) were added to the cells. Cells were incubated with test articles for 72 hours. and viability was detected with CellTiter-Gloreagent.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM
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	Adult hepatocellular carcinoma	SNU-182 cells		CVCL_0090
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.20%	Positive HER2 expression (HER2 +++/++)
Method Description	Mice were orthotopically implanted with 1x107 HCC1569 human breast cancer cells suspended in amixture of Matrigel and culture media in the inguinal fat pad. Following group allocation, mice were treated with a single 10 ml/kg lateral tail vein injection of a Pertuzumab-Compound (XI) conjugate at 3 mg/kg.
In Vivo Model	HCC1569 CDX model
In Vitro Model	Breast ductal carcinoma	HCC1569 cells		CVCL_1255
Experiment 2 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 71.40%	Positive HER2 expression (HER2 +++/++)
Method Description	Mice were orthotopically implanted with 1x107 HCC1569 human breast cancer cells suspended in amixture of Matrigel and culture media in the inguinal fat pad. Following group allocation, mice were treated with a single 10 ml/kg lateral tail vein injection of a Pertuzumab-Compound (XI) conjugate at 10 mg/kg.
In Vivo Model	HCC1569 CDX model
In Vitro Model	Breast ductal carcinoma	HCC1569 cells		CVCL_1255

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.56 pM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 1.5 pM	High HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	57 pM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM
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 carcinoma	ZR-75-30 cells		CVCL_1661
Experiment 5 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Gastric carcinoma	NCC-StC-K140 cells		CVCL_3055
Experiment 6 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM	High HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 7 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	< 0.58 nM
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast ductal carcinoma	HCC202 cells		CVCL_2062
Experiment 8 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.82 nM
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 of no special type	UACC-812 cells		CVCL_1781
Experiment 9 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.86 nM
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-361 cells		CVCL_0620
Experiment 10 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.99 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 11 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.11 nM
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast ductal carcinoma	HCC1419 cells		CVCL_1251
Experiment 12 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.2 nM
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 carcinoma	MDA-MB-175-VII cells		CVCL_1400
Experiment 13 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.2 nM
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast ductal carcinoma	HCC2218 cells		CVCL_1263
Experiment 14 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.69 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	AU565 cells		CVCL_1074
Experiment 15 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.59 nM	Moderate HER2 expression (HER2++; IHC 2+)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Gastric signet ring cell adenocarcinoma	NUGC-4 cells		CVCL_3082
Experiment 16 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.4 nM
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast ductal carcinoma	HCC2157 cells		CVCL_1261
Experiment 17 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.72 pM	High HER2 expression (HER2+++)
Method Description	The cells, at a predetermined concentration, were plated into 96 well plates, and, after overnight incubation at 37°C/5% CO2, serial dilutions of each test article (TA) were added to the cells. Cells were incubated with test articles for 72 hours. and viability was detected with CellTiter-Gloreagent.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.01 pM	High HER2 expression (HER2+++)
Method Description	The cells, at a predetermined concentration, were plated into 96 well plates, and, after overnight incubation at 37°C/5% CO2, serial dilutions of each test article (TA) were added to the cells. Cells were incubated with test articles for 72 hours. and viability was detected with CellTiter-Gloreagent.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.5 pM	High HER2 expression (HER2+++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.26 pM	High HER2 expression (HER2+++)
Method Description	The cells, at a predetermined concentration, were plated into 96 well plates, and, after overnight incubation at 37°C/5% CO2, serial dilutions of each test article (TA) were added to the cells. Cells were incubated with test articles for 72 hours. and viability was detected with CellTiter-Gloreagent.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.51 pM	High HER2 expression (HER2+++)
Method Description	The cells, at a predetermined concentration, were plated into 96 well plates, and, after overnight incubation at 37°C/5% CO2, serial dilutions of each test article (TA) were added to the cells. Cells were incubated with test articles for 72 hours. and viability was detected with CellTiter-Gloreagent.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.95 nM	Positive HER2 expression (HER2 +++)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Negative HER2 expression (HER2 -)
Method Description	Cells were plated at about 500 cells per well in a 96-well plate in 100 uL of media. In vitro activity and targeted delivery of ADCs, the isotype-matched negative controls ADCs, and naked antibodies control were assessed in cells.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0001949 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to BT-474 cells
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.03135 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.6134 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to NCI-N87 cells
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	7.838 nM	Low HER2 expression (HER2+)
Method Description	Cytotoxicity of ADC to T47D cells
In Vitro Model	Invasive breast carcinoma of no special type	T47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.003748 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to BT-474 cells
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01296 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.175 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of ADC to NCI-N87 cells
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.02 nM	Low HER2 expression (HER2+)
Method Description	Cytotoxicity of ADC to T47D cells
In Vitro Model	Invasive breast carcinoma of no special type	T47D cells		CVCL_0553

Ref 1	A Study of SHR-4602 in Subjects With Advanced Malignant Solid Tumors
Ref 2	SHR-4602 for Injection in Subjects With HER2-expressing or -Mutated Unresectable or Metastatic Solid Tumors
Ref 3	A Trial of SHR-4602 Infusion in Patients With SHR-4602 in Subjects With HER2-expressing or HER2-mutated Locally Advanced or Metastatic Solid Tumors
Ref 4	A Phase II Study of SHR-4602 as Montherapy or in Combination With Other Anti-tumor Therapies in Advanced Solid Tumors
Ref 5	A Safety and Activity Study of SBT6050 in Combination With Other HER2-directed Therapies for HER2-positive Cancers
Ref 6	A Study of SBT6050 Alone and in Combination With PD-1 Inhibitors in Subjects With Advanced HER2 Expressing Solid Tumors
Ref 7	A Phase I Pharmacokinetic (PK) and Safety Study of Trph-222 in Patients with Relapsed/Refractory B-Cell Non-Hodgkin Lymphoma (R/R NHL): Dose-Escalation Results. 2020 Dec 7.
Ref 8	An Open-label, Phase 1/2, Dose-escalation and Expansion Study of SBT6050 Combined With Other HER2-directed Therapies in Subjects With Pretreated Unresectable Locally Advanced and/or Metastatic HER2-expressing or HER2-amplified Cancers, NCT05091528
Ref 9	Neodegrader conjugates; 2021-10-07.
Ref 10	Linkers for use in antibody drug conjugates; 2023-03-16.
Ref 11	Ligand-drug conjugate of exatecan analogue, preparation method therefor and application thereof; 2020-04-02.
Ref 12	Domide molecular glue derivative and use thereof