Payload ID	PAY0FSXOW
Name	Monomethyl auristatin E
Synonyms	Monomethyl auristatin E; 474645-27-7; MMAE; Monomethylauristatin E; MMAE (Monomethyl auristatin E); V7I58RC5EJ; SGD-1010; (2S)-N-[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]-3-methyl-2-(methylamino)butanamide; N-Methyl-L-valyl-N-((1S,2R)-4-((2S)-2-((1R,2R)-3-(((1R,2S)-2-hydroxy-1-methyl-2-phenylethyl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-2-methoxy-1-((1S)-1-methylpropyl)-4-oxobutyl)-N-methyl-L-valinamide; MMAE peptide; N-methyl-L-valyl-N-[(3R,4S,5S)-1-{(2S)-2-[(1R,2R)-3-{[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino}-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl}-3-methoxy-5-methyl-1-oxoheptan-4-yl]-N-methyl-L-valinamide; UNII-V7I58RC5EJ; Monomethyl auristatin E (MMAE); MFCD22124498; 4Q5; MMAE, monomethyl auristatin E; SCHEMBL5402144; CHEMBL2103835; AMY9235; DTXSID101028844; MONOMETHYLAURISTATIN E [MI]; (S)-N-((3R,4S,5S)-1-((S)-2-((1R,2R)-3-(((1R,2R)-1-Hydroxy-1-phenylpropan-2-yl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-3-methoxy-5-methyl-1-oxohe; n-methyl-l-valyl-n-[(1s,2r)-4-[(2s)-2-[(1r,2r)-3-[[(1r,2s)-2-hydroxy-1-methyl-2-phenylethyl]amino]-1-methoxy-2-methyl-3-oxopropyl]-1-pyrrolidinyl]-2-methoxy-1-[(1S)-1-methylpropyl]-4-oxobutyl]-n-methyl-l-valinamide; FD9056; NSC791792; NSC832263; s7721; CCG-270400; CS-0837; NSC-791792; NSC-832263; BP-22278; HY-15162; Q6901739; (S)-N-((3R,4S,5S)-1-((S)-2-((1R,2R)-3-(((1S,2R)-1-Hydroxy-1-phenylpropan-2-yl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-3-methoxy-5-methyl-1-oxoheptan-4-yl)-N,3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamide; L-Valinamide, N-methyl-L-valyl-N-((1S,2R)-4-((2S)-2-((1R,2R)-3-(((1R,2S)-2-hydroxy-1- methyl-2-phenylethyl)amino)-1-methoxy-2-methyl-3-oxopropyl)-1-pyrrolidinyl)-2- methoxy-1-((1S)-1-methylpropyl)-4-oxobutyl)-N-methyl-; N(sup 2)-(N-Methyl-L-valyl)-N(sup 1)-((1S,2R)-4-((2S)-2-((1R,2R)-3-(((1R,2S)-2-hydroxy-1-methyl-2- phenylethyl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-2-methoxy-1-((1S)- 1-methylpropyl)-4-oxobutyl)-N(sup 1)-methyl-L-valinamide    Click to Show/Hide
Target	Microtubule (MT)					Target Info
Structure
	3D MOL			2D MOL
Formula	C39H67N5O7
Isosmiles	CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@@H]([C@@H](C)C(=O)N[C@H](C)[C@H](C2=CC=CC=C2)O)OC)OC)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](C(C)C)NC
PubChem CID	11542188
InChI	InChI=1S/C39H67N5O7/c1-13-25(6)34(43(10)39(49)33(24(4)5)42-38(48)32(40-9)23(2)3)30(50-11)22-31(45)44-21-17-20-29(44)36(51-12)26(7)37(47)41-27(8)35(46)28-18-15-14-16-19-28/h14-16,18-19,23-27,29-30,32-36,40,46H,13,17,20-22H2,1-12H3,(H,41,47)(H,42,48)/t25-,26+,27+,29-,30+,32-,33-,34-,35+,36+/m0/s1
InChIKey	DASWEROEPLKSEI-UIJRFTGLSA-N
IUPAC Name	(2S)-N-[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]-3-methyl-2-(methylamino)butanamide
Pharmaceutical Properties	Molecule Weight		718	Polar area		150
	Complexity		1100	xlogp Value		4.1
	Heavy Count		51	Rot Bonds		20
	Hbond acc		8	Hbond Donor		4

Standard Type	Value	Units	Cell line	Disease Model	Cell line ID	Reference
Half Maximal Inhibitory Concentration (IC50)	0.13±0.02	nM	MDA-MB-231 cells	Breast adenocarcinoma	CVCL_0062	[1], [2]
Half Maximal Inhibitory Concentration (IC50)	0.25	nM	Granta-519 cells	Mantle cell lymphoma	CVCL_1818	[1], [2]
Half Maximal Inhibitory Concentration (IC50)	0.25	nM	SU-DHL-4 cells	Diffuse large B-cell lymphoma	CVCL_0539	[1], [2]
Half Maximal Inhibitory Concentration (IC50)	0.54	nM	BJAB cells	Burkitt lymphoma	CVCL_5711	[1], [2]
Half Maximal Inhibitory Concentration (IC50)	0.66±0.06	nM	MDA-MB-468 cells	Breast adenocarcinoma	CVCL_0419	[1], [2]
Half Maximal Inhibitory Concentration (IC50)	1.19	nM	SU-DHL-4 cells	Diffuse large B-cell lymphoma	CVCL_0539	[1], [2]

Experiment 1 Reporting the Activity Date of This ADC					[3]
Patients Enrolled	Inclusion criteria include: age ≥18, life expectancy ≥6 months, informed consent, measurable disease by RECIST v1.1, ECOG 0-1, and adequate organ function. Part B requires Tissue Factor (TF)-positive tumors via IHC. Exclusions involve: TF-negative tumors (Part B), unresolved toxicities (>Grade 1), active CNS metastases, recent anticancer therapy (≤21 days), bleeding/cardiac risks, uncontrolled infections, pregnancy, HIV/hepatitis, strong CYP3A4 modifiers use, or conditions deemed unsafe by investigators. Prior radiotherapy toxicities must resolve to Grade ≤1.    Click to Show/Hide
Administration Dosage	All patients in Part A (dose escalation) and Part B (dose expansion) will be administrated MRG004A on Day 1 of every 3 weeks (21-day cycle).
Related Clinical Trial
NCT Number	NCT04843709	Phase Status	PHASE1|||PHASE2
Clinical Description	An Open-Label, Multi-center, Phase I/II Dose Escalation and Expansion Study to Assess the Safety, Tolerability, Anti-Tumor Activity and Pharmacokinetics of MRG004A in Patients With Tissue Factor Positive Advanced or Metastatic Solid Tumors
Primary Endpoint	The primary endpoints for this study include determining the Maximum Tolerated Dose (MTD) (assessed within the first 21-day treatment cycle) as the highest dose where <33% of patients experience Dose-Limiting Toxicity (DLT), and establishing the Recommended Phase II Dose (RP2D) based on safety, efficacy, and PK data (evaluated over 24 months). Additional metrics are Objective Response Rate (ORR) (CR+PR rate by Independent Central Review) and Adverse Events (AEs) (recorded from informed consent until 45 days post-last dose), covering all trial-related side effects regardless of causality.    Click to Show/Hide
Other Endpoint	Key secondary outcomes encompass efficacy measures: Duration of Response (DoR) (time from initial response to progression/death), Disease Control Rate (DCR) (CR+PR+SD≥6 weeks), Progression-Free Survival (PFS) (time to progression/death), and Overall Survival (OS) (time to death from any cause), all tracked for up to 24 months. Pharmacokinetic parameters (Cmax, Tmax, AUClast) and Anti-Drug Antibody (ADA) incidence are evaluated from baseline to 30 days post-treatment.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[4]
Patients Enrolled	Eligible patients (ECOG 0-1) must have specified metastatic solid tumors and measurable disease, with adequate contraception required. Key exclusions include prior CD47/SIRPalpha therapy, active CNS metastases, HIV/hepatitis infections, recent transfusions or immunosuppression, and cardiovascular events within 6 months. Life expectancy must exceed 12 weeks.    Click to Show/Hide
Related Clinical Trial
NCT Number	NCT03957096	Phase Status	PHASE1
Clinical Description	A Phase 1 Study of SGN-CD47M in Patients With Advanced Solid Tumors
Primary Endpoint	The study will assess safety parameters including adverse events and laboratory abnormalities over 24 months, with dose-limiting toxicities evaluated specifically within the first 28 days of treatment.
Other Endpoint	Efficacy evaluations will include ORR, DOR, PFS and OS according to both RECIST v1.1 and iRECIST criteria, with assessments continuing for up to 4 years. Pharmacokinetic measurements (AUC, Cmax, Tmax, Ctrough) and immunogenicity (ADA) will be monitored for 24 months.

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 42.13%	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg) via the tail vein on Day 0.
In Vivo Model	Gastric cancer PDX model (PDX: GA0045)

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with MKN-45 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg) via the tail vein on Day 0.
In Vivo Model	MKN-45 CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.53%	High LSR expression (LSR+++; 89,382.9 LSR expression (ABC/cell))
Method Description	The model was Ovx6 PDX,which was generated by implanting human tumor tissues expressing LSR at high levels. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (1 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model	Ovarian cancer PDX model (PDX: Ovx6)
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55.47%	High LSR expression (LSR+++; 89,382.9 LSR expression (ABC/cell))
Method Description	The model was Ovx6 PDX,which was generated by implanting human tumor tissues expressing LSR at high levels. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (3 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model	Ovarian cancer PDX model (PDX: Ovx6)
Experiment 3 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 67.50%	High LSR expression (LSR+++; 89,382.9 LSR expression (ABC/cell))
Method Description	To assess the efficacy of LSR-ADC against omental/bowel metastasis,OVCAR3-Luc xenograft models were used. The OVCAR3-Luc xenograft models was established by implanting OVCAR3-Luc cells intraperitoneally,into the subscapular areas. Six or seven weeks after the inoculation,the treatment was initiated. PBS and 10 mg/kg of LSR-ADC were intravenously injected twice a week,for a total of four times.    Click to Show/Hide
In Vivo Model	Ovarian high-grade serous carcinoma PDX model (PDX: OVCAR3-LUC)
Experiment 4 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.24%	High LSR expression (LSR+++; 86,697.7 LSR expression (ABC/cell))
Method Description	The model was Ovx6 PDX,which was generated by implanting human tumor tissues expressing LSR at high levels. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (10 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model	Ovarian cancer PDX model (PDX: Ovx6)

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 21.41%	High LSR expression (LSR+++)
Method Description	The model was established by subcutaneously implanting OVCAR3 cells into CB17/SCID mice. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (1 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model	Ovarian high-grade serous carcinoma CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46.43%	High LSR expression (LSR+++)
Method Description	The model was established by subcutaneously implanting OVCAR3 cells into CB17/SCID mice. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (3 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model	Ovarian high-grade serous carcinoma CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 3 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.01%	High LSR expression (LSR+++)
Method Description	The model was established by subcutaneously implanting OVCAR3 cells into CB17/SCID mice. When the mean tumor size of each cancer type reached approximately 110 mm3,PBS or LSR-ADC (10 mg/kg) were intravenously injected twice a week,for a total of four times.
In Vivo Model	Ovarian high-grade serous carcinoma CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	449 pM	High LSR expression (LSR+++; 89,382.9 LSR expression (ABC/cell))
Method Description	Cytotoxicity assays were performed in the presence of the anti-LSR mAb (#16-6),the mouse IgG2a isotype control antibody,the LSR-ADC or the control-ADC. After 24 h,the cells were incubated with serial dilutions of the agents in triplicate wells for 144 h,at 37°C,in a humidified 5% CO2 atmosphere. Cell viability was determined with the CellTiter-Glo Luminescent Cell Viability Assay Kit.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	High LSR expression (LSR+++; 86,697.7 LSR expression (ABC/cell))
Method Description	Cytotoxicity assays were performed in the presence of the anti-LSR mAb (#16-6),the mouse IgG2a isotype control antibody,the LSR-ADC or the control-ADC. After 24 h,the cells were incubated with serial dilutions of the agents in triplicate wells for 144 h,at 37°C,in a humidified 5% CO2 atmosphere. Cell viability was determined with the CellTiter-Glo Luminescent Cell Viability Assay Kit.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 Luc cells		CVCL_0465
Experiment 3 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.74 nM	High LSR expression (LSR+++; 84,008.8 LSR expression (ABC/cell))
Method Description	Cytotoxicity assays were performed in the presence of the anti-LSR mAb (#16-6),the mouse IgG2a isotype control antibody,the LSR-ADC or the control-ADC. After 24 h,the cells were incubated with serial dilutions of the agents in triplicate wells for 144 h,at 37°C,in a humidified 5% CO2 atmosphere. Cell viability was determined with the CellTiter-Glo Luminescent Cell Viability Assay Kit.    Click to Show/Hide
In Vitro Model	Ovarian cancer ascites	NOVC-7C cells		Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	Moderate LSR expression (LSR++; 2,631.9 LSR expression (ABC/cell))
Method Description	Cytotoxicity assays were performed in the presence of the anti-LSR mAb (#16-6),the mouse IgG2a isotype control antibody,the LSR-ADC or the control-ADC. After 24 h,the cells were incubated with serial dilutions of the agents in triplicate wells for 144 h,at 37°C,in a humidified 5% CO2 atmosphere. Cell viability was determined with the CellTiter-Glo Luminescent Cell Viability Assay Kit.    Click to Show/Hide
In Vitro Model	Ewing sarcoma	ES2 cells		CVCL_AX39

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 57.70%	Positive AXL expression (AXL+++/++)
Method Description	The anti-tumor activity of ADCs were determined in the pancreas cancer patient-derived xenograft (PDX) model PAXF1657. Before treatment,mice were divided into groups of 68 mice each,with equal tumor size distribution (average and variance). ADC is administered at a dose of 2.00 mg/kg in a single dose.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 2 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.30%	Positive AXL expression (AXL+++/++)
Method Description	The anti-tumor activity of ADCs were determined in the pancreas cancer patient-derived xenograft (PDX) model PAXF1657. Before treatment,mice were divided into groups of 68 mice each,with equal tumor size distribution (average and variance). ADC is administered at a dose of 4.00 mg/kg in a single dose.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.20%	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.30%	Positive CLDN18.2 expression (CLDN18.2 +++/++)
Method Description	Conjugates of the exemplary antibodies were tested using an established PDX model of pancreatic cancer cell 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	Pancreatic cancer PDX model

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	501 ng/mL	Positive CLDN18.2 expression (CLDN18.2 +++/++)
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 tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70%	Positive CLDN18.2 expression (CLDN18.2 +++/++)
Method Description	Conjugates of the exemplary antibodies were tested using an established PDX model of pancreatic cancer cell 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	Pancreatic cancer PDX model

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.51 ng/mL	Positive CLDN18.2 expression (CLDN18.2 +++/++)
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 tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	71%	Moderate Tissue factor expression (TF++; IHC H-score=155)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 190 mm3 The model dosed weekly at 25 mg/kg for 3 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived xenograft (PDX) ovarian carcinomamodel
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 140 mm3 The model dosed weekly at 4 mg/kg for 3 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived gastric adenocarcinoma xenograft (PDX) model
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 210 mm3 The model dosed weekly at 5 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived head and neck carcinoma xenograft (PDX) model

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	67%	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	98%	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 5 mg/kg for 3 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 5 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Effective Concentration (EC50)	26 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6 nM	High Tissue factor expression (TF+++; IHC H-score=250)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18 nM	High Tissue factor expression (TF+++; IHC H-score=250)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (25A-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 380,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 73.30%	Positive AXL expression (AXL+++/++)
Method Description	The anti-tumor activity of ADCs were determined in the pancreas cancer patient-derived xenograft (PDX) model PAXF1657. Before treatment,mice were divided into groups of 68 mice each,with equal tumor size distribution (average and variance). ADC is administered at a dose of 2.00 mg/kg in a single dose.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)
Experiment 2 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.20%	Positive AXL expression (AXL+++/++)
Method Description	The anti-tumor activity of ADCs were determined in the pancreas cancer patient-derived xenograft (PDX) model PAXF1657. Before treatment,mice were divided into groups of 68 mice each,with equal tumor size distribution (average and variance). ADC is administered at a dose of 4.00 mg/kg in a single dose.
In Vivo Model	Pancreatic cancer PDX model (PDX: PAXF1657)

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.10%	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	74%	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 190 mm3 The model dosed weekly at 25 mg/kg for 3 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived xenograft (PDX) ovarian carcinomamodel
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low FOLR1 expression (FOLR1+)
Method Description	TF-positive patient-derived xenograft (PDX) models were performed in athymic nude mice to evaluate the efficacy of the ADCs in vivo. Study animals were implanted unilaterally on the left flank with tumor fragments. Animals were randomized and treated as indicated in the figures. Animals were removed from study and euthanized once tumor size reached 1,200 mm3 or skin ulceration was evident. In addition, the MTV curve for the treatment group in question was no longer shown once an animal was removed from study due to size TGI and statistical analyses were conducted in the same manner as for the CDX studies. The CR and PR response definitions were as follows for the PDX studies: a PR responder had a MTV 30% of MTV at day 1 for two consecutive measurements; a CR responder had an undetectable MTV for two consecutive measurement IHC analisys: Formalin-fixed paraffin-embedded (FFPE) tissues were sectioned at 4-m thickness and mounted onto positive-charged glass slides The tissue sections were stained with the anti-TF antibody HTF-1 ADC treatment started on day 1 after animals with a tumor size of approximately 210 mm3 The model dosed weekly at 5 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	Patient-derived xenograft (PDX) head and neck carcinoma model

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	48%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	95%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 5 mg/kg for 3 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 5 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Effective Concentration (EC50)	43 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (43Ea-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.49%	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (1.1 mg/kg) via the tail vein on Day 0.
In Vivo Model	Gastric cancer PDX model (PDX: LU2535)
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg) via the tail vein on Day 0.
In Vivo Model	Gastric cancer PDX model (PDX: LU2535)
Experiment 3 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3.3 mg/kg) via the tail vein on Day 0.
In Vivo Model	Gastric cancer PDX model (PDX: LU2535)
Experiment 4 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (10 mg/kg) via the tail vein on Day 0.
In Vivo Model	Gastric cancer PDX model (PDX: GA0045)

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 22%	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with MKN-45 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (0.75 mg/kg) via the tail vein on Day 0.
In Vivo Model	MKN-45 CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70%	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with MKN-45 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (1.5 mg/kg) via the tail vein on Day 0.
In Vivo Model	MKN-45 CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99%	Positive MET expression (MET+++/++)
Method Description	Inoculate mice with MKN-45 cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg) via the tail vein on Day 0.
In Vivo Model	MKN-45 CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.80%	High GPC1 expression (GPC1+++)
In Vivo Model	Pancreatic cancer PDX model (PDX: PK645)
Experiment 2 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.70%	High GPC1 expression (GPC1+++)
In Vivo Model	Pancreatic cancer PDX model (PDX: PK565)

Experiment 1 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80.9 pM	High GPC1 expression (GPC1+++)
Method Description	GPC1-ADC(MMAE) induces efficient tumor cell killing in cells PDX models from a Pancreatic ductal adenocarcinoma (PDAC) patient with GPC1 expression.
In Vitro Model	Pancreatic carcinoma	KP-2 cells		CVCL_3004
Experiment 2 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.55 nM	High GPC1 expression (GPC1+++)
Method Description	GPC1-ADC(MMAE) induces efficient tumor cell killing in cells PDX models from a Pancreatic ductal adenocarcinoma (PDAC) patient with GPC1 expression.
In Vitro Model	Pancreatic ductal adenocarcinoma	PK-8 cells		CVCL_4718
Experiment 3 Reporting the Activity Date of This ADC					[10]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.68 nM	High GPC1 expression (GPC1+++)
Method Description	GPC1-ADC(MMAE) induces efficient tumor cell killing in cells PDX models from a Pancreatic ductal adenocarcinoma (PDAC) patient with GPC1 expression.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[11]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive CDCP1 expression (CDCP1 +++/++)
Method Description	Mice were randomized into groups of six and administered a single intravenous treatment of 10D7 MMAE (5 mg/kg), 10D7 (5 mg/kg), MMAE (0.17 mg/kg; equivalent to a four molar excess of the 10D7-MMAE dose) or vehicle.
In Vivo Model	Ovarian cancer PDX model (PDX: PH250)

Experiment 1 Reporting the Activity Date of This ADC					[12]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High PODXL expression (PODXL+++)
Method Description	MIA PaCa-2 (1x106) or OV3331 (1x106) cells were injected subcutaneously into the right flank of NSG or nude mice. Tumor dimensions were measured twice a week and tumor volumes (cm3) were calculated by. Once tumors reached 0.15cm3, mice were treated with either PODO447- or palivizumab-Vedotin at concentrations ranging from 4 2 mg/kg. ADC treatments were administered intravenously every 4 days.    Click to Show/Hide
In Vivo Model	Pancreas cancer PDX model (PDX: MIA PaCa-2)

Experiment 1 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Negative EGFR expression (EGFR -)
Method Description	After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 106 NCI-H2228 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model	NCI-H2228 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.65%	Positive EGFR expression (EGFR +++/++)
Method Description	After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 106 HCC827 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model	HCC827 CDX model
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063

Experiment 1 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.5 nM	Positive EGFR expression (EGFR +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative EGFR expression (EGFR -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543

Experiment 1 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Negative EGFR expression (EGFR -)
Method Description	After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 106 NCI-H2228 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model	NCI-H2228 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.65%	Positive EGFR expression (EGFR +++/++)
Method Description	After acclimatization for one week, healthy mice were subcutaneously implanted with 5 x 106 HCC827 cells. Fourteen days after implantation the mice were divided into three groups (n = 8 each): 21, 22 and PBS as control. All the groups received four doses of 20 mg/kg on days 0, 4, 8 and 12, injected intravenously.
In Vivo Model	HCC827 CDX model
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063

Experiment 1 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.5 nM	Positive EGFR expression (EGFR +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative EGFR expression (EGFR -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	An in vivo therapy experiments with c1F6-9a was undertaken in nude mice with subcutaneous Karpas 299 ALCL tumors. The animals (5 per group)were treated with a single intravenous dose of c1F6-9a at 3 mg/kg (mAb component) on day 14.
In Vivo Model	Karpas-299 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					[14]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.45 nM	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 30 nM	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 3 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Moderate EGFR expression (EGFR ++)
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 0.3 mg/kg, i.v., q4d*4 of one of the conjugates listed above or with PBS only.
In Vivo Model	LoVo CDX model
In Vitro Model	Colon adenocarcinoma	LoVo cells		CVCL_0399
Experiment 2 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46%	Positive EGFR expression (EGFR +++/++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 1 mg/kg, i.v., q4d*4 of one of the conjugates listed above or with PBS only.
In Vivo Model	HT-29 CDX model
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 3 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 54%	Positive EGFR expression (EGFR +++/++)
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 5 mg/kg, i.v., q4d*4 of one of the conjugates listed above or with PBS only.
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					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 72.70%	Moderate EGFR expression (EGFR ++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 1 mg/kg, i.v., q4d*4 of one of the conjugates listed above or with PBS only.
In Vivo Model	LoVo CDX model
In Vitro Model	Colon adenocarcinoma	LoVo cells		CVCL_0399
Experiment 5 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.60%	Moderate EGFR expression (EGFR ++)
Method Description	Conjugates of the exemplary antibodies were tested using an established xenograft model implanted subcutaneous into SCID mice. Mice were randomized by body weight into treatment groups and treated once post cell inoculation with 3 mg/kg, i.v., q4d*4 of one of the conjugates listed above or with PBS only.
In Vivo Model	LoVo CDX model
In Vitro Model	Colon adenocarcinoma	LoVo cells		CVCL_0399

Experiment 1 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Effective Concentration (EC50)	5.1 ng/mL	Positive EGFR expression (EGFR +++/++)
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	Colorectal carcinoma	DiFi cells		CVCL_6895
Experiment 2 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Effective Concentration (EC50)	9.8 ng/mL	Positive EGFR expression (EGFR +++/++)
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	Colorectal carcinoma	DiFi cells		CVCL_6895
Experiment 3 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Effective Concentration (EC50)	611 ng/mL	Positive EGFR expression (EGFR +++/++)
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	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 4 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.2 ug/mL	Moderate EGFR expression (EGFR ++)
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	Colon adenocarcinoma	LoVo cells		CVCL_0399
Experiment 5 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Effective Concentration (EC50)	5.3 ug/mL	Positive EGFR expression (EGFR +++/++)
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					[15]
Efficacy Data	Half Maximal Effective Concentration (EC50)	28.3 ug/mL	Positive EGFR expression (EGFR +++/++)
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 1 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 0%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 2 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 18.98%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 3 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 26.28%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 4 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 41.70%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 5 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.30%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 6 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.51%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 7 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.57%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 8 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.92%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 9 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.81%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 10 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.92%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 11 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.77%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 12 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.10%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted MDAMB-468 breast cancer tumor cells, and show responsiveness against the MDA-MB-468 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	MDA-MB-468 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 13 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.25%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490

Experiment 1 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 2 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 3 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 4 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.3 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Neoplasm	Hs 700T cells		CVCL_0858
Experiment 5 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.74 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.89 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 7 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.38 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 8 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.8 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 9 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.59 nM	Low CD276 expression (CD276 +)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 10 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative CD276 expression (CD276 -)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511

Experiment 1 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	0%	Moderate LRRC15 expression (LRRC15++; IHC 2+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) was demonstrated in MC-38 xenografts.
In Vivo Model	MC-38 CDX model
In Vitro Model	Mouse colon adenocarcinoma	MC-38 cells		CVCL_B288
Experiment 2 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	59.41%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in HPAF-II xenografts.
In Vivo Model	HPAF-II CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 3 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	64.94%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) was demonstrated in SCC-15 xenografts.
In Vivo Model	SCC-15 CDX model
In Vitro Model	Squamous carcinoma	SCC-15 cells		CVCL_1681
Experiment 4 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	71.99%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 5 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	80.57%	Moderate LRRC15 expression (LRRC15++; IHC 2+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) plus anti-PD1 mAb (2 mg/kg) were demonstrated in MC-38 xenografts.
In Vivo Model	MC-38 CDX model
In Vitro Model	Mouse colon adenocarcinoma	MC-38 cells		CVCL_B288
Experiment 6 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	87.45%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) was demonstrated in NW-231 xenografts.
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 7 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	88.36%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (4.5 mg/kg) was demonstrated in HN-5 xenografts.
In Vivo Model	HPAF-II CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 8 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	88.55%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) plus Carboplatin (50 mg/kg) were demonstrated in SCC-15 xenografts.
In Vivo Model	SCC-15 CDX model
In Vitro Model	Squamous carcinoma	SCC-15 cells		CVCL_1681
Experiment 9 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	89.39%	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) was demonstrated in PANC-1 xenografts.
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 10 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	89.73%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) plus Cetuximab (3 mg/kg) were demonstrated in SCC-15 xenografts.
In Vivo Model	SCC-15 CDX model
In Vitro Model	Squamous carcinoma	SCC-15 cells		CVCL_1681
Experiment 11 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	90.12%	Moderate LRRC15 expression (LRRC15++; IHC 2+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) was demonstrated in NW-231 xenografts.
In Vivo Model	NW-231 CDX model
In Vitro Model	Triple negative breast cancer	NW231 cells		Homo sapiens
Experiment 12 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	91.24%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 13 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	91.66%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (3 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 14 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	91.84%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in SCC-15 xenografts.
In Vivo Model	NCI-H1650 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 15 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	91.86%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 16 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92.25%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (12 mg/kg) plus Radiation (15 Gy) were demonstrated in SCC-15 xenografts.
In Vivo Model	SCC-15 CDX model
In Vitro Model	Squamous carcinoma	SCC-15 cells		CVCL_1681
Experiment 17 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92.71%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in NCI-H1650 xenografts.
In Vivo Model	NCI-H1650 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 18 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	93.56%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) plus Gemcitabine (80 mg/kg) were demonstrated in HPAF-II xenografts.
In Vivo Model	HPAF-II CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 19 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	96.35%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in NCI-H1650 xenografts.
In Vivo Model	HN-5 CDX model
In Vitro Model	Squamous cell carcinoma	HN-5 cells		CVCL_8128
Experiment 20 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	97.05%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 21 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	98.10%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) plus Gemcitabine (100 mg/kg) were demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891
Experiment 22 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	98.18%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (6 mg/kg) plus Erlotinib (100 mg/kg) were demonstrated in SCC-15 xenografts.
In Vivo Model	NCI-H1650 CDX model
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 23 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	99.13%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-VCMMAE-E2 (3 mg/kg) plus Docetaxel (7.5 mg/kg) were demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891

Experiment 1 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive LRRC15 expression (LRRC15 +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 values were determined by quantitating viable cells using a CellTiter-Glo luminescent assay.
In Vitro Model	Colon carcinoma	HCT 116 cells		CVCL_0291

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 3.53%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 15.69%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 22.02%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 28.11%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.13%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 10 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 52.51%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 30 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	27.4 nM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 5.27%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 2 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 22.47%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 3 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34.64%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 4 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 34.70%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 5 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 36.36%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 6 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.15%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 7 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 65.31%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 8 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.67%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 9 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.74%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted MDAMB-468 breast cancer tumor cells, and show responsiveness against the MDA-MB-468 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	MDA-MB-468 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 10 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.27%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 11 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.12%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 12 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.55%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 13 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.28%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479

Experiment 1 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	31 pM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 2 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	59 pM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 3 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	90 pM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 4 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 5 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Neoplasm	Hs 700T cells		CVCL_0858
Experiment 6 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 8 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.56 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 9 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.77 nM	Low CD276 expression (CD276 +)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 10 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative CD276 expression (CD276 -)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 5.54%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 30 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	128.5 nM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	11%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-vcMMAE-DAR4 (10 mg/kg) was demonstrated in HCC-827-ER xenografts.
In Vivo Model	HCC-827-ER CDX model
In Vitro Model	Lung adenocarcinoma	HCC827 ER1 cells		CVCL_EJ07
Experiment 2 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	59.49%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-vcMMAE-DAR4 (3 mg/kg) was demonstrated in SUM190PT xenografts.
In Vivo Model	SUM190PT CDX model
In Vitro Model	Breast inflammatory carcinoma	SUM190PT cells		CVCL_3423
Experiment 3 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	84.03%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huM25-vcMMAE-DAR4 (3 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891

Experiment 1 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 11.64%	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm3 on average (Day 1), and 0.25 mg/kg of ADC9.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 51.60%	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm3 on average (Day 1), and 1 mg/kg of ADC9.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609

Experiment 1 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.5 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543
Experiment 2 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.58 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 3 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	32.05 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.26 uM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 5 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.81 uM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
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)	≈ 12.50%	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 15.63%	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 3 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 45.63%	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 4 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 54.17%	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 5 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.50%	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 6 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 7 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Median survival time (MST)	14 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 8 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Median survival time (MST)	23 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (0.1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 9 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Median survival time (MST)	24 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 10 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Median survival time (MST)	30 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (1 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 11 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Median survival time (MST)	60 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous MIA PaCa-2 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	MIA PaCa-2 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428
Experiment 12 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Median survival time (MST)	61 Day	Positive EGFR expression (EGFR +++/++)
Method Description	CB17 SCID mice bearing subcutaneous PANC-1 (n = 4-5 pergroup) xenografts were intravenously injected with saline, CTX-MMAE (5 mg/kg) on day 0 and 8 of the study (indicated by vertical dashed lines).
In Vivo Model	PANC-1 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	39 pM	Positive EGFR expression (EGFR +++/++)
Method Description	MIA PaCa-2 and PANC-1 cells were seeded at 1000 and 1500 per well, respectively, in a 96-well plate and left to adhere overnight. Cells were treated with a 5-fold dilution series of CTX-MMAE or CTX ranging from 0.000256 to 500 nM for 96 h.
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 2 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.38 nM	Positive EGFR expression (EGFR +++/++)
Method Description	MIA PaCa-2 and PANC-1 cells were seeded at 1000 and 1500 per well, respectively, in a 96-well plate and left to adhere overnight. Cells were treated with a 5-fold dilution series of CTX-MMAE or CTX ranging from 0.000256 to 500 nM for 96 h.
In Vitro Model	Pancreatic ductal adenocarcinoma	MIA PaCa-2 cells		CVCL_0428

Experiment 1 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 13.21%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 2 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 14.62%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 3 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 25.99%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 4 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.46%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 5 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 30.91%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 6 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 32.04%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 1 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 7 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.42%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted PA-1 ovarian cancer cells, and show responsiveness against the PA-1 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	PA-1 CDX model
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 8 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.12%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 9 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 77.78%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 10 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.78%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted NCI-H1703 non-small cell lung cancer cells, and show responsiveness against the NCI-H1703 tumor cells. The dose was 3 mg/kg on day 30.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 11 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90.90%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted MDAMB-468 breast cancer tumor cells, and show responsiveness against the MDA-MB-468 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	MDA-MB-468 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 12 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.77%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted A375.52 melanoma cells, and show responsiveness against the A375.52 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	A375.52 CDX model
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 13 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.44%	Moderate CD276 expression (CD276 ++)
Method Description	The results of this study with respect to mammary fat pad implanted Calu-6 lung cancer cells, and show responsiveness against the Calu-6 tumor cells. The dose was 10 mg/kg on day 30.
In Vivo Model	Calu-6 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236

Experiment 1 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16 pM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 2 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	30 pM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 3 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	43 pM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 4 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Neoplasm	Hs 700T cells		CVCL_0858
Experiment 5 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 7 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.27 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 8 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 9 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.47 nM	Low CD276 expression (CD276 +)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 10 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative CD276 expression (CD276 -)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 24.70%	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 26.50%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 26.90%	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm3 on average (Day 1), and 1 mg/kg QDx1 of ADC2.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.36%	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 184mm3 on average (Day 1), and 3 mg/kg QWx4 of ADC2.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 3 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85.43%	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm3 on average (Day 1), and 4 mg/kg of ADC2.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 4 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.22%	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing mantle cell lymphoma cell line JeKo-1 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 184mm3 on average (Day 1), and 3 mg/kg QWx4 of ADC2.
In Vivo Model	JeKo-1 CDX model
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 5 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.81%	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing breast cancer cell line HCC1187 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 110 mm3 on average (Day 1), and 0.31 mg/kg QWx4 of ADC5.
In Vivo Model	HCC1187 CDX model
In Vitro Model	Breast ductal carcinoma	HCC1187 cells		CVCL_1247

Experiment 1 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.59 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543
Experiment 2 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.57 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.53 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258
Experiment 4 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.91 uM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 5 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.28 uM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 27.70%	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 0.7 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					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 33.30%	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 2 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 3 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90%	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	BxPC3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91%	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 7 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 5 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.60%	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 6 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99%	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	BxPC3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 7 Reporting the Activity Date of This ADC					[15]
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					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 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 2 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 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 3 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 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 4 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.55 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 5 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	32.49 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					[15]
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 7 Reporting the Activity Date of This ADC					[15]
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					[15]
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					[15]
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					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 32.10%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 2 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 32.20%	High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
Method Description	CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. When the tumor volume reached approximately 230 mm3, a single dose of Ha15-1c25E, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model	Bladder cancer CDX model
In Vitro Model	Bladder carcinoma	RT-4 cells		CVCL_0036

Experiment 1 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 33.50%	High MUC1 expression (MUC1+++)
Method Description	To examine the efficacy of the HzMUC1-MMAE in decreasing pancreatic tumor growth in vivo,pancreatic tumor xenograft mouse model was established. BALB/c nu/nu mice were subcutaneously injected with CFPAC-1 cells. When the CFPAC-1 tumors reached the sizes of 150 mm3,mice were randomized into two groups and treated with PBS and HzMUC1-MMAE (5 mg/kg,every 6 days,for 2 doses).    Click to Show/Hide
In Vivo Model	Pancreatic cancer CDX model
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.10%	High MUC1 expression (MUC1+++)
Method Description	To examine the efficacy of the HzMUC1-MMAE in decreasing pancreatic tumor growth in vivo,pancreatic tumor xenograft mouse model was established. BALB/c nu/nu mice were subcutaneously injected with Capan-2 cells. When the Capan-2 tumors reached the sizes of 120 mm3,mice were randomized into two groups and treated with PBS and HzMUC1-MMAE (5 mg/kg,every 6 days,for 2 doses).    Click to Show/Hide
In Vivo Model	Pancreatic cancer CDX model
In Vitro Model	Pancreatic cancer	Pancreatic cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26 nM	High MUC1 expression (MUC1+++)
Method Description	The inhibitory activity of HzMUC1-ADC against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 5 days.
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-2 cells		CVCL_0026
Experiment 2 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	50 nM	High MUC1 expression (MUC1+++)
Method Description	The inhibitory activity of HzMUC1-ADC against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 5 days.
In Vitro Model	Cystic fibrosis	CFPAC-1 cells		CVCL_1119
Experiment 3 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	59 nM	Moderate MUC1 expression (MUC1++)
Method Description	The inhibitory activity of HzMUC1-ADC against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 5 days.
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 4 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	Negative MUC1 expression (MUC1-)
Method Description	The inhibitory activity of HzMUC1-ADC against cancer cell growth was evaluated in various human cancer cell lines in vitro. The cells were treated 5 days.
In Vitro Model	Pancreatic adenocarcinoma	SW1990 cells		CVCL_1723

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 37.39%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.15%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 40.21%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 40.94%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 30 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.8 nM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Tumor Growth Inhibition value (TGI)	41.21%	Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Method Description	1 mg conjugate/kg/inj.
In Vivo Model	Karpas 299 ALCL cell line xenograft model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Tumor Growth Inhibition value (TGI)	88.67%	Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Method Description	3 mg conjugate/kg/inj.
In Vivo Model	L2987 cell line xenograft model
In Vitro Model	Lung adenocarcinoma	L2987 cells		CVCL_H586
Experiment 3 Reporting the Activity Date of This ADC					[25]
Efficacy Data	Tumor Growth Inhibition value (TGI)	91.60%	Negative Lewis Y expression (Lewis Y-); Positive CD30 expression (CD30+++/++)
Method Description	3 mg conjugate/kg/inj.
In Vivo Model	L2987 cell line xenograft model
In Vitro Model	Lung adenocarcinoma	L2987 cells		CVCL_H586

Experiment 1 Reporting the Activity Date of This ADC					[85]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10 ng/mL	Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =2,111)
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[85]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13 ng/mL	Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =3,500)
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[85]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18 ng/mL	Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =755)
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Breast carcinoma	H3396 cells		CVCL_D348
Experiment 4 Reporting the Activity Date of This ADC					[85]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80 ng/mL	Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =645)
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[85]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80 ng/mL	Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =600)
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Colon carcinoma	RCA cells		CVCL_R735
Experiment 6 Reporting the Activity Date of This ADC					[85]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80 ng/mL	Positive Lewis Y expression (Lewis Y+++/++; FACS analysis =922)
Method Description	The inhibitory activity of the mAb-Val-Cit-MMAE conjugates exhibited greater in vitrospecificity and lower in vivo toxicity was compared with corresponding hydrazone conjugatescorresponding hydrazone conjugates on H3396 cells.The cytotoxic effects of the conjugates on H3396 cells (cBR96 Ag+,cAC10 Ag-) were determined using both pulsed (2 h) and long-term(97 h) drug exposure assays.    Click to Show/Hide
In Vitro Model	Amelanotic melanoma	MDA-MB-435 cells		CVCL_0417

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 44.77%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.85%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 46%	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 1 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					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.80%	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 1 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	BxPC3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[15]
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 10 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	BxPC3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[15]
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 3 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	BxPC3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC					[15]
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 3 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					[15]
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 adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 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					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 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 ductal carcinoma	HCC1937 cells		CVCL_0290
Experiment 4 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 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 5 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 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 ductal carcinoma	HCC38 cells		CVCL_1267
Experiment 6 Reporting the Activity Date of This ADC					[15]
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	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 7 Reporting the Activity Date of This ADC					[15]
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					[15]
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					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 47.70%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 30 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	234 nM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	49%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	93%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Effective Concentration (EC50)	27 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (43D7-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 49.63%	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm3 on average (Day 1), and 0.25 mg/kg of 2A2 dPBD ADC.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 2 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive ROR1 expression (ROR1+++/++)
Method Description	1 x 107 cells/head of human ROR-1 expressing lung cancer cell line Calu-3 were grafted to severe combined immunodeficient (SCID) mice to prepare human cancergrafted mice. After grafting, the mice were grouped when tumor size reached 111mm3 on average (Day 1), and 1 mg/kg of 2A2 dPBD ADC.
In Vivo Model	Calu-3 CDX model
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609

Experiment 1 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1000 pM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.48 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 3 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543
Experiment 5 Reporting the Activity Date of This ADC					[19]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.43 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	In a 96-well plate, each well was seeded with 4,000 to 5,000 of the respective cancer cell lines. After culturing for 24 hours, they were treated with the ADCs at a concentra-tion of 0.0015 to 10.0 nM (serially diluted threefold). 72 hours later, the number of live cells was measured using WST-8.
In Vitro Model	Breast squamous cell carcinoma	HCC1806 cells		CVCL_1258

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 50.60%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.85%	Positive CD19 expression (CD19+++/++)
Method Description	To establish DOHH1 tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice (Harlan,Indianapolis, IN). When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 4 mg/kg single.
In Vivo Model	DOHH1 CDX model
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 51.93%	Positive CLDN1 expression (CLDN1 +++/++)
Method Description	100,000 SW620 cells were suspended in culture medium and Matrigel (v/v) and injected subcutaneously into the right flank of 6-week-old female athymic nude mice. When the tumor volume reached approximately 100 mm3, mice were randomized in different groups. For ADC experiments, mice received by iv injection 0.9% NaCl or ADCs (5 mg/kg per injection) twice per week for 4 weeks.    Click to Show/Hide
In Vivo Model	SW620 CDX model
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547
Experiment 2 Reporting the Activity Date of This ADC					[26]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 55.59%	Positive CLDN1 expression (CLDN1 +++/++)
Method Description	100,000 SW620 cells were suspended in culture medium and Matrigel (v/v) and injected subcutaneously into the right flank of 6-week-old female athymic nude mice. For the sequential combination experiments, mice received oxaliplatin at 3 mg/kg once per week followed by an iv injection of ADC-6F6 at 5 mg/kg after 3 and 6 days.
In Vivo Model	SW620 CDX model
In Vitro Model	Colon adenocarcinoma	SW620 cells		CVCL_0547

Experiment 1 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 52%	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 1 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					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.70%	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 0.3 mg/kg, i.v., qw of one of the conjugates listed above or with PBS only.
In Vivo Model	BxPC3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96%	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 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					[15]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.80%	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 2 Reporting the Activity Date of This ADC					[15]
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	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[15]
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 adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 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 5 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 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 ductal carcinoma	HCC1937 cells		CVCL_0290
Experiment 6 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.18 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 ductal carcinoma	HCC38 cells		CVCL_1267
Experiment 7 Reporting the Activity Date of This ADC					[15]
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	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 8 Reporting the Activity Date of This ADC					[15]
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 9 Reporting the Activity Date of This ADC					[15]
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					[27]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 52.40%	Positive LRG1 expression (LRG1+++/++)
Method Description	Single-cell suspensions of 1 x106 B16F0 cells were injected subcutaneously into the lower back of Lrg1+/+ C57BL/6 mice in 100 mL PBS. Tumours were measured and therapy was initiated when tumour volumes reached 0.1 cm3. ADC was administered at a dose of 20 mg/kg treatments were administered by a single intraperitoneal injection every 7 days for 3 weeks.    Click to Show/Hide
In Vivo Model	Melanoma CDX model
In Vitro Model	Melanoma	Melanoma cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[27]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.9 nM	Positive LRG1 expression (LRG1+++/++)
Method Description	5 x104 cells were seeded in 96-well plates and incubated at 37 overnight. Cells were thenexposed to a range of concentrations of the test compounds diluted in growth medium at pH 6.5 and at 37 as ADC 5 (0100 nM, 72 h). MTT reagent (12 mM) was then added to each well and cells were incubated for 4 h at 37 , followed by the addition of DMSO and further incubation at 37 1C for 1 h.    Click to Show/Hide
In Vitro Model	Mouse melanoma	B16-F0 cells		CVCL_0604

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 53.70%	Positive HER2 expression (HER2 +++/++)
Method Description	N87 tumors were implanted to NOD/SCID mice to the size of about 100 mm3 (day 0) and were then treated with ADCs at day 0, day 7 and day 14 at the dosage of 30 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	46.7 nM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 53.99%	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (2 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.50%	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (5 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.27 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.33 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 54%	High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
Method Description	CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. When the tumor volume reached approximately 230 mm3, a single dose of Ha15-1abe16E, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model	Bladder cancer CDX model
In Vitro Model	Bladder cancer	Bladder cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.18%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.50%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 56.90%	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 57.60%	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 58.49%	Negative HER2 expression (HER2-)
Method Description	The nude mice were implanted with a human cancer cell line(MDA-MB-231) and the ADCs (10 mg/kg) were administered through intraperitoneal injection when the tumor volume reached about 100 cubic millimeters. The tumor volumes were monitored every 3 days and animals were sacrificed at the end of 21 days and the tumors were dissected and weighed.
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					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 58.80%	Positive KKLC1 expression (KKLC1+++/++)
Method Description	The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 0.3 mg/kg.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 2 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.36%	Positive KKLC1 expression (KKLC1+++/++)
Method Description	The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 1 mg/kg.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.05%	Positive KKLC1 expression (KKLC1+++/++)
Method Description	The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 3 mg/kg.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 4 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.92%	Positive KKLC1 expression (KKLC1+++/++)
Method Description	The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 2 mg/kg.
In Vivo Model	Gastric cancer CDX model
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434

Experiment 1 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.87 nM	Positive KKLC1 expression (KKLC1+++/++)
Method Description	The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Gastric signet ring cell adenocarcinoma	NUGC-4 cells		CVCL_3082
Experiment 2 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.26 nM	Positive KKLC1 expression (KKLC1+++/++)
Method Description	The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Gastric adenocarcinoma	MKN45 cells		CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC					[30]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	786 nM	Positive KKLC1 expression (KKLC1+++/++)
Method Description	The inhibitory activity of 1131-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Gastric carcinoma	HGC-27 cells		CVCL_1279

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.61%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.75%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 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					[21]
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					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 59.70%	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 62.76%	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	IC1-MMAE (1 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of MDA-MB-436 or MDA-MB-231 cells with ICAM1 expression with high expression.
In Vivo Model	MDA-MB-436 CDX model
In Vitro Model	Metastasis of ductal carcinoma	MDA-MB-436 cells		CVCL_0623
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.70%	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	IC1-MMAE (5 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of MDA-MB-436 or MDA-MB-231 cells with ICAM1 expression with high expression.
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					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.50%	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	IC1-MMAE (10 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of MDA-MB-436 or MDA-MB-231 cells with ICAM1 expression with high expression.
In Vivo Model	MDA-MB-436 CDX model
In Vitro Model	Metastasis of ductal carcinoma	MDA-MB-436 cells		CVCL_0623
Experiment 4 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.50%	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	IC1-MMAE (5 m ug/kg, every seven days x3) induces efficient tumor cell killing in cell line-derived models of MDA-MB-436 or MDA-MB-231 cells with ICAM1 expression with high expression.
In Vivo Model	MDA-MB-436 CDX model
In Vitro Model	Metastasis of ductal carcinoma	MDA-MB-436 cells		CVCL_0623

Experiment 1 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.1 pM	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	In vitro cytotoxicity of four ICAM1 ADCs against a panel of four human TNBC cell lines.
In Vitro Model	Metastasis of ductal carcinoma	MDA-MB-436 cells		CVCL_0623
Experiment 2 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	In vitro cytotoxicity of four ICAM1 ADCs against a panel of four human TNBC cell lines.
In Vitro Model	Breast carcinoma	MDA-MB-157 cells		CVCL_0618
Experiment 3 Reporting the Activity Date of This ADC					[31]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.25 nM	Positive ICAM1 expression (ICAM1 +++/++)
Method Description	In vitro cytotoxicity of four ICAM1 ADCs against a panel of four human TNBC cell lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	63%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	69%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Effective Concentration (EC50)	18 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (25G1-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.68%	Positive GD2 expression (GD2+++/++)
Method Description	When tumors reached 50 mm3 volume. Three groups received intravenous injections of 100 ug (5 mg/kg) ch14.18-MMAE, ch14.18-MMAF, or naked antibody for five times with an interval of 4 days, and the control group was injected with PBS.
In Vivo Model	B78-D14 CDX model
In Vitro Model	Amelanotic melanoma	B78-D14 cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Thymoma	EL4 cells		CVCL_0255
Experiment 2 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.3 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Neuroblastoma	IMR-32 cells		CVCL_0346
Experiment 3 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Amelanotic melanoma	COLO 38 cells		CVCL_3934
Experiment 4 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.44 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Amelanotic melanoma	B78-D14 cells		Homo sapiens
Experiment 5 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.51 nM	Moderate GD2 expression (GD2++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Pleural malignant mesothelioma	MS-1 [Human mesothelioma] cells		CVCL_E993
Experiment 6 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.68 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Glioblastoma	T98G cells		CVCL_0556
Experiment 7 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.69 nM	Moderate GD2 expression (GD2++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Osteosarcoma	U2OS cells		CVCL_0042
Experiment 8 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.93 nM	Moderate GD2 expression (GD2++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Invasive breast carcinoma	Hs 578T cells		CVCL_0332
Experiment 9 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.48 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Bone marrow neuroblastoma	SH-SY5Y cells		CVCL_0019
Experiment 10 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.28 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Astrocytoma	1321N1 cells		CVCL_0110
Experiment 11 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.8 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Amelanotic melanoma	A375 cells		CVCL_0132
Experiment 12 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.4 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 13 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.1 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Osteosarcoma	MG-63 cells		CVCL_0426
Experiment 14 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 40 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Malignant neoplasms of the mouse mammary gland	M3 cells		CVCL_4Y25
Experiment 15 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 40 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Melanoma	B16 cells		CVCL_F936
Experiment 16 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 40 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 17 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 40 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Osteosarcoma	HOS cells		CVCL_0312
Experiment 18 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 40 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 19 Reporting the Activity Date of This ADC					[32]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 40 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Neuroblastoma	NGP-127 cells		CVCL_UF75
Experiment 20 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.09 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Thymoma	EL4 cells		CVCL_0255
Experiment 21 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.14 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Amelanotic melanoma	COLO 38 cells		CVCL_3934
Experiment 22 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.15 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Neuroblastoma	IMR-32 cells		CVCL_0346
Experiment 23 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.2 nM	Moderate GD2 expression (GD2++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Pleural malignant mesothelioma	MS-1 [Human mesothelioma] cells		CVCL_E993
Experiment 24 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.22 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Amelanotic melanoma	B78-D14 cells		Homo sapiens
Experiment 25 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.23 nM	High GD2 expression (GD2+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Glioblastoma	T98G cells		CVCL_0556
Experiment 26 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.28 nM	Moderate GD2 expression (GD2++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Osteosarcoma	U2OS cells		CVCL_0042
Experiment 27 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.38 nM	Moderate GD2 expression (GD2++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Invasive breast carcinoma	Hs 578T cells		CVCL_0332
Experiment 28 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.48 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Astrocytoma	1321N1 cells		CVCL_0110
Experiment 29 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	0.51 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Bone marrow neuroblastoma	SH-SY5Y cells		CVCL_0019
Experiment 30 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	2.7 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Amelanotic melanoma	A375 cells		CVCL_0132
Experiment 31 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	2.98 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Osteosarcoma	MG-63 cells		CVCL_0426
Experiment 32 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	3 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 33 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	8.47 nM	Low GD2 expression (GD2+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 34 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	17 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Melanoma	B16 cells		CVCL_F936
Experiment 35 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	> 20 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Malignant neoplasms of the mouse mammary gland	M3 cells		CVCL_4Y25
Experiment 36 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	> 20 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 37 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	> 20 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Osteosarcoma	HOS cells		CVCL_0312
Experiment 38 Reporting the Activity Date of This ADC					[32]
Efficacy Data	20% Maximal Inhibitory Concentration (IC20)	> 20 nM	Negative GD2 expression (GD2-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Neuroblastoma	NGP-127 cells		CVCL_UF75

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.30%	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64.72%	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (2 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.72%	Moderate HER2 expression (HER2++)
Method Description	JIMT-1 Cells of 5,000,000 suspended in 50 uL cold-saline were implanted intoright hind leg of balb/c-nude mouse. When the tumor volume reaches to about 200 mm3, mice having average valuewere selected and grouped according to tumor volume. Then, mice were treated with PBs (vehicle control), or ADCs (5 mg/kg, single).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 67.63%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	68%	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Effective Concentration (EC50)	24 nM	Positive Tissue factor expression (TF+++/++; 380,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    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					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (25A3-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 69.34%	High HER2 expression (HER2 +++)
Method Description	An NCI-N87 xenograft model of HER2-positive gastric cancer cells in BALB/c nude mice was designed to assess the efficacy of ADC in vivo. The mice were given vehicle, mil40, or ADC (5 mg/kg) on days 0, 7, 14, and 21.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.21%	High HER2 expression (HER2 +++)
Method Description	An NCI-N87 xenograft model of HER2-positive gastric cancer cells in BALB/c nude mice was designed to assess the efficacy of ADC in vivo. The mice were given vehicle, mil40, or ADC (10 mg/kg) on days 0, 7, 14, and 21.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	High HER2 expression (HER2 +++)
Method Description	Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	High HER2 expression (HER2 +++)
Method Description	Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	High HER2 expression (HER2 +++)
Method Description	Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	97.62 nM	Negative HER2 expression (HER2-)
Method Description	Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 5 Reporting the Activity Date of This ADC					[33]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	110.54 nM	Negative HER2 expression (HER2-)
Method Description	Cells (33000 cells/well) were added to each well of 384-well plates and incubated at 37°C overnight, after which 10 uL of compound aliquots were added to the assay plate.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	70%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Effective Concentration (EC50)	42 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (43B1-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 70.42%	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					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	50.00 - 500.00 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					[34]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 72.92%	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					[34]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	50.00 - 500.00 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)	≈ 73.19%	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 HLvM4 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					[20]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.33%	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 HLvM4 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					[20]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	40.53 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					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 74.65%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 75%	Low HER2 expression (HER2+)
Method Description	1A3-MMAE=5 mg/kg.
In Vivo Model	MCF7 breast cancer xenograft model
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[35]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Low HER2 expression (HER2+)
Method Description	1A3-MMAE=5 mg/kg.
In Vivo Model	MCF7-F breast cancer xenograft model
In Vitro Model	Invasive breast carcinoma	MCF7-F (fulvestrant resistant) cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.50%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	60 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.82%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.97%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 78.90%	Positive CD56 expression (CD56 +++/++)
Method Description	One or two weeks later until the tumor sizes reached about 200 mm3, the mice were divided into four groups, with 6-7 mice in each group. Promiximab-MMAE (2.5 mg/kg), Promiximab (10 mg/kg) and a control (vehicle) were administered via tail vein into the mice every three days, with a total of three times.
In Vivo Model	NCI-H69 CDX model
In Vitro Model	Small cell lung carcinoma	NCI-H69 cells		CVCL_1579
Experiment 2 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.50%	Positive CD56 expression (CD56 +++/++)
Method Description	One or two weeks later until the tumor sizes reached about 200 mm3, the mice were divided into four groups, with 6-7 mice in each group. Promiximab-MMAE (5 mg/kg), Promiximab (10 mg/kg) and a control (vehicle) were administered via tail vein into the mice every three days, with a total of three times.
In Vivo Model	NCI-H69 CDX model
In Vitro Model	Small cell lung carcinoma	NCI-H69 cells		CVCL_1579
Experiment 3 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 90%	Positive CD56 expression (CD56 +++/++)
Method Description	One or two weeks later until the tumor sizes reached about 200 mm3, the mice were divided into four groups, with 6-7 mice in each group. Promiximab-MMAE (10 mg/kg), Promiximab (10 mg/kg) and a control (vehicle) were administered via tail vein into the mice every three days, with a total of three times.
In Vivo Model	NCI-H526 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 4 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91%	Positive CD56 expression (CD56 +++/++)
Method Description	One or two weeks later until the tumor sizes reached about 200 mm3, the mice were divided into four groups, with 6-7 mice in each group. Promiximab-MMAE (10 mg/kg), Promiximab (10 mg/kg) and a control (vehicle) were administered via tail vein into the mice every three days, with a total of three times.
In Vivo Model	NCI-H526 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 5 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive CD56 expression (CD56 +++/++)
Method Description	One or two weeks later until the tumor sizes reached about 200 mm3, the mice were divided into four groups, with 6-7 mice in each group. Promiximab-MMAE (10 mg/kg), Promiximab (10 mg/kg) and a control (vehicle) were administered via tail vein into the mice every three days, with a total of three times.
In Vivo Model	NCI-H526 CDX model
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 6 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive CD56 expression (CD56 +++/++)
Method Description	One or two weeks later until the tumor sizes reached about 200 mm3, the mice were divided into four groups, with 6-7 mice in each group. Promiximab-MMAE (10 mg/kg), Promiximab (10 mg/kg) and a control (vehicle) were administered via tail vein into the mice every three days, with a total of three times.
In Vivo Model	NCI-H69 CDX model
In Vitro Model	Small cell lung carcinoma	NCI-H69 cells		CVCL_1579

Experiment 1 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive CD56 expression (CD56 +++/++)
Method Description	SCLC cell lines and human NK cells were treated with various concentrations of Promiximab and Promiximab-MMAE for 72 h.
In Vitro Model	Small cell lung carcinoma	NCI-H69 cells		CVCL_1579
Experiment 2 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.23 nM	Positive CD56 expression (CD56 +++/++)
Method Description	SCLC cell lines and human NK cells were treated with various concentrations of Promiximab and Promiximab-MMAE for 72 h.
In Vitro Model	Lung small cell carcinoma	NCI-H526 cells		CVCL_1569
Experiment 3 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19.24 nM	Positive CD56 expression (CD56 +++/++)
Method Description	SCLC cell lines and human NK cells were treated with various concentrations of Promiximab and Promiximab-MMAE for 72 h.
In Vitro Model	Lung small cell carcinoma	NCI-H524 cells		CVCL_1568
Experiment 4 Reporting the Activity Date of This ADC					[36]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1200 nM	Negative CD56 expression (CD56 -)
Method Description	SCLC cell lines and human NK cells were treated with various concentrations of Promiximab and Promiximab-MMAE for 72 h.
In Vitro Model	Normal	NK cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 79.49%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80%	High HER2 expression (HER2+++)
Method Description	Mil40-12b induces efficient tumor cell killing in cell PDX models from a breast cancer patient with HER2 expression.
In Vivo Model	Breast ductal carcinoma CDX model
In Vitro Model	Breast ductal carcinoma	Breast ductal carcinoma cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	25.8 pM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
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)	53.6 pM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	102.6 pM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	207.4 pM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.52 nM	Negative HER2 expression (HER2-)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 6 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26.44 nM	Negative HER2 expression (HER2-)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[38]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80%	High PIEZO1 expression (PIEZO1+++)
Method Description	1 x107 TE1 cells were suspended in Matrigel and injected subcutaneously in the right armpit. The treatment of AntiPIEZO1MMAE or control reagents started when the tumor volume reached 300mm3. Treatments for each group were given every 3 days in total four times.
In Vivo Model	Esophageal squamous cell carcinoma CDX model
In Vitro Model	Esophageal squamous cell carcinoma	Esophageal squamous cell carcinoma cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.21%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 80.63%	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					[34]
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					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 81.85%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.83%	Positive HER2 expression (HER2+++/++)
Method Description	Nude mice were implanted with SK-OV-3 tumor cells which were allowed to establish tumors of ~150 mm3 prior to initiation of treatment. ADCs at 10 mg/kg doses were injected through tail vein on days 38, 45, 52 and 59. There were ~10 mice per group. The tumor volume of mice in different group was measured and their survival was recorded.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.7 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 83.10%	High SLITRK6 expression (SLITRK6+++; IHC H-score=280)
Method Description	CDX models were established by subcutaneous injection of between 2 and 10 million SW780, RT4 (ATCC) or NCI-H322M (NCI) cells in SCID mice. When the tumor volume reached approximately 230 mm3, a single dose of Ha15-10ac14E, 5 mg/kg intravenously, was administered intravenously (iv) to the mice.
In Vivo Model	Bladder cancer CDX model
In Vitro Model	Bladder cancer	Bladder cancer cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.40%	Positive ITGA5 expression (ITGA5 +++/++)
Method Description	Mice were administered a single 3 mg/kg IP dose once tumors reached 100 mm3 and tumor size was measured at various time points.
In Vivo Model	HPAF-II CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.10%	Positive ITGA5 expression (ITGA5 +++/++)
Method Description	Mice were administered a single 3 mg/kg IP dose once tumors reached 100 mm3 and tumor size was measured at various time points.
In Vivo Model	Detroit 562 CDX model
In Vitro Model	Pharyngeal squamous cell carcinoma	Detroit 562 cells		CVCL_1171

Experiment 1 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	86.91%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huAD208.4.1-vcMMAE-DAR4 (3 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.40%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 2 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[41]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 87.50%	Positive PSMA expression (PSMA +++/++)
Method Description	In order to specify the pharmacological properties of MMAE.VC.SA.617 we inoculated LNCaP cells into NOD/SCID mice to generate a xenograft model. In vivo therapeutic efficacy studies were conducted with MMAE.VC.SA.617, namely 1.0 mg/kg (corresponding to 0.49 mg MMAE).
In Vivo Model	LNCaP CDX model
In Vitro Model	Prostate carcinoma	LNCaP cells		CVCL_0395

Experiment 1 Reporting the Activity Date of This ADC					[42]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.80%	High GSDME expression (GSDME +++)
Method Description	Comparison of the maximum tested dose of mesoADC (4.4 mg/kg) to PBS vehicle or isotype control ADC confirmed the antitumor effectiveness of the ADC up to day 18 .
In Vivo Model	EMT6 CDX model
In Vitro Model	Mammary gland malignant neoplasms	EMT6 cells		CVCL_1923

Experiment 1 Reporting the Activity Date of This ADC					[42]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.25 ug/mL	High GSDME expression (GSDME +++)
Method Description	EMT6 cells were pulsed with 1 ug/mL mesoADC for 30min then chased for 30 and 60min at 37°C.
In Vitro Model	Mammary gland malignant neoplasms	EMT6 cells		CVCL_1923
Experiment 2 Reporting the Activity Date of This ADC					[42]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.5 ug/mL	Low GSDME expression (GSDME +)
Method Description	CT26 cells were pulsed with 1 ug/mL mesoADC for 30min then chased for 30 and 60min at 37°C.
In Vitro Model	Colon carcinoma	CT26 cells		CVCL_7254

Experiment 1 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.93%	Positive ITGA5 expression (ITGA5 +++/++)
Method Description	Mice were administered a single 3 mg/kg IP dose once tumors reached 100 mm3 and tumor size was measured at various time points.
In Vivo Model	Detroit 562 CDX model
In Vitro Model	Pharyngeal squamous cell carcinoma	Detroit 562 cells		CVCL_1171
Experiment 2 Reporting the Activity Date of This ADC					[40]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 88.94%	Positive ITGA5 expression (ITGA5 +++/++)
Method Description	Mice were administered a single 3 mg/kg IP dose once tumors reached 100 mm3 and tumor size was measured at various time points.
In Vivo Model	HPAF-II CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313

Experiment 1 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 89.73%	Positive ALPPL2 expression (ALPPL2+++/++)
Method Description	Nude mice were subcutaneously (s.c.) implanted with one million M28 cells. When the average tumor volume reached 250 mm3, the mice were randomized into three study groups and treated intravenously (i.v.) with M25ADCMMAF for 3 mg/kg very four days for a total of 5 doses.
In Vivo Model	M28 CDX model
In Vitro Model	Pleural malignant mesothelioma	M28K cells		CVCL_8106
Experiment 2 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.89%	Positive ALPPL2 expression (ALPPL2+++/++)
Method Description	Nude mice were subcutaneously (s.c.) implanted with one million M28 cells. When the average tumor volume reached 250 mm3, the mice were randomized into three study groups and treated intravenously (i.v.) with M25ADCMMAF for 5 mg/kg very four days for a total of 5 doses.
In Vivo Model	M28 CDX model
In Vitro Model	Pleural malignant mesothelioma	M28K cells		CVCL_8106

Experiment 1 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.3 nM	Positive ALPPL2 expression (ALPPL2+++/++)
Method Description	Anti-ALPPL2 ADC and control ADC were assessed for cytotoxicity in vitro against mesothelioma (M28 and VAMT-1) and control cells (normal human fibroblasts, kidney cells, and primary liver cells).
In Vitro Model	Pleural malignant mesothelioma	M28K cells		CVCL_8106
Experiment 2 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.44 nM	Positive ALPPL2 expression (ALPPL2+++/++)
Method Description	Anti-ALPPL2 ADC and control ADC were assessed for cytotoxicity in vitro against mesothelioma (M28 and VAMT-1) and control cells (normal human fibroblasts, kidney cells, and primary liver cells).
In Vitro Model	Pleural sarcomatoid mesothelioma	VAMT-1 cells		CVCL_A731
Experiment 3 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Positive ALPPL2 expression (ALPPL2+++/++)
Method Description	Anti-ALPPL2 ADC and control ADC were assessed for cytotoxicity in vitro against mesothelioma (M28 and VAMT-1) and control cells (normal human fibroblasts, kidney cells, and primary liver cells).
In Vitro Model	Normal	HS-27 cells		CVCL_0E34
Experiment 4 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Positive ALPPL2 expression (ALPPL2+++/++)
Method Description	Anti-ALPPL2 ADC and control ADC were assessed for cytotoxicity in vitro against mesothelioma (M28 and VAMT-1) and control cells (normal human fibroblasts, kidney cells, and primary liver cells).
In Vitro Model	Normal	HS775Li cells		Homo sapiens
Experiment 5 Reporting the Activity Date of This ADC					[43]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Positive ALPPL2 expression (ALPPL2+++/++)
Method Description	Anti-ALPPL2 ADC and control ADC were assessed for cytotoxicity in vitro against mesothelioma (M28 and VAMT-1) and control cells (normal human fibroblasts, kidney cells, and primary liver cells).
In Vitro Model	Normal	HK-2 [Human kidney] cells		CVCL_0302

Experiment 1 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Tumor Growth Inhibition value (TGI)	90.12%	High LRRC15 expression (LRRC15+++; IHC 3+)
Method Description	LRRC15 expression on stromal cells asassessed by IHC in an untreated xenograft tumor of 200-800 mm in volume, representative for eachxenograft model. In vivo activity of huAD208.14.1-vcMMAE-DAR4 (3 mg/kg) was demonstrated in EBC-1 xenografts.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891

Experiment 1 Reporting the Activity Date of This ADC					[44]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.20%	Positive MRC2 expression (MRC2 +++/++)
Method Description	Vehicle (PBS) or 10 mg/kg of A5/158-vc-MMAE were administered into the lateral tail vein of mice twice a week for 2 weeks. Primary tumors were weighed at necropsy.
In Vivo Model	MG-63-mChLuc2 CDX model
In Vitro Model	Osteosarcoma	MG-63 cells		CVCL_0426

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	92%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	99%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	100%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models The A431 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 2 mg/kg for 2 weeks.
In Vivo Model	HPAF-II xenograft model
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 4 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Effective Concentration (EC50)	26 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (39A-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[34]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.91%	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					[34]
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					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.97%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	32 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	39 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.60%	High HER2 expression (HER2+++)
Method Description	The animals were given vehicle, mil40, and ADC on days 0, 7, 14, and 21, and 4 intravenous injections of ADC at doses of 5 mg/kg.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Maximum inhibition efficiency (MIE)	< 10%	Negative HER2 expression (HER2-)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Maximum inhibition efficiency (MIE)	47.80%	Negative HER2 expression (HER2-)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Maximum inhibition efficiency (MIE)	50.50%	High HER2 expression (HER2+++)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Maximum inhibition efficiency (MIE)	87.30%	Moderate HER2 expression (HER2++)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 5 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Maximum inhibition efficiency (MIE)	93.54%	High HER2 expression (HER2+++)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2+++)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Moderate HER2 expression (HER2++)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 8 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	High HER2 expression (HER2+++)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 9 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.74 nM	Negative HER2 expression (HER2-)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 10 Reporting the Activity Date of This ADC					[45]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 nM	Negative HER2 expression (HER2-)
Method Description	HER2 antigen expressing cells or non-expressing cells were seeded in 96-well cell culture plates for 24h before treatment. Cells were treated with 3-fold serially diluted antibody-drug conjugates or free compoundsin duplicate at 10 concentrations.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 94.34%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.45%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.21 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					[21]
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					[46]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95%	High MSLN expression (MSLN+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, qwx3) via the tail vein on Day 0.
In Vivo Model	Oval-CitAR-3 CDX model
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High MSLN expression (MSLN+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (0.75 mg/kg, qwx3) via the tail vein on Day 0.
In Vivo Model	Oval-CitAR-3 CDX model
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High MSLN expression (MSLN+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (1.5 mg/kg, qwx3) via the tail vein on Day 0.
In Vivo Model	Oval-CitAR-3 CDX model
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High MSLN expression (MSLN+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (3 mg/kg, qwx3) via the tail vein on Day 0.
In Vivo Model	Oval-CitAR-3 CDX model
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	High MSLN expression (MSLN+++/++)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Half Maximal Effective Concentration (EC50)	153.5 ng/mL	High MSLN expression (MSLN+++/++)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.28%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	31 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	33 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.28%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 95.79%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.10%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.77%	Positive CD19 expression (CD19+++/++)
Method Description	To establish DOHH1 tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice (Harlan,Indianapolis, IN). When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 4 mg/kg single.
In Vivo Model	DOHH1 CDX model
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[47]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.10%	High AXL expression (AXL+++)
Method Description	Cells were suspended in PBS then injected subcutaneously to the flank of Balb/c female nude mice (46 weeks old). Tumors were measured by caliper every 23 days. Before therapeutic treatment,tumor-bearing mice were staged at initial tumor volume of 100 to 300 mm3 (growth) or 1800 mm3 (regression) and randomized into treatment groups(n = 8). The ADCs were dosed i.v. once weekly,or total twice during entire study.    Click to Show/Hide
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung adenocarcinoma	PC-9 cells		CVCL_B260
Experiment 2 Reporting the Activity Date of This ADC					[47]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.70%	High AXL expression (AXL+++)
Method Description	Cells were suspended in PBS then injected subcutaneously to the flank of Balb/c female nude mice (46 weeks old). Tumors were measured by caliper every 23 days. Before therapeutic treatment,tumor-bearing mice were staged at initial tumor volume of 100 to 300 mm3 (growth) or 1800 mm3 (regression) and randomized into treatment groups(n = 8). The ADCs were dosed i.v. once weekly,or total twice during entire study.    Click to Show/Hide
In Vivo Model	Non-small cell lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	NCI-H1299 cells		CVCL_0060
Experiment 3 Reporting the Activity Date of This ADC					[47]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 98.70%	High AXL expression (AXL+++)
Method Description	Cells were suspended in PBS then injected subcutaneously to the flank of Balb/c female nude mice (46 weeks old). Tumors were measured by caliper every 23 days. Before therapeutic treatment,tumor-bearing mice were staged at initial tumor volume of 100 to 300 mm3 (growth) or 1800 mm3 (regression) and randomized into treatment groups(n = 8). The ADCs were dosed i.v. once weekly,or total twice during entire study.    Click to Show/Hide
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 4 Reporting the Activity Date of This ADC					[47]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.50%	High AXL expression (AXL+++)
Method Description	Cells were suspended in PBS then injected subcutaneously to the flank of Balb/c female nude mice (46 weeks old). Tumors were measured by caliper every 23 days. Before therapeutic treatment,tumor-bearing mice were staged at initial tumor volume of 100 to 300 mm3 (growth) or 1800 mm3 (regression) and randomized into treatment groups(n = 8). The ADCs were dosed i.v. once weekly,or total twice during entire study.    Click to Show/Hide
In Vivo Model	Astrocytic glioblastoma CDX model
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 96.27%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Tumor Growth Inhibition value (TGI)	97%	Low FOLR1 expression (FOLR1+)
Method Description	Cell line-derived xenograft (CDX) models MDA-MB-231 epidermoid carcinoma and the HPAF-II pancreatic carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice Animals were removed from study and euthanized once tumor size reached 1200 mm3 or skin ulceration was evident ADC was dosed weekly at 4 mg/kg for 2 weeks.    Click to Show/Hide
In Vivo Model	MDA-MB-231 cell line xenograft model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Effective Concentration (EC50)	28 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 nM	Low FOLR1 expression (FOLR1+)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to HPAF-II cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 nM	Positive Tissue factor expression (TF+++/++; 570,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to 5-day old cultures of MDA-MB-231 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (29E-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Positive Tissue factor expression (TF+++/++; 380,000 TF receptor copy number)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.02%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.23%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 1 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.64%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg single.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	33 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.76%	Positive HER2 expression (HER2+++/++)
Method Description	Nude mice were implanted with SK-OV-3 tumor cells which were allowed to establish tumors of ~150 mm3 prior to initiation of treatment. ADCs at 10 mg/kg doses were injected through tail vein on days 38, 45, 52 and 59. There were ~10 mice per group. The tumor volume of mice in different group was measured and their survival was recorded.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.3 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.90%	Positive AXL expression (AXL+++/++)
Method Description	In the LCLC-103H xenograft model,therapeutic treatment with a single dose of 1 mg/kg in anti-tumor activity in the AXL-ADC panel.
In Vivo Model	Lung cancer CDX model
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 97.95%	Positive HER2 expression (HER2+++/++)
Method Description	To further evaluate the gsADCs, we determined the in vivo tumor-inhibitory activity in an NCI-N87 nude mice xenograft model. The mice were randomly grouped into 10 groups (n = 5), including a PBS control group, when the tumors grew to 200 mm3. The experimental groups were 3.0 mg/kg gsADCs q3d.
In Vivo Model	NCI-N87 CDX model
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[46]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99%	High MSLN expression (MSLN+++/++)
Method Description	Inoculate mice with gastric cancer cells at 3 million cells/mouse suspended in HBSS/matrigel, in the thoracic mammary fat pad at a volume of 0.2 ml. When tumors have reached a mean tumor volume of 100-250 mm3, they will be grouped. A single treatment will be administered intravenously (2 mg/kg, qwx3) via the tail vein on Day 0.
In Vivo Model	Oval-CitAR-3 CDX model
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[46]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	High MSLN expression (MSLN+++/++)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Ovarian cancer	Oval-CitAR-3 cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[123]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0956&#1770.01 nM	Positive MSLN expression (MSLN+++/++)
Method Description	Oval-Citar-3-MSLN cells with good growth state were added to 96-well cell culture plates (5×104 cells /mL, 100uL/ well) and incubated overnight in a CO2 incubator at 39°C.
In Vitro Model	High grade ovarian serous adenocarcinoma	Oval-Citar-3-MSLN cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[48]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 3 mg/kg to thetail of each mouse.
In Vivo Model	EBC-1 CDX model
In Vitro Model	Lung squamous cell carcinoma	EBC-1 cells		CVCL_2891

Experiment 1 Reporting the Activity Date of This ADC					[48]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were subcutaneously inoculated at a dose of 1,000,000 cells to the right flank region of each female nude mouse (Day 0). On the day 7 of grouping, the antibody-drug conjugate was intravenously administered at doses of 1 mg/kg to thetail of each mouse.
In Vivo Model	NCI-H1703 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive CD70 expression (CD70+++/++)
Method Description	To establish 786-O tumors, 5 x 106 cells were implanted into the right flank of athymic nu/nu female donor mice. When tumors reached ~100 mm3 mice were randomly allocated to treatment groups. The dose of ADC was 0.5 mg/kg.
In Vivo Model	786-O CDX model
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	An in vivo therapy experiments with cAC10-9a was undertaken in nude mice with subcutaneous Karpas 299 ALCL tumors. The animals (5 per group)were treated with a single intravenous dose of cAC10-9a at 3 mg/kg (mAb component) on day 14.
In Vivo Model	Karpas-299 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					[14]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	An in vivo therapy experiments with cAC10-9a was undertaken in nude mice with subcutaneous Karpas 299 ALCL tumors. The animals (5 per group)were treated with a single intravenous dose of cAC10-9a at 1 mg/kg (mAb component) on day 14.
In Vivo Model	Karpas-299 CDX model
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 3 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	An in vivo therapy experiments with cAC10-9a was undertaken in nude mice with subcutaneous Karpas 299 ALCL tumors. The animals (5 per group)were treated with a single intravenous dose of cAC10-9a at 0.75 mg/kg (mAb component) on day 14.
In Vivo Model	Karpas-299 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					[14]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 50 nM	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 3 Reporting the Activity Date of This ADC					[14]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 55 nM	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[49]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive RON expression (RON +++/++)
Method Description	Treatment began when tumors reached a mean tumor volume of 100 to 150 mm3. Zt/g4-MMAE or Zt/g4-DM1 at 20 mg/kg in a Q12 2 regimen was injected through the tail vein.
In Vivo Model	BxPC3 CDX model
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	Positive MUC16 expression (MUC16 +++/++)
Method Description	In vivo efficacy of MUC16 targeting ADCs in the Ovcar3 tumor model. 3A5-mc-VC-PAB-MMAE ADC dosed at 5 mg/kg (in each study with the exact dosing for control) IV in SCID mice.
In Vivo Model	OVCR-3 CDX model
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.82 nM	Positive MUC16 expression (MUC16 +++/++)
Method Description	Cells were seeded in 96 well plates at 3000 cells per well in complete growth media and grown overnight. For cell viability curves, serially diluted conjugates or payloads were added to the cells at final concentrations ranging from 300 nM to 5 pM and incubated for 8 days.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[50]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative MUC16 expression (MUC16-)
Method Description	Cells were seeded in 96 well plates at 3000 cells per well in complete growth media and grown overnight. For cell viability curves, serially diluted conjugates or payloads were added to the cells at final concentrations ranging from 300 nM to 5 pM and incubated for 8 days.
In Vitro Model	Normal	HEK293 cells		CVCL_0045

Experiment 1 Reporting the Activity Date of This ADC					[51]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High EGFR expression (EGFR+++)
Method Description	For the tumor xenograft model, 5.0x106 MDA-MB-468 cells or 3.0x106 MDA-MB-231 cells were injected subcutaneously into the right flank of each 6 week-old female BALB/c nude mice. when the tumor volumes reached approximately 100 mm3 (approximately 8 days), the 24 mice were randomly divided into 4 groups (6 mice per group): control group, LR004 antibody group, LR004-VC-MMAE group, and doxorubicin (positive control) group, which were treated with PBS or different drugs (LR004 antibody 10 mg/kg, LR004-VC-MMAE 10 mg/kg, doxorubicin 2 mg/kg) every 5 days for 4 times through i.v. injections.    Click to Show/Hide
In Vivo Model	Triple-negative breast cancer CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	53.68%	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (0.5 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	89.84%	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (2 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.23 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.27 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.33 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	64.86%	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (2 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	95.44%	Positive HER2 expression (HER2+++/++)
Method Description	JIMT-1 cells of the best condition that the viability was more than 95% were used for implantation. Cells of 5x 106 suspended in 50 L cold-saline were implanted into right hind leg of balb/c-nude mouse.Then, mice were treated with PBS (vehicle control), or ADCs (5 mg/kg).
In Vivo Model	JIMT-1 CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3 nM	Positive Tissue factor expression (TF+++/++; 320,000 TF receptor copy number)
Method Description	Antibody-dependent cellular cytotoxicity (ADCC) A431 cells were plated on a microtiter plate The following day, the cells were incubated with a ten-point 1:3 dilution titration of anti-TF antibodies or the ADCs starting at 50 nM An ADCC effector-to-target cell ratio of 8:1 was added to each well and incubated for 6 h at 37°C Luciferase Assay Reagent was added to each well to measure luminescence on an Envision plate reader Antibody-dependent cellular cytotoxicity (ADCC) reporter luminescence was evaluated after a 6-hour incubation of the reporter Jurkat cell line with TF-positive A431 cells and a titration of anti-TF antibody or ADC The ADCC reporter luminescence EC50 values for each anti-TF antibody or ADC are listed.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Low FOLR1 expression (FOLR1+)
Method Description	A431 cells were pre-incubated for 30 min without or with 50 nM of FVIIa prior to the addition of an anti-TF ADC (54E-vc-MMAE) titration After a 4 h incubation at 37°C, the FVIIa and ADC were washed out and the cells were cultured for another 68 h before cell viability assessment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Low FOLR1 expression (FOLR1+)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 4-hour incubation followed by removal of excess ADC and culture for another 68 hours This treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 nM	Low FOLR1 expression (FOLR1+)
Method Description	To evaluate ADC cytotoxicity, cells were plated in 384-well plates Anti-TF antibodies conjugated to MC-vc-PAB-MMAE were serially diluted as shown Plates were incubated for 3 days, followed by lysis in CTG assay reagent For each ADC, the IC50 and its associated 95% confidence interval (95% CI) were calculated Titrations of the TF-specific ADCs were added to A431 cells, with a 72-hour incubationThis treatment resulted in efficacious cell killing.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[53]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 1.98 ng/mL	Positive HER3 expression (HER3+++/++)
Method Description	Cells were plated in 96-well flat-bottom plates the day before starvation in 1% FCS for 24hr. HER3-ADC at different dilutions was then added for 5 days, with 50ng/ml NRG1. In the absence of NRG1 stimulation, cells were maintained in 10% FCS and treated with HER3-ADC.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[54]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 82.10%	Positive ST14 expression (ST14+++/++)
Method Description	Five thousand cells per well were plated in RPMI 1,640 media supplemented with 10% FBS. After overnight culture, media was removed and fresh media containing the ADC was added and incubated for different time periods.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 2 Reporting the Activity Date of This ADC					[54]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.29 ug/mL	Positive ST14 expression (ST14+++/++)
Method Description	Five thousand cells per well were plated in RPMI 1,640 media supplemented with 10% FBS. After overnight culture, media was removed and fresh media containing the ADC was added and incubated for different time periods.
In Vitro Model	Mantle cell lymphoma	Mino cells		CVCL_1872
Experiment 3 Reporting the Activity Date of This ADC					[54]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.2 ug/mL	Positive ST14 expression (ST14+++/++)
Method Description	Five thousand cells per well were plated in RPMI 1,640 media supplemented with 10% FBS. After overnight culture, media was removed and fresh media containing the ADC was added and incubated for different time periods.
In Vitro Model	Mantle cell lymphoma	MAVER-1 cells		CVCL_1831
Experiment 4 Reporting the Activity Date of This ADC					[54]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.69 ug/mL	Positive ST14 expression (ST14+++/++)
Method Description	Five thousand cells per well were plated in RPMI 1,640 media supplemented with 10% FBS. After overnight culture, media was removed and fresh media containing the ADC was added and incubated for different time periods.
In Vitro Model	Mantle cell lymphoma	Z-138 cells		CVCL_B077
Experiment 5 Reporting the Activity Date of This ADC					[54]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.78 ug/mL	Positive ST14 expression (ST14+++/++)
Method Description	Five thousand cells per well were plated in RPMI 1,640 media supplemented with 10% FBS. After overnight culture, media was removed and fresh media containing the ADC was added and incubated for different time periods.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865

Experiment 1 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	8%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 2 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	65%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 3 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	72%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 4 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	80%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 5 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	84%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 6 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	87%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 7 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 8 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 9 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 10 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	162 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 11 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 2000 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 12 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.32 uM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	32%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	72%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 3 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	78%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 4 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	79%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 5 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	80%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 6 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	86%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 7 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 8 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 9 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 10 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 11 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	31 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 12 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 2000 nM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	33%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 2 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	72%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 3 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	83%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 4 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	83%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 5 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	86%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 6 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	88%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 7 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 8 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 9 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 10 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	104 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 11 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.1 uM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 12 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.64 uM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059

Experiment 1 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	36%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	74%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 3 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	76%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 4 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	85%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 5 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	85%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 6 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	90%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 7 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	28 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 8 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	60 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 9 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	64 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 10 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	369 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 11 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	678 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 12 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 2000 nM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	41%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	71%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 3 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	77%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 4 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	78%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 5 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	81%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 6 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	85%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 7 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 8 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 9 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 10 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 11 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	27 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 12 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 2000 nM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	46%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	75%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 3 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	76%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 4 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	78%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 5 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	80%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 6 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	81%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 7 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 8 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 9 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 10 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 11 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	25 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 12 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.37 uM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	48%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	77%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 3 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	84%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 4 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	87%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 5 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	87%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 6 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	88%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 7 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 8 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 9 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 10 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	56 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 11 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	215 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 12 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.62 uM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	50%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	70%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 3 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	75%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 4 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	80%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 5 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	80%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 6 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	85%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 7 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 8 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 9 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 10 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 11 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 12 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.41 uM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	69%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	73%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 3 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	83%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 4 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	85%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 5 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	87%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 6 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	95%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 7 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 8 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 9 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 10 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 11 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	52 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 12 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	856 nM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	74%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 2 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	81%	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132
Experiment 3 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	84%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 4 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	87%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 5 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	89%	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 6 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Maximum inhibition efficiency (MIE)	93%	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 7 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	COLO 853 cells		CVCL_2003
Experiment 8 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-28 cells		CVCL_0526
Experiment 9 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 10 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	52 nM	Moderate CD228 expression (CD228++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 11 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100 nM	Positive CD228 expression (CD228+++/++)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Melanoma	IGR-37 cells		CVCL_2075
Experiment 12 Reporting the Activity Date of This ADC					[55]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.14 uM	Low CD228 expression (CD228+)
Method Description	Tumor cells were incubated with CD228 antibody-drug conjugates comprising theindicated anti-CD228 antibody, a linker, and MMAE for 96-144 hours at 37 . Cell viability was measured using Cell Titer Glo according to manufacturer's instructions.
In Vitro Model	Amelanotic melanoma	A-375 cells		CVCL_0132

Experiment 1 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Max inhibition rate (MIR)	89%	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 2 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Max inhibition rate (MIR)	96%	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 3 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 4 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.63 nM	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 5 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 70 nM	Negative PSMA expression (PSMA-)
Method Description	DU-145 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105

Experiment 1 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Max inhibition rate (MIR)	90%	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 2 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Max inhibition rate (MIR)	96%	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 3 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.33 nM	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 4 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.28 nM	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 5 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 70 nM	Negative PSMA expression (PSMA-)
Method Description	DU-145 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105

Experiment 1 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Max inhibition rate (MIR)	90%	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 2 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Max inhibition rate (MIR)	96%	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 3 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 4 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.6 nM	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 5 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 70 nM	Negative PSMA expression (PSMA-)
Method Description	DU-145 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105

Experiment 1 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Max inhibition rate (MIR)	91%	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 2 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Max inhibition rate (MIR)	97%	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 3 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.39 nM	Positive PSMA expression (PSMA+++/++)
Method Description	LNCaP C4-2 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Lymph node metastasis of prostate carcinoma	LNCaP C4-2 cells		CVCL_4782
Experiment 4 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.28 nM	Negative PSMA expression (PSMA-)
Method Description	To assess the sensitivity towards cathepsin B, the ADCs were treated for 2 minutes and 4 hours with activated cathepsin B. To measure release of the respective free toxins DUBA or MMAE, PSMA-negative DU-145 cells (1,000 cells/well) was cultured with the ADCs for 6 days,and the cell viability was measured after 6 days using the CellTiter-GloTM (CTG) assay kit.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 5 Reporting the Activity Date of This ADC					[56]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 70 nM	Negative PSMA expression (PSMA-)
Method Description	DU-145 cells were incubated with increasing concentrations of each ADCs at 37°C for 6 days in complete culture medium.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105

Experiment 1 Reporting the Activity Date of This ADC					[57]
Efficacy Data	Inhibition rate (50 nM)	90%	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[57]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.7 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[57]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 20 nM
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Normal	NHEK-iPSCs #1 cells		CVCL_A4HY
Experiment 4 Reporting the Activity Date of This ADC					[57]
Efficacy Data	80% Effective Dose (ED80)	3.6 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[57]
Efficacy Data	Inhibition rate (50 nM)	91%	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[57]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[57]
Efficacy Data	Half Maximal Effective Concentration (EC50)	5.9 nM
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Normal	NHEK-iPSCs #1 cells		CVCL_A4HY
Experiment 4 Reporting the Activity Date of This ADC					[57]
Efficacy Data	80% Effective Dose (ED80)	4.4 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[57]
Efficacy Data	Inhibition rate (50 nM)	92%	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[57]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.1 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[57]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1 nM
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Normal	NHEK-iPSCs #1 cells		CVCL_A4HY
Experiment 4 Reporting the Activity Date of This ADC					[57]
Efficacy Data	80% Effective Dose (ED80)	0.7 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[57]
Efficacy Data	Inhibition rate (50 nM)	93%	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[57]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.4 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[57]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 19 nM
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Normal	NHEK-iPSCs #1 cells		CVCL_A4HY
Experiment 4 Reporting the Activity Date of This ADC					[57]
Efficacy Data	80% Effective Dose (ED80)	2.1 nM	High EGFR expression (EGFR+++/++); Low MET expression (MET-)
Method Description	Cells were plated in 96-well tissue culture plates (SigmaAldrich) 1 day before treatment, serum-starved, and treated with serially diluted antibodies (0-167 nM in starvation medium) for 1 h.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[58]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.6 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-8 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[58]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.5 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-8 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Hodgkin lymphoma	L-540 cells		CVCL_1362
Experiment 3 Reporting the Activity Date of This ADC					[58]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.2 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-8 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Anaplastic large cell lymphoma	SU-DHL-1 cells		CVCL_0538
Experiment 4 Reporting the Activity Date of This ADC					[58]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.1 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-8 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002

Experiment 1 Reporting the Activity Date of This ADC					[58]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.4 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-7 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[58]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.4 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-7 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Hodgkin lymphoma	L-540 cells		CVCL_1362
Experiment 3 Reporting the Activity Date of This ADC					[58]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.2 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-7 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Adult acute myeloid leukemia	HL-60 cells		CVCL_0002
Experiment 4 Reporting the Activity Date of This ADC					[58]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.5 pM	High CD30 expression (CD30+++)
Method Description	The inhibitory activity of Brentuximab-7 against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Anaplastic large cell lymphoma	SU-DHL-1 cells		CVCL_0538

Experiment 1 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.7 pM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[60]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[60]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	16 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17.9 pM	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 2 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	98 pM	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 3 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 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 4 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.6 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	KMS-12-BM cells		CVCL_1334
Experiment 5 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	30.1 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 6 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	46.1 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 7 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	60.9 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-My7 cells		CVCL_E333
Experiment 8 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 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 9 Reporting the Activity Date of This ADC					[61]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 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					[61]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14 uM	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 1 Reporting the Activity Date of This ADC					[60]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[60]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20 pM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[60]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22.1 pM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[59]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	27.2 pM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity data for 5-8 on the HER2 overexpressing cell line SK-BR-3. EC50 of TTZ is significantly different from those of all ADCs.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[60]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	28 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[60]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	30 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[60]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	30 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[60]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	32 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[60]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	34 pM	Positive CD30 expression (CD30+++/++)
Method Description	Cells were incubated for 24 h at 37°C with 5% CO2. The cells were treated by addition of ADCs 4a-f, 5a-b and 6a-b, dilution series (50 uL/well) and were then incubated at 37°C/5% CO2 for a further 96 h. Cell viability assays were carried out using CellTiter-Glo Luminescent reagent as per the manufacturers instructions.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	36.4 pM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	41.6 pM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	53.9 pM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	59.9 pM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[62]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	88 pM	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[62]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.9 ng/mL	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[62]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Low HER2 expression (HER2+)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[63]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	High AXL expression (AXL+++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung squamous cell carcinoma	Calu-1 cells		CVCL_0608
Experiment 2 Reporting the Activity Date of This ADC					[63]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High AXL expression (AXL+++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 3 Reporting the Activity Date of This ADC					[63]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Moderate AXL expression (AXL++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 4 Reporting the Activity Date of This ADC					[63]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High AXL expression (AXL+++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 5 Reporting the Activity Date of This ADC					[63]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Moderate AXL expression (AXL++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung adenocarcinoma	PC-9 cells		CVCL_B260
Experiment 6 Reporting the Activity Date of This ADC					[63]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Low AXL expression (AXL+)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 7 Reporting the Activity Date of This ADC					[63]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Low AXL expression (AXL+)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent solution was added with replacing fresh medium, and cells were incubated for an appropriate time.
In Vitro Model	Lung large cell carcinoma	NCI-H460 cells		CVCL_0459
Experiment 8 Reporting the Activity Date of This ADC					[125]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 0.1 nM	High AXL expression (AXL +++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent (Promega, Cat#G111A, WI, USA) solution was added with replacing fresh medium, and cells were incubated for an appropriate time to ensure that the maximum net absorbance was between 0.5 and 1 at 490 nm.    Click to Show/Hide
In Vitro Model	Lung large cell carcinoma	LCLC-103H cells		CVCL_1375
Experiment 9 Reporting the Activity Date of This ADC					[125]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 0.1 nM	High AXL expression (AXL +++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent (Promega, Cat#G111A, WI, USA) solution was added with replacing fresh medium, and cells were incubated for an appropriate time to ensure that the maximum net absorbance was between 0.5 and 1 at 490 nm.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma of no special type	Hs578T cells		CVCL_0332
Experiment 10 Reporting the Activity Date of This ADC					[125]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 0.1 nM	High AXL expression (AXL +++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent (Promega, Cat#G111A, WI, USA) solution was added with replacing fresh medium, and cells were incubated for an appropriate time to ensure that the maximum net absorbance was between 0.5 and 1 at 490 nm.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	PC9 cells		CVCL_B260
Experiment 11 Reporting the Activity Date of This ADC					[125]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 0.1 nM	High AXL expression (AXL +++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent (Promega, Cat#G111A, WI, USA) solution was added with replacing fresh medium, and cells were incubated for an appropriate time to ensure that the maximum net absorbance was between 0.5 and 1 at 490 nm.    Click to Show/Hide
In Vitro Model	Glioblastoma	U87 MG cells		CVCL_0022
Experiment 12 Reporting the Activity Date of This ADC					[125]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 0.1 nM	High AXL expression (AXL +++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent (Promega, Cat#G111A, WI, USA) solution was added with replacing fresh medium, and cells were incubated for an appropriate time to ensure that the maximum net absorbance was between 0.5 and 1 at 490 nm.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 13 Reporting the Activity Date of This ADC					[125]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 0.1 nM	High AXL expression (AXL +++)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent (Promega, Cat#G111A, WI, USA) solution was added with replacing fresh medium, and cells were incubated for an appropriate time to ensure that the maximum net absorbance was between 0.5 and 1 at 490 nm.    Click to Show/Hide
In Vitro Model	Lung squamous cell carcinoma	Calu-1 cells		CVCL_0608
Experiment 14 Reporting the Activity Date of This ADC					[125]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Low AXL expression (AXL+)
Method Description	Tumor cells were plated in 96-well plates at predetermined density, treated with AXL02-MMAE or hIgG1-MMAE for 5-8 days to ensure that the doubling of the cells is sufficient. Then MTS reagent (Promega, Cat#G111A, WI, USA) solution was added with replacing fresh medium, and cells were incubated for an appropriate time to ensure that the maximum net absorbance was between 0.5 and 1 at 490 nm.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 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					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 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					[21]
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	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[64]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.01 nM	High EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR. After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 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 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 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					[21]
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	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 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					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 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					[21]
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	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 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					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[65]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 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 2 Reporting the Activity Date of This ADC					[65]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 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 3 Reporting the Activity Date of This ADC					[65]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.5 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					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.71 nM	Negative HER2 expression (HER2 -)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 6 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.07 nM	Negative HER2 expression (HER2 -)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.31 nM	Negative HER2 expression (HER2 -)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.14 nM	Negative HER2 expression (HER2 -)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[64]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High EGFR expression (EGFR+++)
Method Description	The effect of MMAE-conjugated cetuximab ADCs on the viability of U87 glioblastoma cells that express EGFR.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
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)	0.06 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.71 nM	Negative HER2 expression (HER2-)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 6 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.07 nM	Negative HER2 expression (HER2-)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.02 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
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)	0.05 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	High HER2 expression (HER2+++)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3 x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	23.31 nM	Negative HER2 expression (HER2-)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[37]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24.14 nM	Negative HER2 expression (HER2-)
Method Description	To evaluate the cytotoxicity, multiple tumor cell lines were treated with three generated maleamic methyl ester-based ADCs. Each group was established three holes, tumor cells (3x104 cells/mL) were added to each well of plate after which 10uL of test compounds solution was added.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.49 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 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 3 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.21 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.51 nM	Negative HER2 expression (HER2 -)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 6 Reporting the Activity Date of This ADC					[66]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26.44 nM	Negative HER2 expression (HER2 -)
Method Description	Each group was established three holes, tumor cells (30,000 cells/mL) were added to each well of plate after which 10L of test compounds solution was added. The plates were incubated for seven days at 37°C, then, incubated at RT. Cell Titer Glo reagent (40L) was added to each well, and incubated the plates for another 30min.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[64]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR. After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 2 Reporting the Activity Date of This ADC					[64]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High EGFR expression (EGFR+++)
Method Description	The effect of MMAE-conjugated cetuximab ADCs on the viability of U87 glioblastoma cells that express EGFR.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[64]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR. After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022
Experiment 2 Reporting the Activity Date of This ADC					[64]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	High EGFR expression (EGFR+++)
Method Description	The effect of MMAE-conjugated cetuximab ADCs on the viability of U87 glioblastoma cells that express EGFR.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.49 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[67]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.03 nM	Positive FZD7 expression (FZD7+++/++)
Method Description	Cells were seeded in a 96-well plate the day before drug treatment. MA-148, PA-1, and MA-148 FZD7-KO were incubated with the indicated drugs for 3 days.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells (FZD7 overexpression)		CVCL_0465
Experiment 2 Reporting the Activity Date of This ADC					[67]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	Positive FZD7 expression (FZD7+++/++)
Method Description	Cells were seeded in a 96-well plate the day before drug treatment. MA-148, PA-1, and MA-148 FZD7-KO were incubated with the indicated drugs for 3 days.
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 3 Reporting the Activity Date of This ADC					[67]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 nM	Positive FZD7 expression (FZD7+++/++)
Method Description	Cells were seeded in a 96-well plate the day before drug treatment. MA-148, PA-1, and MA-148 FZD7-KO were incubated with the indicated drugs for 3 days.
In Vitro Model	Ovarian cystadenocarcinoma	MA148 cells		CVCL_AK47
Experiment 4 Reporting the Activity Date of This ADC					[67]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	25 nM	Negative FZD7 expression (FZD7-)
Method Description	Cells were seeded in a 96-well plate the day before drug treatment. MA-148, PA-1, and MA-148 FZD7-KO were incubated with the indicated drugs for 3 days.
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 5 Reporting the Activity Date of This ADC					[67]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	60 nM	Negative FZD7 expression (FZD7-)
Method Description	Cells were seeded in a 96-well plate the day before drug treatment. MA-148, PA-1, and MA-148 FZD7-KO were incubated with the indicated drugs for 3 days.
In Vitro Model	Ovarian cystadenocarcinoma	MA148 cells (FZD7 knock-out)		CVCL_AK47

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[21]
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					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 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					[21]
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					[65]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 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					[65]
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	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[65]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.62 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					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive CD19 expression (CD19+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using Ramos cells for 72hr.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive CD19 expression (CD19+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using Ramos cells for 72hr.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive CD19 expression (CD19+++/++)
Method Description	Ramos cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative CD19 expression (CD19-)
Method Description	K562 cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Chronic myeloid leukemia	K562 cells		CVCL_0004

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.34 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.3 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 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 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 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	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 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 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 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 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 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 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 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 3 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 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	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 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	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 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	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[65]
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					[65]
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	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[65]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 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					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.3 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.35 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.43 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 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					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 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					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 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					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 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					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[65]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 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					[65]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 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					[65]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.78 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					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.37 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 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 3 Reporting the Activity Date of This ADC					[21]
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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were cultured in a 10% fetal bovine serum (FBS)-containing RPMI 1640 medium and were planted into 96-well plates with 6000 cells per well. The plates were incubated overnight at 37°C in a 5% CO2 cell incubator.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive CD19 expression (CD19+++/++)
Method Description	Ramos cells, which are human Burkitt's lymphoma cells, were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative CD19 expression (CD19-)
Method Description	Cells were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Chronic myeloid leukemia	K562 cells		CVCL_0004

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.44 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13.44 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[68]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM
Method Description	Cytotoxicity of non-irradiated or X-ray-irradiated (8 Gy) mAb-DMBA-SIL-MMAE conjugate in comparison to free MMAE in anaplastic thyroid cancer.
In Vitro Model	Thyroid gland anaplastic carcinoma	8505C cells		CVCL_1054

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.64 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[69]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity of MMAE-conjugated trastuzumab I253Q variant. Serial dilutions of trastuzumab variants (0.01 nM to 20 nM) were incubated for 3 days on SK-BR-3 (HER2) cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2 -)
Method Description	Cytotoxicity of MMAE-conjugated trastuzumab I253Q variant. Serial dilutions of trastuzumab variants (0.01 nM to 20 nM) were incubated for 3 days on SK-BR-3 (HER2) cells.
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.64 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 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					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.13 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.38 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.24 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[62]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[62]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21.8 ng/mL	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[62]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Low HER2 expression (HER2+)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.97 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.04 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 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					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.15 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.31 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.97 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 6 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.01 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 7 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 9 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[69]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity of MMAE-conjugated trastuzumab I253Q variant. Serial dilutions of trastuzumab variants (0.01 nM to 20 nM) were incubated for 3 days on SK-BR-3 (HER2) cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2 -)
Method Description	Cytotoxicity of MMAE-conjugated trastuzumab I253Q variant. Serial dilutions of trastuzumab variants (0.01 nM to 20 nM) were incubated for 3 days on SK-BR-3 (HER2) cells.
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030

Experiment 1 Reporting the Activity Date of This ADC					[62]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.16 nM	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[62]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15.4 ng/mL	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[62]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 ug/mL	Low HER2 expression (HER2+)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Moderate EGFR expression (EGFR++)
Method Description	The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative EGFR expression (EGFR-)
Method Description	The cells were incubated at 37°C in 5% CO, for 24 hours. Then, serial dilutions of monomethyl auristatin F ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4after adding 100 L ofice-cold 10% trichloroacetic acid to each well.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 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					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Moderate EGFR expression (EGFR++)
Method Description	The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Low EGFR expression (EGFR+)
Method Description	The cells were incubated at 37°C in 5% CO2, for 24 hours. Then, serial dilutions of ADCs were added to the cells at concentrations of 100 to 0.00128 nM. The cells were incubated for 72 hours and then fixed for 1 hour at 4C afteradding 100 uL of ice-cold 10% trichloroacetic acid to each well.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.17 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.52 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.7 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[70]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.18 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[71]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.18±0.03 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of Fcab-1-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[71]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of Fcab-1-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.4 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of Fcab-1-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.09 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 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					[21]
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 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.63 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.87 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[71]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19±0.05 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of Fcab-2-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[71]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of Fcab-2-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.4 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of Fcab-2-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.01 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[72]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	High FOLR1 expression(FOLR1+++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Ovarian endometrioid adenocarcinoma	IGROV-1 cells		CVCL_1304
Experiment 2 Reporting the Activity Date of This ADC					[72]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative FOLR1 expression(FOLR1-)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Osteosarcoma	SJSA-1 cells		CVCL_1697
Experiment 3 Reporting the Activity Date of This ADC					[72]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Low FOLR1 expression(FOLR1+)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[72]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Moderate FOLR1 expression(FOLR1++)
Method Description	Cells were sub-cultured and seeded at 5,000 cells/well in complete growth medium in 96-well tissue culture plates, and incubated at 37°C, 5% CO2 overnight. Test reagents were serially diluted and added to the cell plates (initial concentration of 100 nM). Plates were incubated at 37°C, 5% CO2 for an additional 3 d.
In Vitro Model	Lung non-small cell carcinoma	NCI-H2110 cells		CVCL_1530

Experiment 1 Reporting the Activity Date of This ADC					[73]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	High ITGA2B expression (ITGA2B+++/++)
Method Description	The MTT-based cytotoxicity assay in MDA-MB-231 cells that displayed a dose dependent cell killing of ADC treatment.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.04 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.34 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 6 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.63 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 8 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 9 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.51 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.79 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.01 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[74]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.2 nM	High HER2 expression (HER2+++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[74]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	High HER2 expression (HER2+++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[74]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	45 nM	Moderate HER2 expression (HER2++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Invasive breast carcinoma	ZR-75-1 cells		CVCL_0588

Experiment 1 Reporting the Activity Date of This ADC					[71]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22±0.01 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of Fcab-3-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[71]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of Fcab-3-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.4 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of Fcab-3-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.26 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.41 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.47 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.69 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 7 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.33 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 8 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	241 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 9 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	275 nM	Positive HER2 expression (HER2+++/++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours were counted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.29 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.04 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.34 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.63 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[75]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.3 nM	High HER2 expression (HER2+++)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[75]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[74]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.3 nM	High HER2 expression (HER2+++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[74]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 nM	High HER2 expression (HER2+++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[74]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	68 nM	Moderate HER2 expression (HER2++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Invasive breast carcinoma	ZR-75-1 cells		CVCL_0588

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.32 nM	Positive HER2 expression (HER2+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using SK-BR3 cells for 72hr.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[71]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.44±0.03 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of C-IgG-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[71]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of C-IgG-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.4 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of C-IgG-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[75]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.46 nM	High HER2 expression (HER2+++)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[75]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	In vitro cytotoxicity of ADCs against a panel of four human breast cancer cell lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.47 nM	High HER2 expression (HER2 +++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.69 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative HER2 expression (HER2-)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	241 nM	High HER2 expression (HER2+++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	275 nM	Moderate HER2 expression (HER2++)
Method Description	Anti-proliferation activities of the antibodies, drugs, and conjugates with regard tothe cancer cell lines were measured. The cells were plated in 96-well, tissue culture platesat 10,000 cells per well. After 24 hour incubation, the antibodies, drugs, and conjugateswere added in various concentrations. The number of viable cells after 72 hours werecounted using SRB assay.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.5 nM	Positive HER2 expression (HER2 +++/++)
Method Description	N87 cells (10000) were seeded in 96-well plates for the IC50 measurements of cell viability. After incubation at 37°C for 16 h, the medium was replaced by fresh normal medium with serum and the cytotoxicity was assessed using the WST-1 reagent after 72 h of incubation at 37°C.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.61 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Neoplasm	Hs 700T cells		CVCL_0858
Experiment 2 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.7 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Amelanotic melanoma	A375.S2 cells		CVCL_0136
Experiment 3 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236
Experiment 4 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.52 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung squamous cell carcinoma	NCI-H1703 cells		CVCL_1490
Experiment 5 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.1 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 6 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.33 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 7 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.1 nM	High CD276 expression (CD276 +++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 8 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20.15 nM	Low CD276 expression (CD276 +)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Prostate carcinoma	DU145 cells		CVCL_0105
Experiment 9 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	26.98 nM	Moderate CD276 expression (CD276 ++)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 10 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative CD276 expression (CD276 -)
Method Description	Briefly, B7-H3-ADCs and controls are diluted and plated intomicrotiter plates, 5000 cells are added to each well and incubated at 37°C for 4-7 daysAlamar Blue Reagent is added to the plates andread according to the manufacturer's protocol. The number of antibody binding sites presenton these cells was determined using a Bangs QFACSTM Kit.
In Vitro Model	EBV-related Burkitt lymphoma	Raji cells		CVCL_0511

Experiment 1 Reporting the Activity Date of This ADC					[68]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.76 nM
Method Description	The inhibitory activity of Alb-DMBA-SIL-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated MMAE is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model	Thyroid gland anaplastic carcinoma	8505C cells		CVCL_1054
Experiment 2 Reporting the Activity Date of This ADC					[68]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2 nM
Method Description	The inhibitory activity of Alb-DMBA-SIL-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated MMAE is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model	Mouse colon adenocarcinoma	MC-38 cells		CVCL_B288
Experiment 3 Reporting the Activity Date of This ADC					[68]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.29 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of Alb-DMBA-SIL-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated MMAE is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model	Acute erythroid leukemia	TBP-3743 cancer cells		Mus musculus
Experiment 4 Reporting the Activity Date of This ADC					[68]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.92 nM
Method Description	The inhibitory activity of Alb-DMBA-SIL-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated MMAE is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model	Oral cavity squamous cell carcinoma	MOC-L2 cells		CVCL_A9X4
Experiment 5 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.4 nM
Method Description	The inhibitory activity of Alb-DMBA-SIL-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro. Caged and conjugated MMAE is selectively cytotoxic and activated by X-ray irradiation.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[71]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.78±0.03 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of C-Fab-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[71]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of C-Fab-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.4 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of C-Fab-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.8 nM	Positive EGFR expression (EGFR +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative EGFR expression (EGFR -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	NCI-H2228 cells		CVCL_1543

Experiment 1 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.89 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	SNU-16, NCI-H716 and U2OS cells were seeded at a density of 5000 cells per well in a 96-well culture plate and treated with vcMMAE, scFvF7-Fc, or antibody-vcMMAE conjugate scFvF7-Fc-MMAE for 96 hours.
In Vitro Model	Gastric adenocarcinoma	SNU-16 cells		CVCL_0076
Experiment 2 Reporting the Activity Date of This ADC					[76]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.7 nM	Positive FGFR2 expression (FGFR2+++/++)
Method Description	SNU-16, NCI-H716 and U2OS cells were seeded at a density of 5000 cells per well in a 96-well culture plate and treated with vcMMAE, scFvF7-Fc, or antibody-vcMMAE conjugate scFvF7-Fc-MMAE for 96 hours.
In Vitro Model	Cecum adenocarcinoma	NCI-H716 cells		CVCL_1581

Experiment 1 Reporting the Activity Date of This ADC					[70]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[77]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00-2.00 nM	Positive KAAG1 expression (KAAG1 +++/++)
Method Description	In vitro cytotoxicity of ADCs against a panel of four multiple human cancer cell lines.
In Vitro Model	Prostate carcinoma	PC-3 cells		CVCL_0035
Experiment 2 Reporting the Activity Date of This ADC					[77]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00-2.00 nM	Positive KAAG1 expression (KAAG1 +++/++)
Method Description	In vitro cytotoxicity of ADCs against a panel of four multiple human cancer cell lines.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[77]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00-2.00 nM	Positive KAAG1 expression (KAAG1 +++/++)
Method Description	In vitro cytotoxicity of ADCs against a panel of four multiple human cancer cell lines.
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[78]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00-10.00 nM	Positive ENPP1 expression (ENPP1 +++/++)
Method Description	For the cell-killing activity of ADC,293T, 293T-ENPP1, and HepG2 cells were seeded at 2000 cells/well in 96-well white plate and incubated in cell growth medium overnight at 37°C in 5%CO2.
In Vitro Model	Hepatoma	HEK293T cells (ENPP1 expression)		CVCL_0063
Experiment 2 Reporting the Activity Date of This ADC					[78]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	100 nM	Positive ENPP1 expression (ENPP1 +++/++)
Method Description	For the cell-killing activity of ADC,293T, 293T-ENPP1, and HepG2 cells were seeded at 2000 cells/well in 96-well white plate and incubated in cell growth medium overnight at 37°C in 5%CO2.
In Vitro Model	Hepatoblastoma	Hep-G2 cells		CVCL_0027
Experiment 3 Reporting the Activity Date of This ADC					[78]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative ENPP1 expression (ENPP1-)
Method Description	For the cell-killing activity of ADC,293T, 293T-ENPP1, and HepG2 cells were seeded at 2000 cells/well in 96-well white plate and incubated in cell growth medium overnight at 37°C in 5%CO2.
In Vitro Model	Normal	HEK293T cells		CVCL_0063

Experiment 1 Reporting the Activity Date of This ADC					[78]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.00-10.00 nM	Positive ENPP1 expression (ENPP1 +++/++)
Method Description	For the cell-killing activity of ADC,293T, 293T-ENPP1, and HepG2 cells were seeded at 2000 cells/well in 96-well white plate and incubated in cell growth medium overnight at 37°C in 5%CO2.
In Vitro Model	Hepatoma	HEK293T cells (ENPP1 expression)		CVCL_0063
Experiment 2 Reporting the Activity Date of This ADC					[78]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	65 nM	Positive ENPP1 expression (ENPP1 +++/++)
Method Description	For the cell-killing activity of ADC,293T, 293T-ENPP1, and HepG2 cells were seeded at 2000 cells/well in 96-well white plate and incubated in cell growth medium overnight at 37°C in 5%CO2.
In Vitro Model	Hepatoblastoma	Hep-G2 cells		CVCL_0027
Experiment 3 Reporting the Activity Date of This ADC					[78]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative ENPP1 expression (ENPP1-)
Method Description	For the cell-killing activity of ADC,293T, 293T-ENPP1, and HepG2 cells were seeded at 2000 cells/well in 96-well white plate and incubated in cell growth medium overnight at 37°C in 5%CO2.
In Vitro Model	Normal	HEK293T cells		CVCL_0063

Experiment 1 Reporting the Activity Date of This ADC					[70]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.45 nM	Negative HER2 expression (HER2-)
Method Description	Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.47 nM	Positive CD20 expression (CD20+++/++)
Method Description	Ramos cells, which are human Burkitt's lymphoma cells, were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[28]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative CD20 expression (CD20-)
Method Description	Cells were seeded in a 96-well plate at 20,000 cells/well in 100 pL of growth media. The cells were incubated at 37°C in5% CO2, for 1 day. Serial dilutions of anti-CD19 ADCs were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Chronic myeloid leukemia	K562 cells		CVCL_0004

Experiment 1 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.47 nM	Positive CD20 expression (CD20+++/++)
Method Description	Ramos cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 2 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 nM	Positive CD20 expression (CD20+++/++)
Method Description	ADCs wereincubated in human plasma for 5 seconds (0h), followed by SRB invitro cytotoxicity test using Ramos cells for 72hr.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 3 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.13 nM	Positive CD20 expression (CD20+++/++)
Method Description	ADCs wereincubated in human plasma for 168 hours (168h), followed by SRB invitro cytotoxicity test using Ramos cells for 72hr.
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597
Experiment 4 Reporting the Activity Date of This ADC					[52]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 33.3 nM	Negative CD20 expression (CD20-)
Method Description	K562 cells were seeded in a 96-wellplate at 20,000 cells/well in 100 uL of growth media. The cells were incubated at 37°C in5% CO, for 1 day. Serial dilutions of ADCs from 33.33 nM to 5.1 pM in 100 uL media were added to the wells, and the cells were incubated with the antibody & ADCs for 72 hours.
In Vitro Model	Chronic myeloid leukemia	K562 cells		CVCL_0004

Experiment 1 Reporting the Activity Date of This ADC					[70]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	2.4 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cells were seeded at 2000 cells per well in black 96-well proliferation plates and dosed with a titration of conjugates for 3 to 5 days, until control untreated cells reached 80 to 90% confluence.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.45 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					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9.13 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					[79]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18.58 nM	Moderate EGFR expression (EGFR++)
Method Description	1 x104 cells per well in a volume of 100 ull 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 4 Reporting the Activity Date of This ADC					[79]
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 1 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.8 nM	Positive HER2 expression (HER2 +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063

Experiment 1 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.2 nM	High HER2 expression (HER2 +++)
Method Description	HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[80]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24 nM	High HER2 expression (HER2 +++)
Method Description	HER2-expressing cell lines were incubated with concentration series of the drug conjugates, and the viability of the cells was measured.
In Vitro Model	Breast adenocarcinoma	AU565 cells		CVCL_1074

Experiment 1 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11.3 nM	Positive HER2 expression (HER2 +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063

Experiment 1 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14 nM	Positive HER2 expression (HER2 +++/++)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	487 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 500 nM	Negative HER2 expression (HER2 -)
Method Description	ADCs 21-23 was performed on HCC827 and NCI-H2228 cells. cells (5 x 103 cells/well) were cultured in 96-well plates with 100 uL complete medium, and 24 h later the cells were treated in triplicate with varying concentrations of ADCs for 72 h.
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063

Experiment 1 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18 nM	Positive CD4 expression (CD4 +++/++)
Method Description	Receptors (R2) as a function of ADC concentrations, upon incubation with the antibody and following additional 48 h.
In Vitro Model	Adult T acute lymphoblastic leukemia	MOLT-4 cells		CVCL_0013
Experiment 2 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22 nM	Positive CD4 expression (CD4 +++/++)
Method Description	Receptors (R1) as a function of ADC concentrations, upon incubation with the antibody and following additional 48 h.
In Vitro Model	Adult T acute lymphoblastic leukemia	MOLT-4 cells		CVCL_0013
Experiment 3 Reporting the Activity Date of This ADC					[81]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	40 nM	Positive CD4 expression (CD4 +++/++)
Method Description	Receptors (R4) as a function of ADC concentrations, upon incubation with the antibody and following additional 48 h.
In Vitro Model	Adult T acute lymphoblastic leukemia	MOLT-4 cells		CVCL_0013

Experiment 1 Reporting the Activity Date of This ADC					[64]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	34 nM	High EGFR expression (EGFR+++)
Method Description	The effect of MMAE-conjugated cetuximab ADCs on the viability of U87 glioblastoma cells that express EGFR.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[29]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	50 nM	Positive MSL expression (MSL+++/++)
Method Description	The cells were incubated in a CO2 incubat or with saturated water overnight, On the second day, two covalent thiol conjugated ADCs were serially diluted conjugates were added to the 96 well plate containing OVCAR3 cells, 100uL per well. The initial conjugate was 100000 ng/ml and diluted to 0.001 ng/ml. OVCAR3 cells with added ADC were incubated at 37 for 72 hours.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[21]
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 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[21]
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 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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					[21]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 66 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 1 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	682.4 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[39]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	382.4 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO2. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[71]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of huFc-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[71]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 300 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of huFc-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[87]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.4 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of huFc-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	265.3 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Lung squamous cell carcinoma	SK-MES-1 cells		CVCL_0630
Experiment 2 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 663.08 nM	Negative PD-L1 expression (PD-L1-)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Pancreatic ductal adenocarcinoma	AsPC-1 cells		CVCL_0152
Experiment 3 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 663.08 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 663.08 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Lung squamous cell carcinoma	Calu-1 cells		CVCL_0608

Experiment 1 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	272.1 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Lung squamous cell carcinoma	SK-MES-1 cells		CVCL_0630
Experiment 2 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 653.93 nM	Negative PD-L1 expression (PD-L1-)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Pancreatic ductal adenocarcinoma	AsPC-1 cells		CVCL_0152
Experiment 3 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 653.93 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 653.93 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 1 and ADC 2 was evaluated in three PD-L1-positive cell lines, i.e., Calu-1, MDA-MB-231, and SK-MES, and one PD-L1-negative cell line, i.e., AsPC-1.
In Vitro Model	Lung squamous cell carcinoma	Calu-1 cells		CVCL_0608

Experiment 1 Reporting the Activity Date of This ADC					[34]
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					[83]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.4 ng/mL	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 ng/mL	Positive CD30 expression (CD30+++/++); Low CD70 expression (CD70+)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	65 ng/mL	Moderate CD30 expression (CD30++); Low CD70 expression (CD70+)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Hodgkin lymphoma	L-428 cells		CVCL_1361
Experiment 4 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Negative CD30 expression (CD30-); Negative CD70 expression (CD70-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Erythroleukemia	HEL 92.1.7 cells		CVCL_2481

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.5 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.7 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.8 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.8 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.8 ng/mL	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324
Experiment 2 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 ng/mL	Positive CD30 expression (CD30+++/++); Low CD70 expression (CD70+)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 3 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 4 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.94 ng/mL	Positive CLDN18.2 expression (CLDN18.2 +++/++)
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 tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	57 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[8]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.23 ng/mL	Positive CLDN18.2 expression (CLDN18.2 +++/++)
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 tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[84]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.7 ng/mL	High HER2 expression (HER2+++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	15 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[84]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.1 ng/mL	High HER2 expression (HER2+++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	9 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	80 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[84]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.1 ng/mL	High HER2 expression (HER2+++)
Method Description	The MTS cell proliferation assay was performed as follows: CellTiter 96 Aqueous Non-Radioactive Cell proliferation Kit is used to determine the number of viable cells in cell proliferation assay. Tumor cells are plated at certain seeding densities in sterile 384-well black clear bottom Matrix plates at 40 uL per well and incubated overnight at 37°C in 5% CO2 before assaying.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	11 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	18 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	22 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	13 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	34 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	17 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	19 ng/mL	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Positive CD70 expression (CD70+++/++); Negative CD30 expression (CD30-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 3 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Positive CD30 expression (CD30+++/++); Low CD70 expression (CD70+)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	Hodgkin's disease	L540cy cells		Homo sapiens
Experiment 4 Reporting the Activity Date of This ADC					[83]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 1000 ng/mL	Positive CD30 expression (CD30+++/++); Negative CD70 expression (CD70-)
Method Description	Cell-based in vitro assays are used to measure viability (proliferation), cytotoxicity,and induction of apoptosis of the ADC of the invention. Culturing the cells for a period from about 6 hours to about 5 days and measuring cell viability.
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	20 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	24 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	21 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	27 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Clear cell renal cell carcinoma	Caki-1 cells		CVCL_0234
Experiment 2 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	28 ng/mL	Positive CD70 expression (CD70+++/++)
Method Description	Log phase cultures of cells were collected and cells plated at seeding densities ranging from 500 - 10,000 cells/well according to pre-determined conditions.After incubating 24 hours to allow surface protein reconstitution, serial dilutions of test conjugates were added and cultures incubated further for 4 days.
In Vitro Model	Renal cell carcinoma	786-O cells		CVCL_1051

Experiment 1 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.14 ug/mL	Positive VEGFA expression (VEGFA +++/++)
Method Description	The anti-proliferative activity of Bevacizumab Vedotin and Bevacizumab against three different cell lines was determined by MTT method.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.65 ug/mL	Positive VEGFA expression (VEGFA +++/++)
Method Description	The anti-proliferative activity of Bevacizumab Vedotin and Bevacizumab against three different cell lines was determined by MTT method.
In Vitro Model	Hepatoblastoma	Hep-G2 cells		CVCL_0027
Experiment 3 Reporting the Activity Date of This ADC					[86]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	14.17 ug/mL	Positive VEGFA expression (VEGFA +++/++)
Method Description	The anti-proliferative activity of Bevacizumab Vedotin and Bevacizumab against three different cell lines was determined by MTT method.
In Vitro Model	Glioblastoma	U-87MG cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Effective Concentration (EC50)	4.55 nM	High FGFR1 expression (FGFR1+++)
Method Description	Human lung cancer cell lines showing FGFR1 overexpression (NCI-H520 and NCI-H1581) was chosen and a cell line with physiological, low levels of FGFR1 (HCC95) was chosen as a control,.
In Vitro Model	Lung large cell carcinoma	NCI-H1581 cells		CVCL_1479
Experiment 2 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Effective Concentration (EC50)	90.49 nM	High FGFR1 expression (FGFR1+++)
Method Description	Human lung cancer cell lines showing FGFR1 overexpression (NCI-H520 and NCI-H1581) was chosen and a cell line with physiological, low levels of FGFR1 (HCC95) was chosen as a control,.
In Vitro Model	Lung squamous cell carcinoma	NCI-H520 cells		CVCL_1566
Experiment 3 Reporting the Activity Date of This ADC					[88]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 1000 nM	Negative FGFR1 expression (FGFR1-)
Method Description	Human lung cancer cell lines showing FGFR1 overexpression (NCI-H520 and NCI-H1581) was chosen and a cell line with physiological, low levels of FGFR1 (HCC95) was chosen as a control,.
In Vitro Model	Lung squamous cell carcinoma	HCC95 cells		CVCL_5137

Experiment 1 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Half Maximal Effective Concentration (EC50)	9.75 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 3 was quickly evaluated in three PD-L1-positive cell lines, ie, MDA-MB-231, PC 9, and A431, and one PD-L1-negative cell line, ie, Romas.
In Vitro Model	Lung adenocarcinoma	PC-9 cells		CVCL_B260
Experiment 2 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Half Maximal Effective Concentration (EC50)	10.33 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 3 was quickly evaluated in three PD-L1-positive cell lines, ie, MDA-MB-231, PC 9, and A431, and one PD-L1-negative cell line, ie, Romas.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[82]
Efficacy Data	Half Maximal Effective Concentration (EC50)	11.94 nM	High PD-L1 expression (PD-L1+++)
Method Description	The in vitro cytotoxicity of ADC 3 was quickly evaluated in three PD-L1-positive cell lines, ie, MDA-MB-231, PC 9, and A431, and one PD-L1-negative cell line, ie, Romas.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Effective Concentration (EC50)	71.6 ng/mL	Positive EGFR expression (EGFR +++/++)
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	Colorectal carcinoma	DiFi cells		CVCL_6895

Experiment 1 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Effective Concentration (EC50)	72.6 ng/mL	Positive EGFR expression (EGFR +++/++)
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	Colorectal carcinoma	DiFi cells		CVCL_6895

Experiment 1 Reporting the Activity Date of This ADC					[89]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[89]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.04 7.13 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[89]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[89]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.05 8.79 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[89]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[89]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.08 12.68 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[89]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[89]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.10 16.05 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.07 10.67 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.41 6.20 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.04 6.08 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.07 11.07 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.04 6.39 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.07 10.67 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.05 7.06 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[90]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.07 11.07 nM ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	-0.70%	Positive TPBG expression (TPBG+++/++)
Method Description	The patient-derived tumor firagments (2mmx2mmx2mm,TPBG positive cells constituted 58.86% and MET positive cells constituted 24.08% of total cells) were engraftedin the right flank of B-NDG mice (Biocytogen Pharmaceuticals (Beijing) Co., Ltd., Cat#: B-CM-002). Treatment with 3mg/kg (QW&#422,i.v.) ADC after tumor volume about 200-300mm3. Determined tumor volume after the experiment, measured at day 28.    Click to Show/Hide
In Vivo Model	TPBG Patient-derived Xenograft Model

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	9.30%
Method Description	Cell line-derived xenograft models were established in B-NDG mice, by subcutaneous injection of 1x106 (NCI-H1975) tumor cells, and treatmen with 1.5mg/kg ADC (QW&#422,i.v.) after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	NCI-H1975 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Tumor Growth lnhibition value (TGl)	10%	High CD79b expression (CD79b +++)
Experiment 2 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Tumor Growth lnhibition value (TGl)	39%	High CD79b expression (CD79b +++)
Experiment 3 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Tumor Growth lnhibition value (TGl)	41%	High CD79b expression (CD79b +++)
Experiment 4 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Tumor Growth lnhibition value (TGl)	93%	High CD79b expression (CD79b +++)

Experiment 1 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	80.6 ng/mL	High CD79b expression (CD79b +++)
Method Description	A certain number of DoHH2 cells in the logarithmic growth phase were seeded into a 96-well culture plate, and drugs at different concentrations were added to the culture plate for reaction for 72 h. After the reaction was completed, an MTT working solution was added for reaction for 6h, then blue-purple crystalline formazan was dissolved with atriplex solution.    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179
Experiment 2 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	116.9 ng/mL	High CD79b expression (CD79b +++)
Method Description	A certain number of DoHH2 cells in the logarithmic growth phase were seeded into a 96-well culture plate, and drugs at different concentrations were added to the culture plate for reaction for 72 h. After the reaction was completed, an MTT working solution was added for reaction for 6h, then blue-purple crystalline formazan was dissolved with atriplex solution.    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179

Experiment 1 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	11.08%
Method Description	Cell line-derived xenograft models were established in nude mice by subcutaneous injection of 1x106 (HT-29) tumor cells, and treatment with 0.4mg/kg 99961.1-MMAE (BIW&#424) was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model	HT-29 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	15.90%
Method Description	Cell line-derived xenograft models were established in nude mice by subcutaneous injection of 1x106 (HT-29) tumor cells, and treatment with 2mg/kg 99961.1-MMAE (BIW&#424) was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model	HT-29 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	34.60%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x107 (Jeko-1) tumor cells,and treatment with 2.5 (D15)/3.5 (D29)mpk 99961.1-MMAE (Q2W&#422)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 41.
In Vivo Model	Jeko-1 xenograft model
Experiment 4 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	37.81%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x106 (A549) tumor cells,and treatment with 10mpk (mg/kg)99961.1-MMAE (BIW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 48.
In Vivo Model	A549 xenograft model
Experiment 5 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	59.22%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x107 (Jeko-1) tumor cells,and treatment with 2.5mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 41.
In Vivo Model	Jeko-1 xenograft model
Experiment 6 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	64.31%
Method Description	Cell line-derived xenograft models were established in female nude mice (NOD),by subcutaneous injection of 1x107 (MDA-MB-468) tumor cells,and treatment with 10mpk (mg/kg) 99961.1-MMAE (single dose)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 56.
In Vivo Model	MDA-MB-468 xenograft model
Experiment 7 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	67.66%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x106 (MDA-MB-231) tumor cells,and treatment with 5mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 56.
In Vivo Model	MDA-MB-231 xenograft model
Experiment 8 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	89.35%
Method Description	Cell line-derived xenograft models were established in nude mice by subcutaneous injection of 1x106 (HT-29) tumor cells, and treatment with 10mg/kg 99961.1-MMAE (BIW&#424) was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model	HT-29 xenograft model
Experiment 9 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	91.74%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x107 (Jeko-1) tumor cells,and treatment with 10mpk (mg/kg) 99961.1-MMAE (single dose)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 41.
In Vivo Model	Jeko-1 xenograft model
Experiment 10 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	95.77%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x107 (Jeko-1) tumor cells,and treatment with 10mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 41.
In Vivo Model	Jeko-1 xenograft model
Experiment 11 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	96.60%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x106 (MDA-MB-231) tumor cells,and treatment with 10mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 56.
In Vivo Model	MDA-MB-231 xenograft model
Experiment 12 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	97.86%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x106 (NCI-N87) tumor cells,and treatment with 5mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model	NCI-N87 xenograft model
Experiment 13 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.21%
Method Description	Cell line-derived xenograft models were established in female nude mice (NOD),by subcutaneous injection of 1x107 (MDA-MB-468) tumor cells,and treatment with 5mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 56.
In Vivo Model	MDA-MB-468 xenograft model
Experiment 14 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	99.20%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x106 (NCI-N87) tumor cells,and treatment with 10mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model	NCI-N87 xenograft model
Experiment 15 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	100%
Method Description	Cell line-derived xenograft models were established in female nude mice (NOD),by subcutaneous injection of 1x107 (MDA-MB-468) tumor cells,and treatment with 10mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 56.
In Vivo Model	MDA-MB-468 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	21.22 nM	High ROR1 expression (ROR1 +++)
Method Description	MDA-MB-468 cell line was plated at 2×105cell/mL, 90uL/well,12 hours later, ADCs (500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, 0.05nM) were added and incubated for 72h,then 10uL CCK8 (Bimake,B34304)was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	44.56 nM
Method Description	Jeko-1 cell line was plated at 1×105cell/mL, 90uL/well,12 hours later, ADCs (500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, 0.05nM) were added and incubated for 72h,then 10uL CCK8 (Bimake,B34304)was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 3 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	80.79 nM
Method Description	HT-29 cell line (1×104cell/mL,100uL/well) , the ADCs (2000, 500, 250, 125, 62.5, 31.25, 15.625, 7.813, 1.953nM) were added 12 hours later, and incubated for 96h, then 40uL/well MTS (Promega,G3580) was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 4 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	82.09 nM
Method Description	HT-29 cell line (1×104cell/mL,100uL/well) , the ADCs (2000, 500, 250, 125, 62.5, 31.25, 15.625, 7.813, 1.953nM) were added 12 hours later, and incubated for 96h, then 40uL/well MTS (Promega,G3580) was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 5 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	102.8 nM
Method Description	NCI-H1944 cell line was plated at 1.2×105cell/mL, 90uL/well,12 hours later, ADCs (500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, 0.05nM) were added and incubated for 72h,then 10uL CCK8 (Bimake,B34304)was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Lung adenocarcinoma	NCI-H1944 cells		CVCL_1508
Experiment 6 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	250.7 nM	Moderate ROR1 expression (ROR1++)
Method Description	A549 at 1×104cell/mL,100uL/well, 12 hours later,ADCs (2000, 500, 250, 125, 62.5, 31.25, 15.625, 7.813, 1.953nM) were added and incubated for 72h, then 40uL/well MTS (Promega,G3580) was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Lung adenocarcinoma	A549 cells		CVCL_0023
Experiment 7 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	295.6 nM	Moderate ROR1 expression (ROR1++)
Method Description	A549 at 1×104cell/mL,100uL/well, 12 hours later,ADCs (2000, 500, 250, 125, 62.5, 31.25, 15.625, 7.813, 1.953nM) were added and incubated for 72h, then 40uL/well MTS (Promega,G3580) was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Lung adenocarcinoma	A549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	11.08%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously withHT-29 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (0.4 mg/kg) (BIW&#424).
In Vivo Model	HT-29 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	15.90%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously withHT-29 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (2 mg/kg) (BIW&#424).
In Vivo Model	HT-29 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	34.60%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with Jeko-1 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (2.5 mg/kg- D15, 3.5 mg/kg- D29) (Q2W&#422).
In Vivo Model	Jeko-1 xenograft model
Experiment 4 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	37.81%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with A549 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (BIW&#423).
In Vivo Model	A549 xenograft model
Experiment 5 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	59.22%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with Jeko-1 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (2.5 mg/kg) (QW&#423).
In Vivo Model	Jeko-1 xenograft model
Experiment 6 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	64.31%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female NOD SCID nude mice between 6-8 weeks of age were injected subcutaneously with MDA-MB-4681 cells, when tumors reached appproximately 200 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) once.
In Vivo Model	MDA-MB-468 xenograft model
Experiment 7 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	67.66%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with MDA-MB-231 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (5 mg/kg) (QW&#423).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 8 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	89.35%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously withHT-29 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (BIW&#424).
In Vivo Model	HT-29 xenograft model
Experiment 9 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	91.74%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with Jeko-1 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) once.
In Vivo Model	Jeko-1 xenograft model
Experiment 10 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	95.77%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with Jeko-1 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (QW&#423).
In Vivo Model	Jeko-1 xenograft model
Experiment 11 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	96.60%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with MDA-MB-231 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (QW&#423).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 12 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	97.86%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with NCI-N87 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (5 mg/kg) (QW&#423).
In Vivo Model	NCI-N87 xenograft model
Experiment 13 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.21%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female NOD SCID nude mice between 6-8 weeks of age were injected subcutaneously with MDA-MB-4681 cells, when tumors reached appproximately 200 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (5 mg/kg) (QW&#423).
In Vivo Model	MDA-MB-468 xenograft model
Experiment 14 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	99.20%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with NCI-N87 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (QW&#423).
In Vivo Model	NCI-N87 xenograft model
Experiment 15 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	100%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female NOD SCID nude mice between 6-8 weeks of age were injected subcutaneously with MDA-MB-4681 cells, when tumors reached appproximately 200 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (QW&#423).
In Vivo Model	MDA-MB-468 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Effective Concentration (EC50)	21.22 nM
Method Description	ADCs were tested in MDA-MB-468 cells, and were added at final working concentration at 500 nM, 158 nM, 50 nM, 15.8 nM, 5 nM, 1.58 nM, 0.5 nM, 0.158 nM, 0.05 Nm, incubated for 3 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Effective Concentration (EC50)	44.56 nM
Method Description	ADCs were tested in Jeko-1 cells, and were added at final working concentration at 500 nM, 158 nM, 50 nM, 15.8 nM, 5 nM, 1.58 nM, 0.5 nM, 0.158 nM, 0.05 Nm, incubated for 3 days.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 3 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Effective Concentration (EC50)	82.09 nM
Method Description	ADCs were tested in HT-29 cells, and were added at final working concentration at 2000 nM, 500 nM, 250 nM, 125 nM, 62.5 nM, 31.25 nM, 15.625 nM, 7.813 nM, 1.953 nM, incubated for 4 days.
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 4 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Effective Concentration (EC50)	102.8 nM
Method Description	ADCs were tested in NCI-H1944 cells, and were added at final working concentration at 500 nM, 158 nM, 50 nM, 15.8 nM, 5 nM, 1.58 nM, 0.5 nM, 0.158 nM, 0.05 Nm, incubated for 3 days.
In Vitro Model	Lung adenocarcinoma	NCI-H1944 cells		CVCL_1508
Experiment 5 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Effective Concentration (EC50)	295.6 nM
Method Description	ADCs were tested in A549 cells, and were added at final working concentration at 2000 nM, 500 nM, 250 nM, 125 nM, 62.5 nM, 31.25 nM, 15.625 nM, 7.813 nM, 1.953 nM, incubated for 3 days.
In Vitro Model	Lung adenocarcinoma	A549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	11.08%
Method Description	A xenograft model derived from cell lines was established by unilateral subcutaneous injection of 1×10^6 HT-29 cells into female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 0.4 mg/kg. The treatment was given twice a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	HT-29-xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	15.90%
Method Description	A xenograft model derived from cell lines was established by unilateral subcutaneous injection of 1×10^6 HT-29 cells into female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 2 mg/kg. The treatment was given twice a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	HT-29-xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	34.60%
Method Description	A xenograft model derived from cell lines was established by injecting 1×10^7 Jeko cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE at doses of 2.5 mg/kg and 3.5 mg/kg was administered on the 15th and 29th days respectively. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	Jeko-1-xenograft model
Experiment 4 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	37.81%
Method Description	A xenograft model derived from cell lines was established by unilateral subcutaneous injection of 1×10^6 A549 cells into female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg. The treatment was given twice a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	A549-xenograft model
Experiment 5 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	59.22%
Method Description	A xenograft model derived from cell lines was established by injecting 1×10^7 Jeko cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 2.5 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	Jeko-1-xenograft model
Experiment 6 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	64.31%
Method Description	A xenograft model derived from cell lines was established by injecting 1×10^7 MDA-MB-468 cells subcutaneously into female BALB/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg once. The tumor inhibition rate was calculated at the end of the experiment.
In Vivo Model	MDA-MB-468-xenograft model
Experiment 7 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	67.66%
Method Description	A xenograft model derived from the cell line was established by injecting 1×10^6 MDA-MB-231 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 5 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	MDA-MB-231-xenograft model
Experiment 8 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	89.35%
Method Description	A xenograft model derived from cell lines was established by unilateral subcutaneous injection of 1×10^6 HT-29 cells into female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg. The treatment was given twice a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	HT-29-xenograft model
Experiment 9 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	91.74%
Method Description	A xenograft model derived from cell lines was established by injecting 1×10^7 Jeko-1 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg once. The tumor inhibition rate was calculated at the end of the experiment.
In Vivo Model	Jeko-1-xenograft model
Experiment 10 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	95.77%
Method Description	A xenograft model derived from cell lines was established by injecting 1×10^7 Jeko cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	Jeko-1-xenograft model
Experiment 11 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	96.60%
Method Description	A xenograft model derived from the cell line was established by injecting 1×10^6 MDA-MB-231 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	MDA-MB-231-xenograft model
Experiment 12 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	97.86%
Method Description	A xenograft model derived from the cell line was established by injecting 1×10^6 NCI-N87 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 5 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	NCI-N87-xenograft model
Experiment 13 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.21%
Method Description	A xenograft model derived from the cell line was established by injecting 1×10^7 MDA-MB-468 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 5 mg/kg. The treatment was given once a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	MDA-MB-468-xenograft model
Experiment 14 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	99.20%
Method Description	A xenograft model derived from the cell line was established by injecting 1×10^6 NCI-N87 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	NCI-N87-xenograft model
Experiment 15 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	100%
Method Description	A xenograft model derived from the cell line was established by injecting 1×10^7 MDA-MB-468 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, 99961.1-MMAE was administered at a dose of 10 mg/kg. The treatment was given once a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	MDA-MB-468-xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	11.30%
Method Description	The patient-derived tumor firagments (2mmx2mmx2mm) were engraftedin the right flank of B-NDG mice (Biocytogen Pharmaceuticals (Beijing) Co., Ltd., Cat#: B-CM-002). Treatment with 3mg/kg (QW&#422,i.v.) ADC after tumor volume about 200-300mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	TPBG Patient-derived Xenograft Model

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	61.9 ug/ml
Method Description	Series diluted ADCs (maximum concentration: 20 ug/mL, 3-fold dilutions, 10 gradients)were used to treat human lung squamous carcinoma NCI-H226 5000cells cultured in a cellculture plate, and the killing activity was detected after 72 hours of incubation in IncuCyte (Sartorius AG, IncuCytee S3).
In Vitro Model	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544

Experiment 1 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	15.18%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 1x107 (HCC1187) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 21.
In Vivo Model	HCC1187 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	19.87%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (PA-1) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 21.
In Vivo Model	NCI-N87 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	32.09%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 1x107 (PA-1) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	PA-1 xenograft model
Experiment 4 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	53.32%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (PA-1) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 21.
In Vivo Model	NCI-N87 xenograft model
Experiment 5 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	86.60%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 1x107 (HCC1187) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 21.
In Vivo Model	HCC1187 xenograft model
Experiment 6 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	97.06%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 1x107 (PA-1) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	PA-1 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (HCC1187) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1187 cells		CVCL_1247
Experiment 2 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3.35 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (PA-1) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 3 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5.75 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (SK-CO-1) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SKCO1 cells		CVCL_0626
Experiment 4 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	11.24 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (NCI-N87) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	11.62 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (NCI-H446) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H446 cells		CVCL_1562
Experiment 6 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	13.46 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (MDA-MB-231) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 7 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	19.09 nM	Moderate ROR1 expression (ROR1++)
Method Description	A total of 250-1500cells (COLO-678) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon carcinoma	COLO-678 cells		CVCL_1129
Experiment 8 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	24.58 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (HT-29) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 9 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	45.29 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (HCC827) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 10 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	A total of 250-1500cells (SK-BR-3) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 11 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Low ROR1 expression (ROR1+)
Method Description	A total of 250-1500cells (MCF-7) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	15.37%
Method Description	Cell line-derived xenograft models were established in nude mice by subcutaneous injection of 1x106 (HT-29) tumor cells, and treatment with 2mg/kg B31-H3L3-MMAE (BIW&#424) was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model	HT-29 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	16.05%
Method Description	Cell line-derived xenograft models were established in nude mice by subcutaneous injection of 1x106 (HT-29) tumor cells, and treatment with 0.4mg/kg B31-H3L3-MMAE (BIW&#424) was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model	HT-29 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	34.96%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x107 (Jeko-1) tumor cells,and treatment with 2.5 (D15)/3.5 (D29)mpk B31-H3L3-MMAE (Q2W&#422)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 41.
In Vivo Model	Jeko-1 xenograft model
Experiment 4 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	43.98%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x106 (A549) tumor cells,and treatment with 10mpk (mg/kg)B31-H3L3-MMAE (BIW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 48.
In Vivo Model	A549 xenograft model
Experiment 5 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	60.47%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x107 (Jeko-1) tumor cells,and treatment with 2.5mpk (mg/kg) B31-H3L3-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 41.
In Vivo Model	Jeko-1 xenograft model
Experiment 6 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	79.24%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x107 (Jeko-1) tumor cells,and treatment with 10mpk (mg/kg) B31-H3L3-MMAE (single dose)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 41.
In Vivo Model	Jeko-1 xenograft model
Experiment 7 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	79.79%
Method Description	Cell line-derived xenograft models were established in female nude mice (NSG),by subcutaneous injection of 1x106 (MDA-MB-231) tumor cells,and treatment with 5mpk (mg/kg) B31-H3L3-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 56.
In Vivo Model	MDA-MB-231 xenograft model
Experiment 8 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	85.53%
Method Description	Cell line-derived xenograft models were established in nude mice by subcutaneous injection of 1x106 (HT-29) tumor cells, and treatment with 10mg/kg B31-H3L3-MMAE (BIW&#424) was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model	HT-29 xenograft model
Experiment 9 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	91.52%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x106 (NCI-N87) tumor cells,and treatment with 5mpk (mg/kg) B31-H3L3-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model	NCI-N87 xenograft model
Experiment 10 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	95.44%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x107 (Jeko-1) tumor cells,and treatment with 10mpk (mg/kg) B31-H3L3-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 41.
In Vivo Model	Jeko-1 xenograft model
Experiment 11 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	96.60%
Method Description	Cell line-derived xenograft models were established in female nude mice (NSG),by subcutaneous injection of 1x106 (MDA-MB-231) tumor cells,and treatment with 10mpk (mg/kg) B31-H3L3-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 56.
In Vivo Model	MDA-MB-231 xenograft model
Experiment 12 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.02%
Method Description	Cell line-derived xenograft models were established in female nude mice (NOD),by subcutaneous injection of 1x107 (MDA-MB-468) tumor cells,and treatment with 5mpk (mg/kg) B31-H3L3-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 56.
In Vivo Model	MDA-MB-468 xenograft model
Experiment 13 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	99.31%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x106 (NCI-N87) tumor cells,and treatment with 10mpk (mg/kg) 99961.1-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model	NCI-N87 xenograft model
Experiment 14 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	100%
Method Description	Cell line-derived xenograft models were established in female nude mice (NOD),by subcutaneous injection of 1x107 (MDA-MB-468) tumor cells,and treatment with 10mpk (mg/kg) B31-H3L3-MMAE (QW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 56.
In Vivo Model	MDA-MB-468 xenograft model
Experiment 15 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	100%
Method Description	Cell line-derived xenograft models were established in female nude mice (NOD),by subcutaneous injection of 1x107 (MDA-MB-468) tumor cells,and treatment with 10mpk (mg/kg) B31-H3L3-MMAE (single dose)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 56.
In Vivo Model	MDA-MB-468 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	15.24 nM	High ROR1 expression (ROR1 +++)
Method Description	MDA-MB-468 cell line was plated at 2×105cell/mL, 90uL/well,12 hours later, ADCs (500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, 0.05nM) were added and incubated for 72h,then 10uL CCK8 (Bimake,B34304)was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	38.24 nM
Method Description	Jeko-1 cell line was plated at 1×105cell/mL, 90uL/well,12 hours later,ADCs (500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, 0.05nM) were added and incubated for 72h,then 10uL CCK8 (Bimake,B34304)was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 3 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	58.45 nM
Method Description	HT-29 cell line (1×104cell/mL,100uL/well) , the ADCs (2000, 500, 250, 125, 62.5, 31.25, 15.625, 7.813, 1.953nM) were added 12 hours later, and incubated for 96h, then 40uL/well MTS (Promega,G3580) was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 4 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	117.3 nM
Method Description	NCI-H1944 cell line was plated at 1.2×105cell/mL, 90uL/well,12 hours later, ADCs (500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, 0.05nM) were added and incubated for 72h,then 10uL CCK8 (Bimake,B34304)was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Lung adenocarcinoma	NCI-H1944 cells		CVCL_1508
Experiment 5 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	280.6 nM	Moderate ROR1 expression (ROR1++)
Method Description	A549 at 1×104cell/mL,100uL/well, 12 hours later,ADCs (2000, 500, 250, 125, 62.5, 31.25, 15.625, 7.813, 1.953nM) were added and incubated for 72h, then 40uL/well MTS (Promega,G3580) was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Lung adenocarcinoma	A549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	15.37%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously withHT-29 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (2 mg/kg) (BIW&#424).
In Vivo Model	HT-29 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	16.05%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously withHT-29 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (0.4 mg/kg) (BIW&#424).
In Vivo Model	HT-29 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	34.96%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with Jeko-1 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (2.5 mg/kg- D15, 3.5 mg/kg- D29) (Q2W&#422).
In Vivo Model	Jeko-1 xenograft model
Experiment 4 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	43.98%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with A549 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (BIW&#423).
In Vivo Model	A549 xenograft model
Experiment 5 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	60.47%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with Jeko-1 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (2.5 mg/kg) (QW&#423).
In Vivo Model	Jeko-1 xenograft model
Experiment 6 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	79.24%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with Jeko-1 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) once.
In Vivo Model	Jeko-1 xenograft model
Experiment 7 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	79.79%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with MDA-MB-231 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (5 mg/kg) (QW&#423).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 8 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	85.53%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously withHT-29 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (BIW&#424).
In Vivo Model	HT-29 xenograft model
Experiment 9 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	91.52%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with NCI-N87 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (5 mg/kg) (QW&#423).
In Vivo Model	NCI-N87 xenograft model
Experiment 10 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	95.44%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with Jeko-1 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (QW&#423).
In Vivo Model	Jeko-1 xenograft model
Experiment 11 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	96.60%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with MDA-MB-231 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (QW&#423).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 12 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.02%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female NOD SCID nude mice between 6-8 weeks of age were injected subcutaneously with MDA-MB-4681 cells, when tumors reached appproximately 200 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (5 mg/kg) (QW&#423).
In Vivo Model	MDA-MB-468 xenograft model
Experiment 13 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	99.31%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with NCI-N87 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (QW&#423).
In Vivo Model	NCI-N87 xenograft model
Experiment 14 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	100%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female NOD SCID nude mice between 6-8 weeks of age were injected subcutaneously with MDA-MB-4681 cells, when tumors reached appproximately 200 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (QW&#423).
In Vivo Model	MDA-MB-468 xenograft model
Experiment 15 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	100%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female NOD SCID nude mice between 6-8 weeks of age were injected subcutaneously with MDA-MB-4681 cells, when tumors reached appproximately 200 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) once.
In Vivo Model	MDA-MB-468 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Effective Concentration (EC50)	15.24 nM
Method Description	ADCs were tested in MDA-MB-468 cells, and were added at final working concentration at 500 nM, 158 nM, 50 nM, 15.8 nM, 5 nM, 1.58 nM, 0.5 nM, 0.158 nM, 0.05 Nm, incubated for 3 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Effective Concentration (EC50)	38.24 nM
Method Description	ADCs were tested in Jeko-1 cells, and were added at final working concentration at 500 nM, 158 nM, 50 nM, 15.8 nM, 5 nM, 1.58 nM, 0.5 nM, 0.158 nM, 0.05 Nm, incubated for 3 days.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 3 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Effective Concentration (EC50)	58.45 nM
Method Description	ADCs were tested in HT-29 cells, and were added at final working concentration at 2000 nM, 500 nM, 250 nM, 125 nM, 62.5 nM, 31.25 nM, 15.625 nM, 7.813 nM, 1.953 nM, incubated for 4 days.
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 4 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Effective Concentration (EC50)	117.3 nM
Method Description	ADCs were tested in NCI-H1944 cells, and were added at final working concentration at 500 nM, 158 nM, 50 nM, 15.8 nM, 5 nM, 1.58 nM, 0.5 nM, 0.158 nM, 0.05 Nm, incubated for 3 days.
In Vitro Model	Lung adenocarcinoma	NCI-H1944 cells		CVCL_1508
Experiment 5 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Effective Concentration (EC50)	280.6 nM
Method Description	ADCs were tested in A549 cells, and were added at final working concentration at 2000 nM, 500 nM, 250 nM, 125 nM, 62.5 nM, 31.25 nM, 15.625 nM, 7.813 nM, 1.953 nM, incubated for 3 days.
In Vitro Model	Lung adenocarcinoma	A549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	15.37%
Method Description	A xenograft model derived from cell lines was established by unilateral subcutaneous injection of 1×10^6 HT-29 cells into female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 2 mg/kg. The treatment was given twice a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	HT-29-xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	16.05%
Method Description	A xenograft model derived from cell lines was established by unilateral subcutaneous injection of 1×10^6 HT-29 cells into female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 0.4 mg/kg. The treatment was given twice a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	HT-29-xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	34.96%
Method Description	A xenograft model derived from cell lines was established by injecting 1×10^7 Jeko cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE at doses of 2.5 mg/kg and 3.5 mg/kg was administered on the 15th and 29th days respectively. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	Jeko-1-xenograft model
Experiment 4 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	43.98%
Method Description	A xenograft model derived from cell lines was established by unilateral subcutaneous injection of 1×10^6 A549 cells into female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 10 mg/kg. The treatment was given twice a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	A549-xenograft model
Experiment 5 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	60.47%
Method Description	A xenograft model derived from cell lines was established by injecting 1×10^7 Jeko cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 2.5 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	Jeko-1-xenograft model
Experiment 6 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	79.24%
Method Description	A xenograft model derived from cell lines was established by injecting 1×10^7 Jeko-1 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 10 mg/kg once. The tumor inhibition rate was calculated at the end of the experiment.
In Vivo Model	Jeko-1-xenograft model
Experiment 7 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	79.79%
Method Description	A xenograft model derived from the cell line was established by injecting 1×10^6 MDA-MB-231 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 5 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	MDA-MB-231-xenograft model
Experiment 8 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	85.53%
Method Description	A xenograft model derived from cell lines was established by unilateral subcutaneous injection of 1×10^6 HT-29 cells into female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 10 mg/kg. The treatment was given twice a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	HT-29-xenograft model
Experiment 9 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	91.52%
Method Description	A xenograft model derived from the cell line was established by injecting 1×10^6 NCI-N87 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 5 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	NCI-N87-xenograft model
Experiment 10 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	95.44%
Method Description	A xenograft model derived from cell lines was established by injecting 1×10^7 Jeko cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 10 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	Jeko-1-xenograft model
Experiment 11 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	96.60%
Method Description	A xenograft model derived from the cell line was established by injecting 1×10^6 MDA-MB-231 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 10 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	MDA-MB-231-xenograft model
Experiment 12 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.02%
Method Description	A xenograft model derived from the cell line was established by injecting 1×10^7 MDA-MB-468 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 5 mg/kg. The treatment was given once a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	MDA-MB-468-xenograft model
Experiment 13 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	99.31%
Method Description	A xenograft model derived from the cell line was established by injecting 1×10^6 NCI-N87 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 10 mg/kg. The treatment was given once a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	NCI-N87-xenograft model
Experiment 14 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	100%
Method Description	A xenograft model derived from the cell line was established by injecting 1×10^7 MDA-MB-468 cells subcutaneously into the left side of female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 10 mg/kg. The treatment was given once a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	MDA-MB-468-xenograft model
Experiment 15 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	100%
Method Description	A xenograft model derived from cell lines was established by injecting 1×10^7 MDA-MB-468 cells subcutaneously into female BALB/C nude mice. When the tumor volume reached approximately 100 mm^3, B31-H3L3-MMAE was administered at a dose of 10 mg/kg once. The tumor inhibition rate was calculated at the end of the experiment.
In Vivo Model	MDA-MB-468-xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC55)	117.3 nM
Method Description	NCI-H1944 cells were added with ADC samples, and the drug concentration gradient was diluted to 500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, and 0.05 nM. The cells were cultured at 37°C with 5% CO2 for 72 hours. Then, 10 uL of LCK8 (Bimake, B34304) was added to each well, and the cells were incubated at 37°C for 1 hour. The data were read at OD450 using a microplate reader.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1944 cells		CVCL_1508
Experiment 2 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC54)	15.24 nM
Method Description	MDA-MB-468 cells were added with ADC samples, and the drug concentration gradient was diluted to 500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, and 0.05 nM. The cells were cultured at 37°C with 5% CO2 for 72 hours. Then, 10 uL of LCK8 (Bimake, B34304) was added to each well, and the cells were incubated at 37°C for 1 hour. The data were read at OD450 using a microplate reader.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC53)	38.24 nM
Method Description	Jeko-1 cells were co-cultured with ADC samples, and the drug concentration gradient was diluted to 500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, and 0.05 nM. The cells were cultured at 37°C with 5% CO2 for 72 hours. Then, 10 uL of LCK8 (Bimake, B34304) was added to each well, and the reaction was incubated at 37°C for 1 hour. The data were read at OD450 using a microplate reader.    Click to Show/Hide
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865

Experiment 1 Reporting the Activity Date of This ADC					[97]
Efficacy Data	Tumor Growth lnhibition value (TGl)	20%
Method Description	1 mg/kg: Six-week-old B-NDG female mice (Biocytogen, China) were injected subcutaneously with 5 × 106 MV4-11 cells. Tumor growth was monitored, and mice were assigned to four treatment groups when tumor volumes reached approximately 100 mm3. Each group received two intravenous tail vein injections of one of the following treatments: vehicle or LA-057-MMAE (1, 3, and 6 mg/kg) on day 0 and 7. Tumor volume (V) = (LxW2)/2, where L is the longest dimension of the tumor and W is the corresponding tumor width. Mice were monitored for survival until they either succumbed to the disease or were euthanized when tumor volumes exceeded 1500 mm3.    Click to Show/Hide
In Vivo Model	MV-4-11 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[97]
Efficacy Data	Tumor Growth lnhibition value (TGl)	86%
Method Description	3 mg/kg: Six-week-old B-NDG female mice (Biocytogen, China) were injected subcutaneously with 5 × 106 MV4-11 cells. Tumor growth was monitored, and mice were assigned to four treatment groups when tumor volumes reached approximately 100 mm3. Each group received two intravenous tail vein injections of one of the following treatments: vehicle or LA-057-MMAE (1, 3, and 6 mg/kg) on day 0 and 7. Tumor volume (V) = (LxW2)/2, where L is the longest dimension of the tumor and W is the corresponding tumor width. Mice were monitored for survival until they either succumbed to the disease or were euthanized when tumor volumes exceeded 1500 mm3.    Click to Show/Hide
In Vivo Model	MV-4-11 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[97]
Efficacy Data	Tumor Growth lnhibition value (TGl)	114%
Method Description	6 mg/kg: Six-week-old B-NDG female mice (Biocytogen, China) were injected subcutaneously with 5 × 106 MV4-11 cells. Tumor growth was monitored, and mice were assigned to four treatment groups when tumor volumes reached approximately 100 mm3. Each group received two intravenous tail vein injections of one of the following treatments: vehicle or LA-057-MMAE (1, 3, and 6 mg/kg) on day 0 and 7. Tumor volume (V) = (LxW2)/2, where L is the longest dimension of the tumor and W is the corresponding tumor width. Mice were monitored for survival until they either succumbed to the disease or were euthanized when tumor volumes exceeded 1500 mm3.    Click to Show/Hide
In Vivo Model	MV-4-11 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[97]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	Positive LAIR1 expression (LAIR1+++/++)
Method Description	LA-057-MMAE or isotype control-MMAE was serially diluted in cell culture media and added to AML cells (U937, MV-4-11, and HL60) at a density of 1 × 104 cells per well. The cells were incubated for different durations: U937 cells for 2 days, HL-60 cells for 6 days, and MV4-11 cells for 3 days. For AML patient PBMCs, 3000 cells per well were incubated with serially diluted ADC in StemSpan Leukemic Cell Culture kit (STEMCELL Technologies, USA) for 7 days. Cell viability was measured (Promega) and calculated the growth inhibition of each well by a percentage of cell viability relative to blank wells. The assays were conducted following the guidelines established by Junx Bio for the use of PBMCs from AML patients.    Click to Show/Hide
In Vitro Model	Acute monoblastic/monocytic leukemia, Adult acute monocytic leukemia	U937 cells		CVCL_0007
Experiment 2 Reporting the Activity Date of This ADC					[97]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.09 nM	Positive LAIR1 expression (LAIR1+++/++)
Method Description	LA-057-MMAE or isotype control-MMAE was serially diluted in cell culture media and added to AML cells (U937, MV-4-11, and HL60) at a density of 1 × 104 cells per well. The cells were incubated for different durations: U937 cells for 2 days, HL-60 cells for 6 days, and MV4-11 cells for 3 days. For AML patient PBMCs, 3000 cells per well were incubated with serially diluted ADC in StemSpan Leukemic Cell Culture kit (STEMCELL Technologies, USA) for 7 days. Cell viability was measured (Promega) and calculated the growth inhibition of each well by a percentage of cell viability relative to blank wells. The assays were conducted following the guidelines established by Junx Bio for the use of PBMCs from AML patients.    Click to Show/Hide
In Vitro Model	Acute myeloblastic leukemia with maturation, Adult acute myeloid leukemia with maturation	HL60 cells		CVCL_0002
Experiment 3 Reporting the Activity Date of This ADC					[97]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.22 nM	Positive LAIR1 expression (LAIR1+++/++)
Method Description	LA-057-MMAE or isotype control-MMAE was serially diluted in cell culture media and added to AML cells (U937, MV-4-11, and HL60) at a density of 1 × 104 cells per well. The cells were incubated for different durations: U937 cells for 2 days, HL-60 cells for 6 days, and MV4-11 cells for 3 days. For AML patient PBMCs, 3000 cells per well were incubated with serially diluted ADC in StemSpan Leukemic Cell Culture kit (STEMCELL Technologies, USA) for 7 days. Cell viability was measured (Promega) and calculated the growth inhibition of each well by a percentage of cell viability relative to blank wells. The assays were conducted following the guidelines established by Junx Bio for the use of PBMCs from AML patients.    Click to Show/Hide
In Vitro Model	Childhood acute monocytic leukemia	MV4-11 cells		CVCL_0064

Experiment 1 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	22.14%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (PA-1) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 21.
In Vivo Model	NCI-N87 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	45.08%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (MDA-MB-231) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.    Click to Show/Hide
In Vivo Model	MDA-MB-231 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	64.97%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (PA-1) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 21.
In Vivo Model	NCI-N87 xenograft model
Experiment 4 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	93.69%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (MDA-MB-231) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	MDA-MB-231 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.58 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (PA-1) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 2 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.95 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (NCI-H446) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H446 cells		CVCL_1562
Experiment 3 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3.84 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (HCC1187) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1187 cells		CVCL_1247
Experiment 4 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5.16 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (NCI-N87) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	9.11 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (SK-CO-1) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SKCO1 cells		CVCL_0626
Experiment 6 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	10.32 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (MDA-MB-231) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 7 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	11.57 nM	Moderate ROR1 expression (ROR1++)
Method Description	A total of 250-1500cells (COLO-678) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon carcinoma	COLO-678 cells		CVCL_1129
Experiment 8 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	16.85 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (HT-29) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 9 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	19.99 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (HCC827) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 10 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	A total of 250-1500cells (SK-BR-3) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 11 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Low ROR1 expression (ROR1+)
Method Description	A total of 250-1500cells (MCF-7) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[98]
Efficacy Data	Tumor Growth lnhibition value (TGl)	25.61%
Method Description	Proliferation Inhibition Action of Different Drugs on Tumor Cell (the maximum killing percentage relative to the control group) in HepG2
In Vivo Model	HepG2 CDX Mouse Model
Experiment 2 Reporting the Activity Date of This ADC					[98]
Efficacy Data	Tumor Growth lnhibition value (TGl)	72.22%
Method Description	Proliferation Inhibition Action of Different Drugs on Tumor Cell (the maximum killing percentage relative to the control group) in FaDu
In Vivo Model	FaDu CDX Mouse Model
Experiment 3 Reporting the Activity Date of This ADC					[98]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.21%
Method Description	Proliferation Inhibition Action of Different Drugs on Tumor Cell (the maximum killing percentage relative to the control group) in BxPC-3
In Vivo Model	BxPC-3 CDX Mouse Model
Experiment 4 Reporting the Activity Date of This ADC					[98]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.21%
Method Description	Proliferation Inhibition Action of Different Drugs on Tumor Cell (the maximum killing percentage relative to the control group) in BxPC-3
In Vivo Model	BxPC-3 CDX Mouse Model

Experiment 1 Reporting the Activity Date of This ADC					[98]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1017 nM
Method Description	Proliferation Inhibition Action of Different Drugs on Tumor Cells (IC50, nM) in BxPC-3
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	28.90%	Positive TPBG expression (TPBG+++/++)
Method Description	The patient-derived tumor firagments (2mmx2mmx2mm,TPBC positive cells constituted 19.5% of total cells and MET positive cells constituted 8.3% of total cells) were engraftedin the right flank of B-NDG mice (Biocytogen Pharmaceuticals (Beijing) Co., Ltd., Cat#: B-CM-002). Treatment with 1.5mg/kg (QW&#422,i.v.) ADC after tumor volume about 200-300mm3. Determined tumor volume after the experiment, measured at day 45.    Click to Show/Hide
In Vivo Model	TPBG Patient-derived Xenograft Model
Experiment 2 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	60.70%	Positive TPBG expression (TPBG+++/++)
Method Description	The patient-derived tumor firagments (2mmx2mmx2mm,TPBC positive cells constituted 19.5% of total cells and MET positive cells constituted 8.3% of total cells) were engraftedin the right flank of B-NDG mice (Biocytogen Pharmaceuticals (Beijing) Co., Ltd., Cat#: B-CM-002). Treatment with 3mg/kg (QW&#422,i.v.) ADC after tumor volume about 200-300mm3. Determined tumor volume after the experiment, measured at day 45.    Click to Show/Hide
In Vivo Model	TPBG Patient-derived Xenograft Model
Experiment 3 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	64.50%	Positive TPBG expression (TPBG+++/++)
Method Description	The patient-derived tumor firagments (2mmx2mmx2mm,TPBG positive cells constituted 58.86% and MET positive cells constituted 24.08% of total cells) were engraftedin the right flank of B-NDG mice (Biocytogen Pharmaceuticals (Beijing) Co., Ltd., Cat#: B-CM-002). Treatment with 3mg/kg (QW&#422,i.v.) ADC after tumor volume about 200-300mm3. Determined tumor volume after the experiment, measured at day 28.    Click to Show/Hide
In Vivo Model	TPBG Patient-derived Xenograft Model

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	87.70%
Method Description	Cell line-derived xenograft models were established in B-NDG mice, by subcutaneous injection of 1x106 (NCI-H1975) tumor cells, and treatmen with 3mg/kg ADC (QW&#422,i.v.) after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	NCI-H1980 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	94.50%
Method Description	Cell line-derived xenograft models were established in B-NDG mice, by subcutaneous injection of 5x106 (NUGC-4) tumor cells, and treatmen with 3mg/kg ADC (QW&#422,i.v.) after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 35.
In Vivo Model	NUGC-6 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.9855 ug/ml
Method Description	Series diluted ADCs (maximum concentration: 20 ug/mL, 3-fold dilutions, 10 gradients)were used to treat human lung squamous carcinoma NCI-H226 5000cells cultured in a cellculture plate, and the killing activity was detected after 72 hours of incubation in IncuCyte (Sartorius AG, IncuCytee S3).
In Vitro Model	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	29.20%	Positive TPBG expression (TPBG+++/++)
Method Description	The patient-derived tumor firagments (2mmx2mmx2mm,TPBC positive cells constituted 19.5% of total cells and MET positive cells constituted 8.3% of total cells) were engraftedin the right flank of B-NDG mice (Biocytogen Pharmaceuticals (Beijing) Co., Ltd., Cat#: B-CM-002). Treatment with 1.5mg/kg (QW&#422,i.v.) ADC after tumor volume about 200-300mm3. Determined tumor volume after the experiment, measured at day 45.    Click to Show/Hide
In Vivo Model	TPBG Patient-derived Xenograft Model
Experiment 2 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	62.90%	Positive TPBG expression (TPBG+++/++)
Method Description	The patient-derived tumor firagments (2mmx2mmx2mm,TPBC positive cells constituted 19.5% of total cells and MET positive cells constituted 8.3% of total cells) were engraftedin the right flank of B-NDG mice (Biocytogen Pharmaceuticals (Beijing) Co., Ltd., Cat#: B-CM-002). Treatment with 3mg/kg (QW&#422,i.v.) ADC after tumor volume about 200-300mm3. Determined tumor volume after the experiment, measured at day 45.    Click to Show/Hide
In Vivo Model	TPBG Patient-derived Xenograft Model
Experiment 3 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	96.40%	Positive TPBG expression (TPBG+++/++)
Method Description	The patient-derived tumor firagments (2mmx2mmx2mm,TPBG positive cells constituted 58.86% and MET positive cells constituted 24.08% of total cells) were engraftedin the right flank of B-NDG mice (Biocytogen Pharmaceuticals (Beijing) Co., Ltd., Cat#: B-CM-002). Treatment with 3mg/kg (QW&#422,i.v.) ADC after tumor volume about 200-300mm3. Determined tumor volume after the experiment, measured at day 28.    Click to Show/Hide
In Vivo Model	TPBG Patient-derived Xenograft Model

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	57%
Method Description	Cell line-derived xenograft models were established in B-NDG mice, by subcutaneous injection of 1x106 (NCI-H1975) tumor cells, and treatmen with 1.5mg/kg ADC (QW&#422,i.v.) after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	NCI-H1977 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	87.60%
Method Description	Cell line-derived xenograft models were established in B-NDG mice, by subcutaneous injection of 5x106 (NUGC-4) tumor cells, and treatmen with 3mg/kg ADC (QW&#422,i.v.) after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 35.
In Vivo Model	NUGC-5 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	91.90%
Method Description	Cell line-derived xenograft models were established in B-NDG mice, by subcutaneous injection of 1x106 (NCI-H1975) tumor cells, and treatmen with 3mg/kg ADC (QW&#422,i.v.) after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	NCI-H1979 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.5044 ug/ml
Method Description	Series diluted ADCs (maximum concentration: 20 ug/mL, 3-fold dilutions, 10 gradients)were used to treat human lung squamous carcinoma NCI-H226 5000cells cultured in a cellculture plate, and the killing activity was detected after 72 hours of incubation in IncuCyte (Sartorius AG, IncuCytee S3).
In Vitro Model	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544

Experiment 1 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	33.54%
Method Description	Cell line-derived xenograft models were established in nude mice by subcutaneous injection of 1x106 (HT-29) tumor cells, and treatment with 2mg/kg B62-H3L3-MMAE (BIW&#424) was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model	HT-29 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	36.38%
Method Description	Cell line-derived xenograft models were established in female nude mice (Balb/C),by subcutaneous injection of 1x106 (A549) tumor cells,and treatment with 10mpk (mg/kg)B62-H3L3-MMAE (BIW&#423)was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 48.
In Vivo Model	A549 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Tumor Growth lnhibition value (TGl)	73.87%
Method Description	Cell line-derived xenograft models were established in nude mice by subcutaneous injection of 1x106 (HT-29) tumor cells, and treatment with 10mg/kg B62-H3L3-MMAE (BIW&#424) was initiated after tumor volume about 100mm3. Determined tumor volume after the experiment, measured at day 51.
In Vivo Model	HT-29 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	28.64 nM	High ROR1 expression (ROR1 +++)
Method Description	MDA-MB-468 cell line was plated at 2×105cell/mL, 90uL/well,12 hours later, ADCs (500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, 0.05nM) were added and incubated for 72h,then 10uL CCK8 (Bimake,B34304)was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	50.14 nM
Method Description	Jeko-1 cell line was plated at 1×105cell/mL, 90uL/well,12 hours later, ADCs (500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, 0.05nM) were added and incubated for 72h,then 10uL CCK8 (Bimake,B34304)was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 3 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	121.6 nM
Method Description	HT-29 cell line (1×104cell/mL,100uL/well) , the ADCs (2000, 500, 250, 125, 62.5, 31.25, 15.625, 7.813, 1.953nM) were added 12 hours later, and incubated for 96h, then 40uL/well MTS (Promega,G3580) was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 4 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	128.6 nM
Method Description	NCI-H1944 cell line was plated at 1.2×105cell/mL, 90uL/well,12 hours later, ADCs (500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, 0.05nM) were added and incubated for 72h,then 10uL CCK8 (Bimake,B34304)was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Lung adenocarcinoma	NCI-H1944 cells		CVCL_1508
Experiment 5 Reporting the Activity Date of This ADC					[93]
Efficacy Data	Half Maximal Effective Concentration (EC50)	311.4 nM	Moderate ROR1 expression (ROR1++)
Method Description	A549 cell line at 1×104cell/mL,100uL/well, 12 hours later,ADCs (2000, 500, 250, 125, 62.5, 31.25, 15.625, 7.813, 1.953nM) were added and incubated for 72h, then 40uL/well MTS (Promega,G3580) was added to each well and a microplate reader was used for detection OD492.
In Vitro Model	Lung adenocarcinoma	A549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	33.54%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously withHT-29 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (2 mg/kg) (BIW&#424).
In Vivo Model	HT-29 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	36.38%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously with A549 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (BIW&#423).
In Vivo Model	A549 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Tumor Growth lnhibition value (TGl)	73.87%	Positive ROR1 expression (ROR1+++/++)
Method Description	Female Balb/C nude mice between 6-8 weeks of age were injected subcutaneously withHT-29 cells, when tumors reached appproximately 100 mm^3, animals were matched by tumor volume into treatment or controls groups. The test articles were given by tail vein at a dose (10 mg/kg) (BIW&#424).
In Vivo Model	HT-29 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Effective Concentration (EC50)	28.64 nM
Method Description	ADCs were tested in MDA-MB-468 cells, and were added at final working concentration at 500 nM, 158 nM, 50 nM, 15.8 nM, 5 nM, 1.58 nM, 0.5 nM, 0.158 nM, 0.05 Nm, incubated for 3 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Effective Concentration (EC50)	50.14 nM
Method Description	ADCs were tested in Jeko-1 cells, and were added at final working concentration at 500 nM, 158 nM, 50 nM, 15.8 nM, 5 nM, 1.58 nM, 0.5 nM, 0.158 nM, 0.05 Nm, incubated for 3 days.
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865
Experiment 3 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Effective Concentration (EC50)	121.6 nM
Method Description	ADCs were tested in HT-29 cells, and were added at final working concentration at 2000 nM, 500 nM, 250 nM, 125 nM, 62.5 nM, 31.25 nM, 15.625 nM, 7.813 nM, 1.953 nM, incubated for 4 days.
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 4 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Effective Concentration (EC50)	128.6 nM
Method Description	ADCs were tested in NCI-H1944 cells, and were added at final working concentration at 500 nM, 158 nM, 50 nM, 15.8 nM, 5 nM, 1.58 nM, 0.5 nM, 0.158 nM, 0.05 Nm, incubated for 3 days.
In Vitro Model	Lung adenocarcinoma	NCI-H1944 cells		CVCL_1508
Experiment 5 Reporting the Activity Date of This ADC					[94]
Efficacy Data	Half Maximal Effective Concentration (EC50)	311.4 nM
Method Description	ADCs were tested in A549 cells, and were added at final working concentration at 2000 nM, 500 nM, 250 nM, 125 nM, 62.5 nM, 31.25 nM, 15.625 nM, 7.813 nM, 1.953 nM, incubated for 3 days.
In Vitro Model	Lung adenocarcinoma	A549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	33.54%
Method Description	A xenograft model derived from cell lines was established by unilateral subcutaneous injection of 1×10^6 HT-29 cells into female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B62-H3L3-MMAE was administered at a dose of 2 mg/kg. The treatment was given twice a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	HT-29-xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	36.38%
Method Description	A xenograft model derived from cell lines was established by unilateral subcutaneous injection of 1×10^6 A549 cells into female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B62-H3L3-MMAE was administered at a dose of 10 mg/kg. The treatment was given twice a week for 3 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	A549-xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Tumor Growth lnhibition value (TGl)	73.87%
Method Description	A xenograft model derived from cell lines was established by unilateral subcutaneous injection of 1×10^6 HT-29 cells into female Balb/C nude mice. When the tumor volume reached approximately 100 mm^3, B62-H3L3-MMAE was administered at a dose of 10 mg/kg. The treatment was given twice a week for 4 weeks. The tumor inhibition rate was calculated at the end of the experiment.    Click to Show/Hide
In Vivo Model	HT-29-xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC52)	128.6 nM
Method Description	NCI-H1944 cells were added with ADC samples, and the drug concentration gradient was diluted to 500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, and 0.05 nM. The cells were cultured at 37°C with 5% CO2 for 72 hours. Then, 10 uL of LCK8 (Bimake, B34304) was added to each well, and the cells were incubated at 37°C for 1 hour. The data were read at OD450 using a microplate reader.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1944 cells		CVCL_1508
Experiment 2 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC51)	28.64 nM
Method Description	MDA-MB-468 cells were added with ADC samples, and the drug concentration gradient was diluted to 500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, and 0.05 nM. The cells were cultured at 37°C with 5% CO2 for 72 hours. Then, 10 uL of LCK8 (Bimake, B34304) was added to each well, and the cells were incubated at 37°C for 1 hour. The data were read at OD450 using a microplate reader.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[95]
Efficacy Data	Half Maximal Effective Concentration (EC50)	50.14 nM
Method Description	Jeko-1 cells were co-cultured with ADC samples, and the drug concentration gradient was diluted to 500, 158, 50, 15.8, 5, 1.58, 0.5, 0.158, and 0.05 nM. The cells were cultured at 37°C with 5% CO2 for 72 hours. Then, 10 uL of LCK8 (Bimake, B34304) was added to each well, and the reaction was incubated at 37°C for 1 hour. The data were read at OD450 using a microplate reader.    Click to Show/Hide
In Vitro Model	Mantle cell lymphoma	JeKo-1 cells		CVCL_1865

Experiment 1 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Tumor Growth lnhibition value (TGl)	37.50%	Positive IL13Ra2 expression (IL13Ra2+++/++)
Method Description	Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper flank region with 0.5x10 6of SK-MES-1 tumor cells (a non-small cell lung cancer (NSCLC)cell line having an IL13Ra2 copy number of about 4x104)in 0.1 mL of PBS for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (8 mice per group)and received intravenous injections of PBS vehicle or a single dose of the tested ADC 33-2 at 1 mg/kg on Day 1. The end of the study was day 44.    Click to Show/Hide
In Vivo Model	CDX Model-SK-MES-1
Experiment 2 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Tumor Growth lnhibition value (TGl)	55%	Positive IL13Ra2 expression (IL13Ra2+++/++)
Method Description	Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper flank region with 0.5x10 6of SK-MES-1 tumor cells (a non-small cell lung cancer (NSCLC)cell line having an IL13Ra2 copy number of about 4x104)in 0.1 mL of PBS for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (8 mice per group)and received intravenous injections of PBS vehicle or a single dose of the tested ADC 33-2 at 3 mg/kg on Day 1. The end of the study was day 44.    Click to Show/Hide
In Vivo Model	CDX Model-SK-MES-1
Experiment 3 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Tumor Growth lnhibition value (TGl)	82.20%	Positive IL13Ra2 expression (IL13Ra2+++/++)
Method Description	Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper flank region with 0.5x10 6of SK-MES-1 tumor cells (a non-small cell lung cancer (NSCLC)cell line having an IL13Ra2 copy number of about 4x104)in 0.1 mL of PBS for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (8 mice per group)and received intravenous injections of PBS vehicle or a single dose of the tested ADC 33-2 at 6 mg/kg on Day 1. The end of the study was day 44.    Click to Show/Hide
In Vivo Model	CDX Model-SK-MES-1
Experiment 4 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Tumor Growth lnhibition value (TGl)	88.60%	Positive IL13Ra2 expression (IL13Ra2+++/++)
Method Description	Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper/lower flank region with 1x10 7of H2228 tumor cells (an NSCLC cell line having an IL13Ra2 copy number of about 2,000)in 0.1 mL of PBS mixed with MATRIGELR (1:1)for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (10 mice per group)and received intravenous injections of vehicle or a single dose of the tested ADCs at 10 mg/kg on Day 1. Body weights and tumor volumes were measured twice per week until the end of the study (Day 48).    Click to Show/Hide
In Vivo Model	CDX Model-H2228
Experiment 5 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Tumor Growth lnhibition value (TGl)	100%	Positive IL13Ra2 expression (IL13Ra2+++/++)
Method Description	Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper flank region with 0.5x10 6of SK-MES-1 tumor cells (a non-small cell lung cancer (NSCLC)cell line having an IL13Ra2 copy number of about 4x104)in 0.1 mL of PBS for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (8 mice per group)and received intravenous injections of PBS vehicle or a single dose of the tested ADC 33-2 at 10 mg/kg on Day 1. The end of the study was day 44.    Click to Show/Hide
In Vivo Model	CDX Model-SK-MES-1
Experiment 6 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Tumor Growth lnhibition value (TGl)	101.10%	Positive IL13Ra2 expression (IL13Ra2+++/++)
Method Description	Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper flank region with 0.5x10 6of SK-MES-1 tumor cells (a non-small cell lung cancer (NSCLC)cell line having an IL13Ra2 copy number of about 4x104)in 0.1 mL of PBS for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (10 mice per group)and received intravenous injections of PBS vehicle or a single dose of the tested ADCs at 10 mg/kg on Day 1. The end of the study was day 49.    Click to Show/Hide
In Vivo Model	CDX Model-SK-MES-1
Experiment 7 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Tumor Growth lnhibition value (TGl)	111%	Positive IL13Ra2 expression (IL13Ra2+++/++)
Method Description	Each female NOD.Cg-Prkdcscid II2rgmIVst/Vst (NPG)mouse was inoculated subcutaneously in the right upper flank region with 1x10 7of H1792 tumor cells (an NSCLC cell line having an IL13Ra2 copy number of about 47000)in 0.1 mL of PBS mixed with MATRIGELR (1:1)for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (10 mice per group)and received intravenous injections of vehicle or a single dose of the tested ADCs at 10 mg/kg on Day 1. Body weights and tumor volumes were measured twice per week until the end of the study (Day 57).    Click to Show/Hide
In Vivo Model	CDX Model-H1792

Experiment 1 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01 nM	High hIL13Ra2 expression (hIL13Ra2 +++)
Method Description	The cytotoxic activity of ADC 33-2 was determined against cancer cell lines A375.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model	Amelanotic melanoma	A375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02-0.03 nM	Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description	The cytotoxic activity of ADC 33-2 was determined against cancer cell lines H1792.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model	Lung adenocarcinoma	H1792 cells		CVCL_1495
Experiment 3 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04-0.08 nM	Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description	The cytotoxic activity of ADC 33-2 was determined against cancer cell lines H2228.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model	Lung adenocarcinoma	H2228 cells		CVCL_1543
Experiment 4 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3-63 nM	Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description	The cytotoxic activity of ADC 33-2 was determined against cancer cell lines SK-MES-1.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model	Lung squamous cell carcinoma	SK-MES-1 cells		CVCL_0630

Experiment 1 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	39.12%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (PA-1) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 21.
In Vivo Model	NCI-N87 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	39.71%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 1x107 (HCC1187) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 21.
In Vivo Model	HCC1187 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	60.02%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 1x107 (PA-1) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	PA-1 xenograft model
Experiment 4 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	69.85%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (PA-1) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 21.
In Vivo Model	NCI-N87 xenograft model
Experiment 5 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	79.68%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (MDA-MB-231) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.    Click to Show/Hide
In Vivo Model	MDA-MB-231 xenograft model
Experiment 6 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	92.31%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 1x107 (HCC1187) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 21.
In Vivo Model	HCC1187 xenograft model
Experiment 7 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	93.61%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (MDA-MB-231) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	MDA-MB-231 xenograft model
Experiment 8 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	95.79%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 1x107 (PA-1) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	PA-1 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.09 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (PA-1) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 2 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.3 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (NCI-H446) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H446 cells		CVCL_1562
Experiment 3 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.8 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (HCC1187) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1187 cells		CVCL_1247
Experiment 4 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	6.66 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (SK-CO-1) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SKCO1 cells		CVCL_0626
Experiment 5 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	8.32 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (NCI-N87) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	12.19 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (HCC827) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 7 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	12.54 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (MDA-MB-231) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 8 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	13.28 nM	Moderate ROR1 expression (ROR1++)
Method Description	A total of 250-1500cells (COLO-678) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon carcinoma	COLO-678 cells		CVCL_1129
Experiment 9 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	17.24 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (HT-29) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 10 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	A total of 250-1500cells (SK-BR-3) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 11 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Low ROR1 expression (ROR1+)
Method Description	A total of 250-1500cells (MCF-7) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	39.72%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (PA-1) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 21.
In Vivo Model	NCI-N87 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	59.85%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (MDA-MB-231) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.    Click to Show/Hide
In Vivo Model	MDA-MB-231 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	69.98%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 1x107 (PA-1) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	PA-1 xenograft model
Experiment 4 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	71.49%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (PA-1) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 21.
In Vivo Model	NCI-N87 xenograft model
Experiment 5 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	93.85%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (MDA-MB-231) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	MDA-MB-231 xenograft model
Experiment 6 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	96.22%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 1x107 (PA-1) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	PA-1 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.64 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (NCI-H446) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H446 cells		CVCL_1562
Experiment 2 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.45 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (PA-1) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 3 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.11 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (HCC1187) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1187 cells		CVCL_1247
Experiment 4 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.28 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (SK-CO-1) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SKCO1 cells		CVCL_0626
Experiment 5 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5.65 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (MDA-MB-231) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 6 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	6.41 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (NCI-N87) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 7 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	12.13 nM	Moderate ROR1 expression (ROR1++)
Method Description	A total of 250-1500cells (COLO-678) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon carcinoma	COLO-678 cells		CVCL_1129
Experiment 8 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	13.48 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (HCC827) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 9 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	19.11 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (HT-29) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 10 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	A total of 250-1500cells (SK-BR-3) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 11 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Low ROR1 expression (ROR1+)
Method Description	A total of 250-1500cells (MCF-7) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	45%	Positive TPBG expression (TPBG+++/++)
Method Description	The patient-derived tumor firagments (2mmx2mmx2mm,TPBC positive cells constituted 19.5% of total cells and MET positive cells constituted 8.3% of total cells) were engraftedin the right flank of B-NDG mice (Biocytogen Pharmaceuticals (Beijing) Co., Ltd., Cat#: B-CM-002). Treatment with 3mg/kg (QW&#422,i.v.) ADC after tumor volume about 200-300mm3. Determined tumor volume after the experiment, measured at day 45.    Click to Show/Hide
In Vivo Model	TPBG Patient-derived Xenograft Model

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	64.90%
Method Description	Cell line-derived xenograft models were established in B-NDG mice, by subcutaneous injection of 1x106 (NCI-H1975) tumor cells, and treatmen with 3mg/kg ADC (QW&#422,i.v.) after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	NCI-H1980 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	9.533 ug/ml
Method Description	Series diluted ADCs (maximum concentration: 20 ug/mL, 3-fold dilutions, 10 gradients)were used to treat human lung squamous carcinoma NCI-H226 5000cells cultured in a cellculture plate, and the killing activity was detected after 72 hours of incubation in IncuCyte (Sartorius AG, IncuCytee S3).
In Vitro Model	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	45.90%	Positive TPBG expression (TPBG+++/++)
Method Description	The patient-derived tumor firagments (2mmx2mmx2mm,TPBG positive cells constituted 58.86% and MET positive cells constituted 24.08% of total cells) were engraftedin the right flank of B-NDG mice (Biocytogen Pharmaceuticals (Beijing) Co., Ltd., Cat#: B-CM-002). Treatment with 3mg/kg (QW&#422,i.v.) ADC after tumor volume about 200-300mm3. Determined tumor volume after the experiment, measured at day 28.    Click to Show/Hide
In Vivo Model	TPBG Patient-derived Xenograft Model

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	59.20%
Method Description	Cell line-derived xenograft models were established in B-NDG mice, by subcutaneous injection of 1x106 (NCI-H1975) tumor cells, and treatmen with 1.5mg/kg ADC (QW&#422,i.v.) after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	NCI-H1976 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	97.70%
Method Description	Cell line-derived xenograft models were established in B-NDG mice, by subcutaneous injection of 5x106 (NUGC-4) tumor cells, and treatmen with 3mg/kg ADC (QW&#422,i.v.) after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 35.
In Vivo Model	NUGC-4 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.70%
Method Description	Cell line-derived xenograft models were established in B-NDG mice, by subcutaneous injection of 1x106 (NCI-H1975) tumor cells, and treatmen with 3mg/kg ADC (QW&#422,i.v.) after tumor volume about 200mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	NCI-H1978 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	48%	Positive TF expression (TF+++/++)
Method Description	In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 2 mg/kg (qwk × 2, IV).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	96%	Positive TF expression (TF+++/++)
Method Description	In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 4 mg/kg (qwk × 2, IV).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	131%	Positive TF expression (TF+++/++)
Method Description	The A431 epidermoid carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice. Animals were randomized and treated with drugs (5 mg/kg, qwk × 3, IP).
In Vivo Model	A431 xenograft model
Experiment 4 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	135%	Positive TF expression (TF+++/++)
Method Description	HPAF-II pancreatic carcinoma epidermoid carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice. Animals were randomized and treated with drugs (2 mg/kg, qwk × 2, IV).
In Vivo Model	HPAF-II pancreatic carcinoma xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	74%	Positive TF expression (TF+++/++)
Method Description	TF-positive PDX models were performed in athymic nude mice (Envigo, Indianapolis, IN) to evaluate the efficacy of the ADCs in vivo. The animals' care was in accordance with institutional guidelines. Study animals were implanted unilaterally on the left flank with tumor fragments. In the head and neck and ovarian PDX model, the mice were treated with drugs (2.5 mg/kg, qwk × 3, IP).    Click to Show/Hide
In Vivo Model	The head and neck and ovarian PDX model
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	119%	Positive TF expression (TF+++/++)
Method Description	TF-positive PDX models were performed in athymic nude mice (Envigo, Indianapolis, IN) to evaluate the efficacy of the ADCs in vivo. The animals' care was in accordance with institutional guidelines. Study animals were implanted unilaterally on the left flank with tumor fragments. In the head and neck and ovarian PDX model, the mice were treated with drugs (5 mg/kg, qwk × 2, IP).    Click to Show/Hide
In Vivo Model	The head and neck and ovarian PDX model

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.06 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to HPAF-II cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 76 h. HPAF-II cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.13 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to A431 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. A439cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.15 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to MDA-MB-231 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. MDA-MB-231 cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	49%	Positive TF expression (TF+++/++)
Method Description	In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 2 mg/kg (qwk × 2, IV).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	93%	Positive TF expression (TF+++/++)
Method Description	In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 4 mg/kg (qwk × 2, IV).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	137%	Positive TF expression (TF+++/++)
Method Description	HPAF-II pancreatic carcinoma epidermoid carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice. Animals were randomized and treated with drugs (2 mg/kg, qwk × 2, IV).
In Vivo Model	HPAF-II pancreatic carcinoma xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.05 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to HPAF-II cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 75 h. HPAF-II cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to A431 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. A438cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.14 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to MDA-MB-231 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. MDA-MB-231 cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[101]
Efficacy Data	Tumor Growth lnhibition value (TGl)	56%
Method Description	Treatment with hSD5-vedotin at a dose of 1 mg/kg resulted in a 56 % tumor growth inhibition (TGI): The freshly cultured BxPc-3 cancer cells were harvested during the logarithmic growth phase, suspended in PBS, and subcutaneously implanted into NOD/SCID mice (5 × 106 cells per mouse) to induce tumor formation. Tumor size was measured bi-weekly, and the volume was calculated using the formula V = 0.5lw2, where l represents the length and w represents the width of the tumor. When the tumor size reached approximately 100 mm3, the animals were divided into groups that received the indicated treatments (1, 0.2, 0.04 mg/kg, iv, qwk). The mice were monitored frequently for any signs of adverse drug-related side effects.    Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[101]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.4 nM	High DDR1 expression (DDR1 +++)
Method Description	The proliferation of PDAC cells was measured using the 3- (4,5-dimethylthiazol-2-yl)-5- (3-carboxymethoxyphenyl)-2- (4-sulfophenyl)-2H-tetrazolium (MTS) cell proliferation assay kit (Promega). The cells were seeded in a 96-well culture plate for attachment. The hSD5-vedotin at various concentrations was added to the cell culture and incubated for 5 days. Finally, MTS and phenazine methosulfate solutions were added and set for development. After the SDS reagent was added to stop the reaction, the absorbance of each well was measured at OD 490 nm.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Tumor Growth lnhibition value (TGl)	62.36%	Low HER2 expression (HER2+)
Method Description	Investigated the antitumour effect of 12 MG/KG AZO-ADC-2 in a Herceptin-resistant, HER2low JIMT-1 xenograft tumour model.
In Vivo Model	Herceptin-resistant, HER2-low JIMT-1 xenograft tumour model
Experiment 2 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Tumor Growth lnhibition value (TGl)	90.97%	High HER2 expression (HER2+++)
Method Description	In the HER2high NCI-N87 xenograft model, Herceptin, AZO-ADC-2 and VC-ADC were administered once a week at a dose of 5 or 10 mg/kg for four consecutive weeks. Compared with the control group, AZO-ADC-2 (5 mg/kg) treatment group displayed significant and sustained suppression of tumour growth with an inhibition rate of 90.97 %
In Vivo Model	HER2high NCI-N87 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.016 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to HER2+ SK-BR-3 cells
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.027 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to HER2+ BK474 cells
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.053 nM
Method Description	Cytotoxicity of AZO-ADC-2 to SKOV3/MCF-7 co-culture under 0.1% O2
In Vitro Model	Ovarian serous cystadenocarcinoma; Invasive breast carcinoma of no special type	SKOV3/MCF-7 co-culture cells		CVCL_0532; CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.063 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to SKOV-3 cells under 0.1 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.069 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to HER2+ NCI-N87 cells
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 6 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.079 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to SKOV-3 cells under 1 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 7 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.088 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 0.1 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 8 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.19 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to BT474-HDR cells under 0.1% O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 9 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.28 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to BT474-HDR cells under 0.1 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 10 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.57 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to BT474-HDR cells under 1 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 11 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.74 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to SKOV-3 cells under 5 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 12 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	9.12 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to BT474-HDR cells under 5 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 13 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	11.05 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 toBT474-HDR cells under 20 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 14 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	27.67 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 20 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 15 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	66.8 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to SKOV-3 cells under 20 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 16 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	109.1 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-2 to BT474-HDR cells under 20 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 17 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	115.4 nM	Low HER2 expression (HER2+)
Method Description	Cytotoxicity of AZO-ADC-2 to HER2- MCF-7 cells
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 18 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	134.7 nM
Method Description	Cytotoxicity of AZO-ADC-2 to SKOV3/MCF-7 co-culture under 20% O2
In Vitro Model	Ovarian serous cystadenocarcinoma; Invasive breast carcinoma of no special type	SKOV3/MCF-7 co-culture cells		CVCL_0532; CVCL_0031
Experiment 19 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	266.93 nM
Method Description	Cytotoxicity of AZO-ADC-2 to normal cells, LO2 cells
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	LO2 cells		CVCL_6926
Experiment 20 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 666 nM	Low HER2 expression (HER2+)
Method Description	Cytotoxicity of AZO-ADC-2 to HER2- MDA-MB-231 cells
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 21 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 666 nM
Method Description	Cytotoxicity of AZO-ADC-2 to normal cells, NIH3T3 cells
In Vitro Model	Normal	NIH3T3 cells		CVCL_0594
Experiment 22 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 666 nM
Method Description	Cytotoxicity of AZO-ADC-2 to normal cells, 293T cells
In Vitro Model	Normal	293T cells		CVCL_0063

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	63%	Positive TF expression (TF+++/++)
Method Description	In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 2 mg/kg (qwk × 2, IV).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	69%	Positive TF expression (TF+++/++)
Method Description	In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 4 mg/kg (qwk × 2, IV).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	138%	Positive TF expression (TF+++/++)
Method Description	HPAF-II pancreatic carcinoma epidermoid carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice. Animals were randomized and treated with drugs (2 mg/kg, qwk × 2, IV).
In Vivo Model	HPAF-II pancreatic carcinoma xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to HPAF-II cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 71 h. HPAF-II cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.08 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to A431 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. A434cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.09 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to MDA-MB-231 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. MDA-MB-231 cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Tumor Growth lnhibition value (TGl)	64.40%	High Claudin 18.2 expression (Claudin 18.2 +++)
Method Description	Patient-derived Xenograft Model were established by tumor tissue with a volume of about 15-30 mm3 was transplanted into the back of BALB/c nude mice subcutaneously, and treatment with 1mg/kg ADCs when the tumor volume reached 150-260 mm3.
In Vivo Model	STO #523 patient-derived xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Tumor Growth lnhibition value (TGl)	0.70%	High Claudin 18.2 expression (Claudin 18.2 +++)
Method Description	Patient-derived Xenograft Model were established by tumor tissue with a volume of about 15-30 mm3 was transplanted into the back of BALB/c nude mice subcutaneously, and treatment with 1mg/kg ADCs when the tumor volume reached 150-260 mm3.
In Vivo Model	STO #025 patient-derived xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Tumor Growth lnhibition value (TGl)	93.21%	High Claudin 18.2 expression (Claudin 18.2 +++)
Method Description	Patient-derived Xenograft Model were established by tumor tissue with a volume of about 15-30 mm3 was transplanted into the back of BALB/c nude mice subcutaneously, and treatment with 3mg/kg ADCs when the tumor volume reached 150-260 mm3.
In Vivo Model	STO #523 patient-derived xenograft model
Experiment 4 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Tumor Growth lnhibition value (TGl)	100%	High Claudin 18.2 expression (Claudin 18.2 +++)
Method Description	Patient-derived Xenograft Model were established by tumor tissue with a volume of about 15-30 mm3 was transplanted into the back of BALB/c nude mice subcutaneously, and treatment with 3mg/kg ADCs when the tumor volume reached 150-260 mm3.
In Vivo Model	STO #025 patient-derived xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	113.8 ng/mL	High Claudin 18.2 expression (Claudin 18.2 +++)
Method Description	LI-M11 cells at 5000 cells/well, 1.2mg/ml ADCs were added and incubated for 96 hours, then CCK-8 or Presto-Blue detection reagent was added to each well, and a microplate reader was used for detection and four parameter fitting was carried out.
In Vitro Model	Lung lymphangioleiomyomatosis, Lymphangioleiomyomatosis	LI-M11 cells		CVCL_8891
Experiment 2 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	253.9 ng/mL	Moderate Claudin 18.2 expression (Claudin 18.2++)
Method Description	LT-1C8 at 5000 or 10000 cells/well, 1.2mg/ml ADCs were added and incubated for 96 hours, then CCK-8 or Presto-Blue detection reagent was added to each well, and a microplate reader was used for detection and four parameter fitting was carried out.
In Vitro Model	Lung lymphangioleiomyomatosis, Lymphangioleiomyomatosis	LT-1C8 cells		CVCL_8891
Experiment 3 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4632 ng/mL	Negative Claudin 18.2 expression (Claudin 18.2-)
Method Description	BxPC-3 at 3000 cells/well, 1.2mg/ml ADCs were added and incubated for 96 hours, then CCK-8 or Presto-Blue detection reagent was added to each well, and a microplate reader was used for detection and four parameter fitting was carried out.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Half Maximal Effective Concentration (EC50)	16.37 ng/mL	High Claudin 18.2 expression (Claudin 18.2 +++)
Method Description	KATO III cell line was plated at 5000 cells/well, and the samples were added 24 hours later. All samples to be tested were diluted 2.4 folds starting from a final concentration of 1000 ng/mL for 9 times and incubated for 96 hours, and the fluorescence intensity was read by a microplate reader after color development for 60 min with PrestoBlue.
In Vitro Model	Down syndrome	KATO III cells		CVCL_0371

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	66%	Positive TF expression (TF+++/++)
Method Description	In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 2 mg/kg (qwk × 2, IV).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	100%	Positive TF expression (TF+++/++)
Method Description	In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 4 mg/kg (qwk × 2, IV).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	129%	Positive TF expression (TF+++/++)
Method Description	HPAF-II pancreatic carcinoma epidermoid carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice. Animals were randomized and treated with drugs (2 mg/kg, qwk × 2, IV).
In Vivo Model	HPAF-II pancreatic carcinoma xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.05 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to HPAF-II cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 70 h. HPAF-II cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.09 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to A431 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. A433cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.11 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to MDA-MB-231 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. MDA-MB-231 cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Tumor Growth lnhibition value (TGl)	66%	High CD79b expression (CD79b +++)
Experiment 2 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Tumor Growth lnhibition value (TGl)	86%	High CD79b expression (CD79b +++)
Experiment 3 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Tumor Growth lnhibition value (TGl)	108%	High CD79b expression (CD79b +++)
Experiment 4 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Tumor Growth lnhibition value (TGl)	125%	High CD79b expression (CD79b +++)
Experiment 5 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Tumor Growth lnhibition value (TGl)	127%	High CD79b expression (CD79b +++)

Experiment 1 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3.3 ng/mL	High CD79b expression (CD79b +++)
Method Description	A certain number of DoHH2 cells in the logarithmic growth phase were seeded into a 96-well culture plate, and drugs at different concentrations were added to the culture plate for reaction for 72 h. After the reaction was completed, an MTT working solution was added for reaction for 6h, then blue-purple crystalline formazan was dissolved with atriplex solution.    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179
Experiment 2 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	54.2 ng/mL	High CD79b expression (CD79b +++)
Method Description	A certain number of DoHH2 cells in the logarithmic growth phase were seeded into a 96-well culture plate, and drugs at different concentrations were added to the culture plate for reaction for 72 h. After the reaction was completed, an MTT working solution was added for reaction for 6h, then blue-purple crystalline formazan was dissolved with atriplex solution.    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	67%	Positive TF expression (TF+++/++)
Method Description	In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 2 mg/kg (qwk × 2, IV).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98%	Positive TF expression (TF+++/++)
Method Description	In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 4 mg/kg (qwk × 2, IV).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	132%	Positive TF expression (TF+++/++)
Method Description	The A431 epidermoid carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice. Animals were randomized and treated with drugs (5 mg/kg, qwk × 3, IP).
In Vivo Model	A431 xenograft model
Experiment 4 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	139%	Positive TF expression (TF+++/++)
Method Description	HPAF-II pancreatic carcinoma epidermoid carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice. Animals were randomized and treated with drugs (2 mg/kg, qwk × 2, IV).
In Vivo Model	HPAF-II pancreatic carcinoma xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	71%	Positive TF expression (TF+++/++)
Method Description	TF-positive PDX models were performed in athymic nude mice (Envigo, Indianapolis, IN) to evaluate the efficacy of the ADCs in vivo. The animals' care was in accordance with institutional guidelines. Study animals were implanted unilaterally on the left flank with tumor fragments. In the head and neck and ovarian PDX model, the mice were treated with drugs (2.5 mg/kg, qwk × 3, IP).    Click to Show/Hide
In Vivo Model	The head and neck and ovarian PDX model
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	112%	Positive TF expression (TF+++/++)
Method Description	TF-positive PDX models were performed in athymic nude mice (Envigo, Indianapolis, IN) to evaluate the efficacy of the ADCs in vivo. The animals' care was in accordance with institutional guidelines. Study animals were implanted unilaterally on the left flank with tumor fragments. In the gastric PDX model, the mice were treated with drugs (4 mg/kg, qwk × 2, IV).    Click to Show/Hide
In Vivo Model	The gastric PDX model
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	124%	Positive TF expression (TF+++/++)
Method Description	TF-positive PDX models were performed in athymic nude mice (Envigo, Indianapolis, IN) to evaluate the efficacy of the ADCs in vivo. The animals' care was in accordance with institutional guidelines. Study animals were implanted unilaterally on the left flank with tumor fragments. In the head and neck and ovarian PDX model, the mice were treated with drugs (5 mg/kg, qwk × 2, IP).    Click to Show/Hide
In Vivo Model	The head and neck and ovarian PDX model

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.06 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to HPAF-II cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 69 h. HPAF-II cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.11 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to A431 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. A432cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.14 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to MDA-MB-231 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. MDA-MB-231 cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Tumor Growth lnhibition value (TGl)	69%	High CD79b expression (CD79b +++)
Experiment 2 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Tumor Growth lnhibition value (TGl)	86%	High CD79b expression (CD79b +++)
Experiment 3 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Tumor Growth lnhibition value (TGl)	88%	High CD79b expression (CD79b +++)

Experiment 1 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	8.5 ng/mL	High CD79b expression (CD79b +++)
Method Description	A certain number of DoHH2 cells in the logarithmic growth phase were seeded into a 96-well culture plate, and drugs at different concentrations were added to the culture plate for reaction for 72 h. After the reaction was completed, an MTT working solution was added for reaction for 6h, then blue-purple crystalline formazan was dissolved with atriplex solution.    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179
Experiment 2 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	68.3 ng/mL	High CD79b expression (CD79b +++)
Method Description	A certain number of DoHH2 cells in the logarithmic growth phase were seeded into a 96-well culture plate, and drugs at different concentrations were added to the culture plate for reaction for 72 h. After the reaction was completed, an MTT working solution was added for reaction for 6h, then blue-purple crystalline formazan was dissolved with atriplex solution.    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	70%	Positive TF expression (TF+++/++)
Method Description	In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 2 mg/kg (qwk × 2, IV).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	92%	Positive TF expression (TF+++/++)
Method Description	In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 4 mg/kg (qwk × 2, IV).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	137%	Positive TF expression (TF+++/++)
Method Description	HPAF-II pancreatic carcinoma epidermoid carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice. Animals were randomized and treated with drugs (2 mg/kg, qwk × 2, IV).
In Vivo Model	HPAF-II pancreatic carcinoma xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.05 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to HPAF-II cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 74 h. HPAF-II cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.12 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to A431 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. A437cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.14 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to MDA-MB-231 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. MDA-MB-231 cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	73.82%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (MDA-MB-231) tumor cells, and treatmen with 2.5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.    Click to Show/Hide
In Vivo Model	MDA-MB-231 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Tumor Growth lnhibition value (TGl)	94.89%	High ROR1 expression (ROR1 +++)
Method Description	Cell line-derived xenograft models were established the back of immunodeficient mice (NCG or Balb/c nude), by subcutaneous injection of 5x106 (MDA-MB-231) tumor cells, and treatmen with 5mg/kg ADC (via the tail vein, Qw&#423) after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 28.
In Vivo Model	MDA-MB-231 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.13 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (PA-1) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 2 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.15 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (NCI-H446) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H446 cells		CVCL_1562
Experiment 3 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.18 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (HCC1187) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1187 cells		CVCL_1247
Experiment 4 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	6.25 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (NCI-N87) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	9.6 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (SK-CO-1) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SKCO1 cells		CVCL_0626
Experiment 6 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	14.72 nM	Moderate ROR1 expression (ROR1++)
Method Description	A total of 250-1500cells (COLO-678) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon carcinoma	COLO-678 cells		CVCL_1129
Experiment 7 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15.79 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (MDA-MB-231) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 8 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	17.78 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (HT-29) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	HT-29 cells		CVCL_0320
Experiment 9 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	26.67 nM	High ROR1 expression (ROR1 +++)
Method Description	A total of 250-1500cells (HCC827) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 10 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	A total of 250-1500cells (SK-BR-3) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 11 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Low ROR1 expression (ROR1+)
Method Description	A total of 250-1500cells (MCF-7) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Tumor Growth lnhibition value (TGl)	76%	High CD79b expression (CD79b +++)

Experiment 1 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3.3 ng/mL	High CD79b expression (CD79b +++)
Method Description	A certain number of DoHH2 cells in the logarithmic growth phase were seeded into a 96-well culture plate, and drugs at different concentrations were added to the culture plate for reaction for 72 h. After the reaction was completed, an MTT working solution was added for reaction for 6h, then blue-purple crystalline formazan was dissolved with atriplex solution.    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179
Experiment 2 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5.9 ng/mL	High CD79b expression (CD79b +++)
Method Description	A certain number of DoHH2 cells in the logarithmic growth phase were seeded into a 96-well culture plate, and drugs at different concentrations were added to the culture plate for reaction for 72 h. After the reaction was completed, an MTT working solution was added for reaction for 6h, then blue-purple crystalline formazan was dissolved with atriplex solution.    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179

Experiment 1 Reporting the Activity Date of This ADC					[104]
Efficacy Data	Tumor Growth lnhibition value (TGl)	80.32%	Positive her2 expression (her2+++/++)
Method Description	Cell line-derived xenograft models were established in in female BALB/c Nude mice, by subcutaneous injection of 1x106 (NCI-N87) tumor cells, and treatmen with 1.33mg/kg ADC (single dosee) after tumor volume about 198mm3. Determined tumor volume after the experiment, measured at day 36.
In Vivo Model	NCI-N87 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[104]
Efficacy Data	Tumor Growth lnhibition value (TGl)	107.47%	Positive her2 expression (her2+++/++)
Method Description	Cell line-derived xenograft models were established in in female BALB/c Nude mice, by subcutaneous injection of 1x106 (NCI-N87) tumor cells, and treatmen with 4mg/kg ADC (single dosee) after tumor volume about 198mm3. Determined tumor volume after the experiment, measured at day 36.
In Vivo Model	NCI-N87 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[104]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.008 nM	High HER2 expression (HER2 +++)
Method Description	5000cells/well for SK-BR-3 (100 uL) of cells were seeded onto 96-well plates and incubated for 24 hours before adding the ADC. After 24 hours, growth medium was replaced with ADC in growth medium. After 96 hours, viability was detected using the CellTiter-Glo® luminescence assay. Assay plates were equilibrated at room temperature for 20 minutes before addition of 100ul CellTiter-Glo® reagent per well. The plates were then mixed for 3minutes at 300 rpm to assist cell lysis and incubated for a further 20 minutes at room temperatureto stabilise the luminescence signal. Luminescence was recorded using a SpectraMax i3x platereader with a default integration time of 0.5 s/well.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 2 Reporting the Activity Date of This ADC					[104]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.228 nM	Low HER2 expression (HER2+)
Method Description	2000cells/well for JIMT-1 (100 uL) of cells were seeded onto 96-well plates and incubated for 24 hours before adding the ADC. After 24 hours, growth medium was replaced with ADC in growth medium. After 96 hours, viability was detected using the CellTiter-Glo® luminescence assay. Assay plates were equilibrated at room temperature for 20 minutes before addition of 100ul CellTiter-Glo® reagent per well. The plates were then mixed for 3minutes at 300 rpm to assist cell lysis and incubated for a further 20 minutes at room temperatureto stabilise the luminescence signal. Luminescence was recorded using a SpectraMax i3x platereader with a default integration time of 0.5 s/well.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[104]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	2500cells/well for NCI-H520 (100 uL) of cells were seeded onto 96-well plates and incubated for 24 hours before adding the ADC. After 24 hours, growth medium was replaced with ADC in growth medium. After 96 hours, viability was detected using the CellTiter-Glo® luminescence assay. Assay plates were equilibrated at room temperature for 20 minutes before addition of 100ul CellTiter-Glo® reagent per well. The plates were then mixed for 3minutes at 300 rpm to assist cell lysis and incubated for a further 20 minutes at room temperatureto stabilise the luminescence signal. Luminescence was recorded using a SpectraMax i3x platereader with a default integration time of 0.5 s/well.    Click to Show/Hide
In Vitro Model	Lung squamous cell carcinoma	NCI-H520 cells		CVCL_1566

Experiment 1 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Tumor Growth lnhibition value (TGl)	81.20%	Positive IL13Ra2 expression (IL13Ra2+++/++)
Method Description	Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper flank region with 0.5x10 6of SK-MES-1 tumor cells (a non-small cell lung cancer (NSCLC)cell line having an IL13Ra2 copy number of about 4x104)in 0.1 mL of PBS for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (10 mice per group)and received intravenous injections of PBS vehicle or a single dose of the tested ADCs at 10 mg/kg on Day 1. The end of the study was day 49.    Click to Show/Hide
In Vivo Model	CDX Model-SK-MES-1
Experiment 2 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Tumor Growth lnhibition value (TGl)	82.30%	Positive IL13Ra2 expression (IL13Ra2+++/++)
Method Description	Each female BALB/c Nude mouse was inoculated subcutaneously in the right upper/lower flank region with 1x10 7of H2228 tumor cells (an NSCLC cell line having an IL13Ra2 copy number of about 2,000)in 0.1 mL of PBS mixed with MATRIGELR (1:1)for tumor development.When the mean tumor size reached about 80-150 mm 3,mice were randomized into respective treatment groups (10 mice per group)and received intravenous injections of vehicle or a single dose of the tested ADCs at 10 mg/kg on Day 1. Body weights and tumor volumes were measured twice per week until the end of the study (Day 48).    Click to Show/Hide
In Vivo Model	CDX Model-H2228

Experiment 1 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01 nM	High hIL13Ra2 expression (hIL13Ra2 +++)
Method Description	The cytotoxic activity of ADC 22-2 was determined against cancer cell lines A375.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model	Amelanotic melanoma	A375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02-0.03 nM	Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description	The cytotoxic activity of ADC 22-2 was determined against cancer cell lines H1792.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model	Lung adenocarcinoma	H1792 cells		CVCL_1495
Experiment 3 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04-0.08 nM	Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description	The cytotoxic activity of ADC 22-2 was determined against cancer cell lines H2228.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model	Lung adenocarcinoma	H2228 cells		CVCL_1543
Experiment 4 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3-63 nM	Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description	The cytotoxic activity of ADC 22-2 was determined against cancer cell lines SK-MES-1.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model	Lung squamous cell carcinoma	SK-MES-1 cells		CVCL_0630

Experiment 1 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Tumor Growth lnhibition value (TGl)	≈ 85%	Positive CD138 expression (CD138+++/++)
Method Description	1x107cells/100 uL, ADC3 at 1 mg/kg, intravenous injection,
In Vivo Model	Capan-1 derived Xenograft Model
Experiment 2 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Tumor Growth lnhibition value (TGl)	≈ 98%	Positive CD138 expression (CD138+++/++)
Method Description	1x107cells/100 uL, ADC3 at 1 mg/kg, intravenous injection,
In Vivo Model	Capan-1 derived Xenograft Model

Experiment 1 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	13 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 2 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2357 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 1 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Tumor Growth lnhibition value (TGl)	≈ 85%	Positive CD138 expression (CD138+++/++)
Method Description	1x107cells/100 uL, ADC3 at 1 mg/kg, intravenous injection,
In Vivo Model	Capan-1 derived Xenograft Model

Experiment 1 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	21 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 2 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4028 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 1 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Tumor Growth lnhibition value (TGl)	≈ 85%	Positive CD138 expression (CD138+++/++)
Method Description	1x107cells/100 uL, ADC3 at 1 mg/kg, intravenous injection,
In Vivo Model	Capan-1 derived Xenograft Model

Experiment 1 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	40 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 2 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4377 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 1 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Tumor Growth lnhibition value (TGl)	≈ 85%	Positive CD138 expression (CD138+++/++)
Method Description	1x107cells/100 uL, ADC3 at 1 mg/kg, intravenous injection,
In Vivo Model	Capan-1 derived Xenograft Model

Experiment 1 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	57 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 2 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4761 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 1 Reporting the Activity Date of This ADC					[106]
Efficacy Data	Tumor Growth lnhibition value (TGl)	85.15%
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					[106]
Efficacy Data	Tumor Growth Inhibition value (TGI)	38.69%
Method Description	Cell line-derived xenograft models were established in SCID-17B female mice, by subcutaneous injection of 5x106 (NCI-H1650) tumor cells, and treatmen with 2.5mg/kg ADC (single dosee) after tumor volume about 137mm3. Determined tumor volume after the experiment, measured at day 31.
In Vivo Model	NCI-H1650 breast tumor model
Experiment 3 Reporting the Activity Date of This ADC					[106]
Efficacy Data	Tumor Growth Inhibition value (TGI)	62.06%
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 4 Reporting the Activity Date of This ADC					[106]
Efficacy Data	Tumor Growth Inhibition value (TGI)	107.99%
Method Description	Cell line-derived xenograft models were established in SCID-17B female mice, by subcutaneous injection of 5x106 (NCI-H1650) tumor cells, and treatmen with 5mg/kg ADC (single dosee) after tumor volume about 137mm3. Determined tumor volume after the experiment, measured at day 31.
In Vivo Model	NCI-H1650 breast tumor model
Experiment 5 Reporting the Activity Date of This ADC					[106]
Efficacy Data	Tumor Growth Inhibition value (TGI)	107.99%
Method Description	Cell line-derived xenograft models were established in SCID-17B female mice, by subcutaneous injection of 5x106 (NCI-H1650) tumor cells, and treatmen with 5mg/kg ADC (single dosee) after tumor volume about 137mm3. Determined tumor volume after the experiment, measured at day 31.
In Vivo Model	NCI-H1650 breast tumor model
Experiment 6 Reporting the Activity Date of This ADC					[106]
Efficacy Data	Tumor Growth Inhibition value (TGI)	122.67%
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 2.5mg/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					[106]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0..011 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					[106]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.027 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 3 Reporting the Activity Date of This ADC					[106]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.065 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 4 Reporting the Activity Date of This ADC					[106]
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					[106]
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					[106]
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					[106]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.023 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					[106]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.18 nM
Method Description	The thawed antibodies were serially diluted and added to 1x103 well (HCT-116) and incubated for 1 hourat 4°C.ADC were added to the cells and incubated at 4°C for30 minutes. Cells were washed twice in the same bufer andthe mean fluorescence (MFl) of stained cells was measuredusing a FACS Canto I cytometer (BD Biosciences)andanalyzed by FlowJo. Wells containing no antibody or sec-ondary antibody only were used to establish background fluorescence. Four-parameter non-linear regression analysiswas used to obtain EC50 values for cell binding usingGraphPad Prism6 software at Day14.    Click to Show/Hide
Experiment 9 Reporting the Activity Date of This ADC					[106]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.22 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					[92]
Efficacy Data	Tumor Growth lnhibition value (TGl)	91%	High CD79b expression (CD79b +++)

Experiment 1 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2 ng/mL	High CD79b expression (CD79b +++)
Method Description	A certain number of DoHH2 cells in the logarithmic growth phase were seeded into a 96-well culture plate, and drugs at different concentrations were added to the culture plate for reaction for 72 h. After the reaction was completed, an MTT working solution was added for reaction for 6h, then blue-purple crystalline formazan was dissolved with atriplex solution.    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179
Experiment 2 Reporting the Activity Date of This ADC					[92]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	53.4 ng/mL	High CD79b expression (CD79b +++)
Method Description	A certain number of DoHH2 cells in the logarithmic growth phase were seeded into a 96-well culture plate, and drugs at different concentrations were added to the culture plate for reaction for 72 h. After the reaction was completed, an MTT working solution was added for reaction for 6h, then blue-purple crystalline formazan was dissolved with atriplex solution.    Click to Show/Hide
In Vitro Model	Diffuse large B-cell lymphoma germinal center B-cell type	DoHH2 cells		CVCL_1179

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	92%	Positive TF expression (TF+++/++)
Method Description	In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 2 mg/kg (qwk × 2, IV).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	99%	Positive TF expression (TF+++/++)
Method Description	In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 4 mg/kg (qwk × 2, IV).
In Vivo Model	MDA-MB-231 xenograft model
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	137%	Positive TF expression (TF+++/++)
Method Description	HPAF-II pancreatic carcinoma epidermoid carcinoma cell lines were implanted subcutaneously in the flank of athymic nude mice. Animals were randomized and treated with drugs (2 mg/kg, qwk × 2, IV).
In Vivo Model	HPAF-II pancreatic carcinoma xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to HPAF-II cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 73 h. HPAF-II cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.05 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to MDA-MB-231 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. MDA-MB-231 cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.08 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to A431 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. A436cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[107]
Efficacy Data	Tumor Growth lnhibition value (TGl)	96.70%
Method Description	For the in vivo efficacy studies, orthotopic TNBC tumors (MDA-MB-436 or MDA-MB-231) were established in 6- to 8-week-old female nude mice as described above. Tumors were grown to reach 100 mm3 for standard setting treatment or 500 mm3 for late-stage treatment. Then, tumor-bearing mice were randomly divided into various treatment groups (n ≥ 5 per group) and received treatment of PBS (sham), free Dox, IC1 Ab, IC1-MMAE, or IC1-MMAF at an equivalent dosage of 5 mg/kg per week for 3 weeks via tail vein injection. Tumor growth was monitored weekly using a caliper. At the end point, animals were euthanized with CO2 and orthotopic tumors were excised to measure their mass. In dosage-dependent experiments, three ascending IC1-MMAE dosages (1, 5, and 10 mg/kg) were evaluated in orthotopic TNBC tumors (MDA-MB-436) using the same protocol. Then, mice were euthanized with CO2 and 500 ul of mouse blood was collected immediately via cardiac puncture. Collected blood was incubated for 20 min at RT to allow clotting, and then mouse serum was isolated after centrifuging at 2000g for 10 min in a refrigerated centrifuge. Serum levels of ALT, AST, creatinine, and BUN were determined using their activity assay kits purchased from Sigma-Aldrich (St. Louis, MO, USA) with provided protocols. In MTD studies, the in vivo tolerability of IC1-MMAE was examined in 6- to 8-week-old female BALB/c mice. Healthy mice were randomized into various treatment groups (n = 10 per group) and received intravenous injections of IC1-MMAE at three ascending dosages (25, 50, and 75 mg/kg) for one injection. After injection, mouse body weight loss was used as the acute toxicity indicator and was closely monitored for up to 14 days.    Click to Show/Hide
In Vivo Model	Refractory MDA-MB-231 tumor model
Experiment 2 Reporting the Activity Date of This ADC					[107]
Efficacy Data	Tumor Growth lnhibition value (TGl)	99.50%
Method Description	For the in vivo efficacy studies, orthotopic TNBC tumors (MDA-MB-436 or MDA-MB-231) were established in 6- to 8-week-old female nude mice as described above. Tumors were grown to reach 100 mm3 for standard setting treatment or 500 mm3 for late-stage treatment. Then, tumor-bearing mice were randomly divided into various treatment groups (n ≥ 5 per group) and received treatment of PBS (sham), free Dox, IC1 Ab, IC1-MMAE, or IC1-MMAF at an equivalent dosage of 5 mg/kg per week for 3 weeks via tail vein injection. Tumor growth was monitored weekly using a caliper. At the end point, animals were euthanized with CO2 and orthotopic tumors were excised to measure their mass. In dosage-dependent experiments, three ascending IC1-MMAE dosages (1, 5, and 10 mg/kg) were evaluated in orthotopic TNBC tumors (MDA-MB-436) using the same protocol. Then, mice were euthanized with CO2 and 500 ul of mouse blood was collected immediately via cardiac puncture. Collected blood was incubated for 20 min at RT to allow clotting, and then mouse serum was isolated after centrifuging at 2000g for 10 min in a refrigerated centrifuge. Serum levels of ALT, AST, creatinine, and BUN were determined using their activity assay kits purchased from Sigma-Aldrich (St. Louis, MO, USA) with provided protocols. In MTD studies, the in vivo tolerability of IC1-MMAE was examined in 6- to 8-week-old female BALB/c mice. Healthy mice were randomized into various treatment groups (n = 10 per group) and received intravenous injections of IC1-MMAE at three ascending dosages (25, 50, and 75 mg/kg) for one injection. After injection, mouse body weight loss was used as the acute toxicity indicator and was closely monitored for up to 14 days.    Click to Show/Hide
In Vivo Model	MDA-MB-436 orthotopic TNBC model

Experiment 1 Reporting the Activity Date of This ADC					[107]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	13.1 pM	Moderate ICAM1 expression (ICAM1++)
Method Description	Cells were seeded in a 96-well plate at a density of 5 × 103 cells per well and allowed to attach overnight. Then, cells were treated with four different ICAM1 ADCs (IC1-DM1, IC1-DM4, IC1-MMAE, and IC1-MMAF) at different drug concentrations ranging from 0 to 10 ug/ml using a serial dilution factor of 10. After cells were cultured for another 48 hours, the cytotoxicity was determined by CCK-8 assay. The plate was read at the absorbance wavelength of 450 nm using a Molecular Devices SpectraMax microplate reader (San Jose, CA, USA). Cell viability was determined by comparing the absorbance of cells incubated with drugs to that of the control cells incubated without the presence of the drug.    Click to Show/Hide
In Vitro Model	Metastasis of ductal carcinoma	MDA-MB-436 cells		CVCL_0623
Experiment 2 Reporting the Activity Date of This ADC					[107]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	221.7 pM	Moderate ICAM1 expression (ICAM1++)
Method Description	Cells were seeded in a 96-well plate at a density of 5 × 103 cells per well and allowed to attach overnight. Then, cells were treated with four different ICAM1 ADCs (IC1-DM1, IC1-DM4, IC1-MMAE, and IC1-MMAF) at different drug concentrations ranging from 0 to 10 ug/ml using a serial dilution factor of 10. After cells were cultured for another 48 hours, the cytotoxicity was determined by CCK-8 assay. The plate was read at the absorbance wavelength of 450 nm using a Molecular Devices SpectraMax microplate reader (San Jose, CA, USA). Cell viability was determined by comparing the absorbance of cells incubated with drugs to that of the control cells incubated without the presence of the drug.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[107]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	250 pM	High ICAM1 expression (ICAM1 +++)
Method Description	Cells were seeded in a 96-well plate at a density of 5 × 103 cells per well and allowed to attach overnight. Then, cells were treated with four different ICAM1 ADCs (IC1-DM1, IC1-DM4, IC1-MMAE, and IC1-MMAF) at different drug concentrations ranging from 0 to 10 ug/ml using a serial dilution factor of 10. After cells were cultured for another 48 hours, the cytotoxicity was determined by CCK-8 assay. The plate was read at the absorbance wavelength of 450 nm using a Molecular Devices SpectraMax microplate reader (San Jose, CA, USA). Cell viability was determined by comparing the absorbance of cells incubated with drugs to that of the control cells incubated without the presence of the drug.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Tumor Growth lnhibition value (TGl)	97%	Positive TF expression (TF+++/++)
Method Description	In the MDA-MB-231 xenograft model, the ADCs were administered on day 1 and 8 post-randomization at 4 mg/kg (qwk × 2, IV).
In Vivo Model	MDA-MB-231 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to HPAF-II cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 72 h. HPAF-II cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to MDA-MB-231 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. MDA-MB-231 cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to A431 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. A435cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[108]
Efficacy Data	Tumor Growth lnhibition value (TGl)	98.30%
Method Description	Next, we further increased the dose to 6 mg/kg, 4XQ1W and found that F12-MMAE almost eradicated tumors (complete remission, CR; %TGI = 98.3%) : For evaluation of in vivo ADCC effects of IgG1 F12, PC-3-PSCA cells (5 × 106 cells/mouse) in 200 ul of 1:1 PBS/Matrigel (BD Biosciences, Cat# 354234) were injected subcutaneously (s.c.) into the right flank of the Balb/c scid mice. When tumor volume reached 100 mm3, mice were divided randomly into IgG1 F12 treatment or vehicle group and i.p. administered four times total with a four-day interval. For evaluation of the ADC (F12-MMAE or Ab1-MMAE) efficacy in vivo, PC-3-PSCA cells (5 × 106 cells/mouse, 5 mice per group) in 200 ul of 1:1 PBS/Matrigel were injected s.c. into the right flank of the NSG mice. Mice were randomly divided into the different treatment groups when tumors reached 100 mm3. We conducted ADC treatment studies at three different dosing regimens, comparing PSCA-ADC with the isotype control Ab1-ADC. The regimens design were as follows: dose 1): 1 mg/kg and 3 mg/kg, administered twice weekly (2XQ1W); dose 2): 6 mg/kg, administered twice weekly (2XQ1W), followed by a single injection of 3 mg/kg when tumors regrew to 140 mm3; dose 3): 6 mg/kg, administered four times weekly (4XQ1W). All ADCs were i.p. administered. Tumor dimensions and mouse weight were measured periodically with a slide caliper and scale. Tumor volume was calculated by the formula: V = 0.5×length × (width)2. Tumor growth inhibition was calculated by the formula: %TGI = [1- (mean tumor volume (MTV)ADC treated/MTVcontrol)] × 100. Mice were euthanized when the tumor volume exceeded 1000 mm3 or if the animals showed any signs of suffering. At the end of the experiment time point, tumors were isolated and weighed. In the dose 2 experiment, one week after two 6 mg/kg ADC treatments, ~50 ul blood were collected to the purple-topped K+/EDTA tubes, and subjected to complete blood counts using the Abaxis HM5 machine from In vivo Imaging Facilities in Hillman Cancer Center of the University of Pittsburgh. In the dose 3 experiment (6 mg/kg, 4×Q1W), mouse spleen, kidney, heart, lung, and liver were collected and fixed in formalin. The H&E staining were completed by the Biospecimen Core of the University of Pittsburgh.    Click to Show/Hide
In Vivo Model	PC-3-PSCA xenograft mouse model

Experiment 1 Reporting the Activity Date of This ADC					[108]
Efficacy Data	Half Maximal Effective Concentration (EC50)	5.41 nM	High PSCA expression (PSCA +++)
Method Description	The PC-3 or PC-3-PSCA cells (2.5 × 104 cells) were pre-seeded in 96-well plates overnight. The cells were then incubated with serially diluted ADC, or naked IgG1 antibody or linker-payload combination compound for 4-5 days at 37°C, 8% CO2 with 95% humidity. Then the cell viability was detected by the Promega CellTiter-Glo® Luminescent Cell Viability Assay (CAT# G7570), which is based on quantitation of the ATP present, an indicator of metabolically active cells. The Luminescence was recorded by the BioTek synergy multi-mode reader (Winooski, VT). The killing percentage was calculated by the formula: (1-Lumi with compounds/Lumi without compounds) ×100. The GraphPad Prism9 for was used for calculation of killing IC50. All experiments were performed in duplicate and the error bars denote ±1 SD.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	PC-3-PSCA cells		CVCL_0035

Experiment 1 Reporting the Activity Date of This ADC					[109]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 100%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[109]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[109]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 100%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[109]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[109]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 101%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[109]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[109]
Efficacy Data	Tumor Growth lnhibition value (TGl)	> 102%	Positive HER2 expression (HER2+++/++)
Method Description	A mixed solvent of PBS and and Matrigel was used to prepare a cell suspension of 5.0x107 cells / mL. The prepared cell suspension was subcutaneously injected to the right flank region of female BALB/c-nu/nu mice at 0.1 mL per mouse. Individuals having a tumor volume within a range of 50 to 500 mm 3 were selected. test compound at a concentration of 3 mg/kg or the solvent alone was intravenously administered. the tumor volume was measured at Day 0 and Day 21.    Click to Show/Hide
In Vivo Model	NCI-N87 female BALB/c-nu/nu mice model

Experiment 1 Reporting the Activity Date of This ADC					[109]
Efficacy Data	Cell growth inhibition rate (%)	> 14%	Positive HER2 expression (HER2+++/++)
Method Description	Cell growth inhibition test was carried out on HER2-positive human gastric cancer cell line (NCI-N87), the cells were treated with a test compound or an anti-HER2 antibody (trastuzumab) at a concentration of 100 ng/mL. The cells were cultured for 6 days, then CellTiter-Glo was added and the luminescence amount was measured.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[110]
Efficacy Data	Tumor Growth lnhibition value (TGl)	115.07%	Positive her2 expression (her2+++/++)
Method Description	Cell line-derived xenograft models were established in female nude mice (BALB/C),by subcutaneous injection of 1x106 (NCI-N87) tumor cells, and treatment with 3mg/kg ADC after tumor volume about 100-300mm3. Determined tumor volume after the experiment, measured at day 35.
In Vivo Model	NCI-N87 xenograft model

Experiment 1 Reporting the Activity Date of This ADC					[110]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	. nM	Negativeher2 expression (her2-)
Method Description	HepG2 at 100uL/well (1000 to 10000 cells), 0.9mg/ml ADCs (10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015, and 0.00051 nM) were added and incubated for 72 to 120 h, then 100 L of CellTiter Glo reagent was added into each well, a shaker shook for 2 min, followed by standing in a dark place at rt for 10 min, and the relative light unit (RLU) was measured with a Cytation 3 microplate reader.    Click to Show/Hide
In Vitro Model	Hepatoblastoma	HepG2 cells		CVCL_0027
Experiment 2 Reporting the Activity Date of This ADC					[110]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04636 nM	Positive her2 expression (her2+++/++)
Method Description	BT-474 at 100uL/well (1000 to 10000 cells), 0.9mg/ml ADCs (10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015, and 0.00051 nM) were added and incubated for 72 to 120 h, then 100 L of CellTiter Glo reagent was added into each well, a shaker shook for 2 min, followed by standing in a dark place at rt for 10 min, and the relative light unit (RLU) was measured with a Cytation 3 microplate reader.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[110]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.08706 nM	Positive her2 expression (her2+++/++)
Method Description	NCI-N87 at 100uL/well (1000 to 10000 cells), 0.9mg/ml ADCs (10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015, and 0.00051 nM) were added and incubated for 72 to 120 h, then 100 L of CellTiter Glo reagent was added into each well, a shaker shook for 2 min, followed by standing in a dark place at rt for 10 min, and the relative light unit (RLU) was measured with a Cytation 3 microplate reader.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[110]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.045 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	Ntera-2 cell at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.    Click to Show/Hide
In Vitro Model	Embryonal carcinoma	Ntera-2 cells		CVCL_0034
Experiment 5 Reporting the Activity Date of This ADC					[110]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 nM	Negative ROR1 expression (ROR1-)
Method Description	MCF-7 cells at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[98]
Efficacy Data	Tumor Growth lnhibition value (TGl)	115.07%
Method Description	Inhibition Effect of ADC-1,3mg/kg on NCI-N87 CDX Mouse Model
In Vivo Model	NCI-N87 CDX Mouse Model

Experiment 1 Reporting the Activity Date of This ADC					[98]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04636 nM
Method Description	Proliferation Inhibition Effect of Different Drugs on Tumor Cells (IC50, nM)in BT-474,
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[98]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.08706 nM
Method Description	Proliferation Inhibition Effect of Different Drugs on Tumor Cells (IC50, nM)in NCI-N87
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[111]
Efficacy Data	half-maximal cytotoxicity Concentration (CC50)	0.582 nM	High TROP2 expression (TROP2 +++)
Method Description	Specifically, human pancreatic cancer cell lines (BxPC - 3, Capan - 1 and PATU - 8988s), breast cancer cell lines (JIMT - 1 and MDA - MB - 468), gastric cancer cell lines (NCI - N87, SNU - 601 and SNU - 620), colon cancer cell lines (HCT15, HT29, DLD - 1, SW480 and COLO205), ovarian cancer cell lines (OVCAR - 3), prostate cancer cell lines (PC - 3 and LNCaP) and Non small cell lung cancer cell lines (NCI - H1781, HCC827, Calu - 1 and Calu - 3). Use MMAE in standalone drug form and SG2057 (cAS #: 260417-62-7, MedKooBiosciences) as PBD dimer included in the ADC prepared according to Example 3. Inoculate each cancer cell line from 500 cells/well to 5000 cells/well into a 96 well plate and culture for 24 hours, followed by treatment with concentrations ranging from 0.256pM to 100nM (5-fold continuous dilution) of ADC1, ADC2, and ADC3 produced according to Example 3, as well as individual drugs MMAE and SG2057. After 144 hours, the number of live cells was quantified using sulforhodamine B (SRB) dye or Cell titrer glo.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[111]
Efficacy Data	half-maximal cytotoxicity Concentration (CC50)	1.412 nM	High TROP2 expression (TROP2 +++)
Method Description	Specifically, human pancreatic cancer cell lines (BxPC - 3, Capan - 1 and PATU - 8988s), breast cancer cell lines (JIMT - 1 and MDA - MB - 468), gastric cancer cell lines (NCI - N87, SNU - 601 and SNU - 620), colon cancer cell lines (HCT15, HT29, DLD - 1, SW480 and COLO205), ovarian cancer cell lines (OVCAR - 3), prostate cancer cell lines (PC - 3 and LNCaP) and Non small cell lung cancer cell lines (NCI - H1781, HCC827, Calu - 1 and Calu - 3). Use MMAE in standalone drug form and SG2057 (cAS #: 260417-62-7, MedKooBiosciences) as PBD dimer included in the ADC prepared according to Example 3. Inoculate each cancer cell line from 500 cells/well to 5000 cells/well into a 96 well plate and culture for 24 hours, followed by treatment with concentrations ranging from 0.256pM to 100nM (5-fold continuous dilution) of ADC1, ADC2, and ADC3 produced according to Example 3, as well as individual drugs MMAE and SG2057. After 144 hours, the number of live cells was quantified using sulforhodamine B (SRB) dye or Cell titrer glo.    Click to Show/Hide
In Vitro Model	Pancreatic adenocarcinoma	Patu8988s cells		CVCL_1846
Experiment 3 Reporting the Activity Date of This ADC					[111]
Efficacy Data	half-maximal cytotoxicity Concentration (CC50)	3.538 nM	High TROP2 expression (TROP2 +++)
Method Description	Specifically, human pancreatic cancer cell lines (BxPC - 3, Capan - 1 and PATU - 8988s), breast cancer cell lines (JIMT - 1 and MDA - MB - 468), gastric cancer cell lines (NCI - N87, SNU - 601 and SNU - 620), colon cancer cell lines (HCT15, HT29, DLD - 1, SW480 and COLO205), ovarian cancer cell lines (OVCAR - 3), prostate cancer cell lines (PC - 3 and LNCaP) and Non small cell lung cancer cell lines (NCI - H1781, HCC827, Calu - 1 and Calu - 3). Use MMAE in standalone drug form and SG2057 (cAS #: 260417-62-7, MedKooBiosciences) as PBD dimer included in the ADC prepared according to Example 3. Inoculate each cancer cell line from 500 cells/well to 5000 cells/well into a 96 well plate and culture for 24 hours, followed by treatment with concentrations ranging from 0.256pM to 100nM (5-fold continuous dilution) of ADC1, ADC2, and ADC3 produced according to Example 3, as well as individual drugs MMAE and SG2057. After 144 hours, the number of live cells was quantified using sulforhodamine B (SRB) dye or Cell titrer glo.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-3 cells		CVCL_0609
Experiment 4 Reporting the Activity Date of This ADC					[111]
Efficacy Data	half-maximal cytotoxicity Concentration (CC50)	4.043 nM	High TROP2 expression (TROP2 +++)
Method Description	Specifically, human pancreatic cancer cell lines (BxPC - 3, Capan - 1 and PATU - 8988s), breast cancer cell lines (JIMT - 1 and MDA - MB - 468), gastric cancer cell lines (NCI - N87, SNU - 601 and SNU - 620), colon cancer cell lines (HCT15, HT29, DLD - 1, SW480 and COLO205), ovarian cancer cell lines (OVCAR - 3), prostate cancer cell lines (PC - 3 and LNCaP) and Non small cell lung cancer cell lines (NCI - H1781, HCC827, Calu - 1 and Calu - 3). Use MMAE in standalone drug form and SG2057 (cAS #: 260417-62-7, MedKooBiosciences) as PBD dimer included in the ADC prepared according to Example 3. Inoculate each cancer cell line from 500 cells/well to 5000 cells/well into a 96 well plate and culture for 24 hours, followed by treatment with concentrations ranging from 0.256pM to 100nM (5-fold continuous dilution) of ADC1, ADC2, and ADC3 produced according to Example 3, as well as individual drugs MMAE and SG2057. After 144 hours, the number of live cells was quantified using sulforhodamine B (SRB) dye or Cell titrer glo.    Click to Show/Hide
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 5 Reporting the Activity Date of This ADC					[111]
Efficacy Data	half-maximal cytotoxicity Concentration (CC50)	4.639 nM	High TROP2 expression (TROP2 +++)
Method Description	Specifically, human pancreatic cancer cell lines (BxPC - 3, Capan - 1 and PATU - 8988s), breast cancer cell lines (JIMT - 1 and MDA - MB - 468), gastric cancer cell lines (NCI - N87, SNU - 601 and SNU - 620), colon cancer cell lines (HCT15, HT29, DLD - 1, SW480 and COLO205), ovarian cancer cell lines (OVCAR - 3), prostate cancer cell lines (PC - 3 and LNCaP) and Non small cell lung cancer cell lines (NCI - H1781, HCC827, Calu - 1 and Calu - 3). Use MMAE in standalone drug form and SG2057 (cAS #: 260417-62-7, MedKooBiosciences) as PBD dimer included in the ADC prepared according to Example 3. Inoculate each cancer cell line from 500 cells/well to 5000 cells/well into a 96 well plate and culture for 24 hours, followed by treatment with concentrations ranging from 0.256pM to 100nM (5-fold continuous dilution) of ADC1, ADC2, and ADC3 produced according to Example 3, as well as individual drugs MMAE and SG2057. After 144 hours, the number of live cells was quantified using sulforhodamine B (SRB) dye or Cell titrer glo.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 6 Reporting the Activity Date of This ADC					[111]
Efficacy Data	half-maximal cytotoxicity Concentration (CC50)	6.104 nM	High TROP2 expression (TROP2 +++)
Method Description	Specifically, human pancreatic cancer cell lines (BxPC - 3, Capan - 1 and PATU - 8988s), breast cancer cell lines (JIMT - 1 and MDA - MB - 468), gastric cancer cell lines (NCI - N87, SNU - 601 and SNU - 620), colon cancer cell lines (HCT15, HT29, DLD - 1, SW480 and COLO205), ovarian cancer cell lines (OVCAR - 3), prostate cancer cell lines (PC - 3 and LNCaP) and Non small cell lung cancer cell lines (NCI - H1781, HCC827, Calu - 1 and Calu - 3). Use MMAE in standalone drug form and SG2057 (cAS #: 260417-62-7, MedKooBiosciences) as PBD dimer included in the ADC prepared according to Example 3. Inoculate each cancer cell line from 500 cells/well to 5000 cells/well into a 96 well plate and culture for 24 hours, followed by treatment with concentrations ranging from 0.256pM to 100nM (5-fold continuous dilution) of ADC1, ADC2, and ADC3 produced according to Example 3, as well as individual drugs MMAE and SG2057. After 144 hours, the number of live cells was quantified using sulforhodamine B (SRB) dye or Cell titrer glo.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 7 Reporting the Activity Date of This ADC					[111]
Efficacy Data	half-maximal cytotoxicity Concentration (CC50)	18.06 nM	High TROP2 expression (TROP2 +++)
Method Description	Specifically, human pancreatic cancer cell lines (BxPC - 3, Capan - 1 and PATU - 8988s), breast cancer cell lines (JIMT - 1 and MDA - MB - 468), gastric cancer cell lines (NCI - N87, SNU - 601 and SNU - 620), colon cancer cell lines (HCT15, HT29, DLD - 1, SW480 and COLO205), ovarian cancer cell lines (OVCAR - 3), prostate cancer cell lines (PC - 3 and LNCaP) and Non small cell lung cancer cell lines (NCI - H1781, HCC827, Calu - 1 and Calu - 3). Use MMAE in standalone drug form and SG2057 (cAS #: 260417-62-7, MedKooBiosciences) as PBD dimer included in the ADC prepared according to Example 3. Inoculate each cancer cell line from 500 cells/well to 5000 cells/well into a 96 well plate and culture for 24 hours, followed by treatment with concentrations ranging from 0.256pM to 100nM (5-fold continuous dilution) of ADC1, ADC2, and ADC3 produced according to Example 3, as well as individual drugs MMAE and SG2057. After 144 hours, the number of live cells was quantified using sulforhodamine B (SRB) dye or Cell titrer glo.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	Capan-1 cells		CVCL_0237

Experiment 1 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC70)	1556 nM
Method Description	Tumor cells (A375) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Amelanotic melanoma	A375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC64)	223 nM
Method Description	Tumor cells (IGR37) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Melanoma	IGR37 cells		CVCL_2075
Experiment 3 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC64)	1823 nM	Moderate MELTF expression (MELTF++)
Method Description	Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 4 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC63)	8.5 nM
Method Description	Tumor cells (Colo853) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	Colo853 cells		CVCL_2003
Experiment 5 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC56)	3.9 nM
Method Description	Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 6 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5.9 nM
Method Description	Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527

Experiment 1 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC65)	14.9 nM
Method Description	Tumor cells (A375) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Amelanotic melanoma	A375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC64)	7.3 nM	Moderate MELTF expression (MELTF++)
Method Description	Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 3 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC64)	13.7 nM
Method Description	Tumor cells (IGR37) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Melanoma	IGR37 cells		CVCL_2075
Experiment 4 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC58)	3.7 nM
Method Description	Tumor cells (Colo853) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	Colo853 cells		CVCL_2003
Experiment 5 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC51)	2.5 nM
Method Description	Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 6 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.8 nM
Method Description	Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527

Experiment 1 Reporting the Activity Date of This ADC					[110]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	. nM	Negative TROP2 expression (TROP2-)
Method Description	HepG2 at 100uL/well (1000 to 10000 cells), 0.9mg/ml ADCs (10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015, and 0.00051 nM) were added and incubated for 72 to 120 h, then 100 L of CellTiter Glo reagent was added into each well, a shaker shook for 2 min, followed by standing in a dark place at rt for 10 min, and the relative light unit (RLU) was measured with a Cytation 3 microplate reader.    Click to Show/Hide
In Vitro Model	Hepatoblastoma	HepG2 cells		CVCL_0027
Experiment 2 Reporting the Activity Date of This ADC					[110]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.09995 nM	High TROP2 expression (TROP2 +++)
Method Description	BxPC-3 at 100uL/well (1000 to 10000 cells), 0.9mg/ml ADCs (10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015, and 0.00051 nM) were added and incubated for 72 to 120 h, then 100 L of CellTiter Glo reagent was added into each well, a shaker shook for 2 min, followed by standing in a dark place at rt for 10 min, and the relative light unit (RLU) was measured with a Cytation 3 microplate reader.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[110]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1297 nM	High TROP2 expression (TROP2 +++)
Method Description	FaDu at 100uL/well (1000 to 10000 cells), 0.9mg/ml ADCs (10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015, and 0.00051 nM) were added and incubated for 72 to 120 h, then 100 L of CellTiter Glo reagent was added into each well, a shaker shook for 2 min, followed by standing in a dark place at rt for 10 min, and the relative light unit (RLU) was measured with a Cytation 3 microplate reader.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 4 Reporting the Activity Date of This ADC					[110]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	Ntera-2 cell at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.    Click to Show/Hide
In Vitro Model	Embryonal carcinoma	Ntera-2 cells		CVCL_0034
Experiment 5 Reporting the Activity Date of This ADC					[110]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 nM	Negative ROR1 expression (ROR1-)
Method Description	MCF-7 cells at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[110]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	. nM	Negative TROP2 expression (TROP2-)
Method Description	HepG2 at 100uL/well (1000 to 10000 cells), 0.9mg/ml ADCs (10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015, and 0.00051 nM) were added and incubated for 72 to 120 h, then 100 L of CellTiter Glo reagent was added into each well, a shaker shook for 2 min, followed by standing in a dark place at rt for 10 min, and the relative light unit (RLU) was measured with a Cytation 3 microplate reader.    Click to Show/Hide
In Vitro Model	Hepatoblastoma	HepG2 cells		CVCL_0027
Experiment 2 Reporting the Activity Date of This ADC					[110]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1017 nM	High TROP2 expression (TROP2 +++)
Method Description	BxPC-3 at 100uL/well (1000 to 10000 cells), 0.9mg/ml ADCs (10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015, and 0.00051 nM) were added and incubated for 72 to 120 h, then 100 L of CellTiter Glo reagent was added into each well, a shaker shook for 2 min, followed by standing in a dark place at rt for 10 min, and the relative light unit (RLU) was measured with a Cytation 3 microplate reader.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[110]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1121 nM	High TROP2 expression (TROP2 +++)
Method Description	FaDu at 100uL/well (1000 to 10000 cells), 0.9mg/ml ADCs (10, 3.3, 1.1, 0.37, 0.12, 0.041, 0.014, 0.0046, 0.0015, and 0.00051 nM) were added and incubated for 72 to 120 h, then 100 L of CellTiter Glo reagent was added into each well, a shaker shook for 2 min, followed by standing in a dark place at rt for 10 min, and the relative light unit (RLU) was measured with a Cytation 3 microplate reader.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218

Experiment 1 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.006 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 2 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.017 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.019 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.066 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 5 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.086 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Breast acantholytic squamous cell carcinoma	HCC-1806 cells		CVCL_1258
Experiment 6 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236

Experiment 1 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.008 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 2 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.021 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.035 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.067 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 5 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.076 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Breast acantholytic squamous cell carcinoma	HCC-1806 cells		CVCL_1258
Experiment 6 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236

Experiment 1 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.009 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 2 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.064 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.078 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 4 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.183 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 5 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3.184 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Breast acantholytic squamous cell carcinoma	HCC-1806 cells		CVCL_1258
Experiment 6 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236

Experiment 1 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01 nM	High hIL13Ra2 expression (hIL13Ra2 +++)
Method Description	The cytotoxic activity of ADC 52-2 was determined against cancer cell lines A375.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model	Amelanotic melanoma	A375 cells		CVCL_0132
Experiment 2 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02-0.03 nM	Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description	The cytotoxic activity of ADC 52-2 was determined against cancer cell lines H1792.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model	Lung adenocarcinoma	H1792 cells		CVCL_1495
Experiment 3 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04-0.08 nM	Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description	The cytotoxic activity of ADC 52-2 was determined against cancer cell lines H2228.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model	Lung adenocarcinoma	H2228 cells		CVCL_1543
Experiment 4 Reporting the Activity Date of This ADC					[99]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3-63 nM	Positive hIL13Ra2 expression (hIL13Ra2+++/++)
Method Description	The cytotoxic activity of ADC 52-2 was determined against cancer cell lines SK-MES-1.FITC and anti-Hen egg-white lysozyme isotype control antibody (HEWL)conjugated to the same linker payloads.
In Vitro Model	Lung squamous cell carcinoma	SK-MES-1 cells		CVCL_0630

Experiment 1 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.011 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 2 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.056 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.073 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.233 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 5 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.592 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Breast acantholytic squamous cell carcinoma	HCC-1806 cells		CVCL_1258
Experiment 6 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236

Experiment 1 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.014 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma, Multiple myeloma	KMS-27 cells		CVCL_2993
Experiment 2 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.016 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600
Experiment 3 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.021 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Multiple myeloma	KMS-21 cells		CVCL_2991
Experiment 4 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.037 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma, Multiple myeloma	KMS-20 cells		CVCL_2990

Experiment 1 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.016 nM	Positive HER2 expression (HER2+++/++)
Method Description	SKBR3 8000 cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. For cell viability curves, serially diluted conjugates or naked payloads were added to the cells at final concentrations ranging from 100 nM to 5 pM and incubated for 3 days. To measure viability, cells were incubated with CCK8 (Dojindo) for the final 2 hours and the absorbance at 450 nm (OD450) was determined on a Victor (Perkin Elmer).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	NCI-H1975 8000 cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. For cell viability curves, serially diluted conjugates or naked payloads were added to the cells at final concentrations ranging from 100 nM to 5 pM and incubated for 3 days. To measure viability, cells were incubated with CCK8 (Dojindo) for the final 2 hours and the absorbance at 450 nm (OD450) was determined on a Victor (Perkin Elmer).    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511

Experiment 1 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.017 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma, Multiple myeloma	KMS-27 cells		CVCL_2993
Experiment 2 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.018 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600
Experiment 3 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.021 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Multiple myeloma	KMS-21 cells		CVCL_2991
Experiment 4 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.043 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma, Multiple myeloma	KMS-20 cells		CVCL_2990

Experiment 1 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.018 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 2 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.028 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.034 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.124 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 5 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.564 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Breast acantholytic squamous cell carcinoma	HCC-1806 cells		CVCL_1258
Experiment 6 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236

Experiment 1 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.019 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 2 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.024 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 3 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.042 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.044 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 5 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.188 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Breast acantholytic squamous cell carcinoma	HCC-1806 cells		CVCL_1258
Experiment 6 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236

Experiment 1 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 nM	High ITGA2 expression (ITGA2 +++)
Method Description	Human bile duct cancer cells HuCC-T1 available from Zhejiang MeisenCTCC, human epidermal cancer cells A431 available from Procell Life Science&Technology Co.,Ltd. (Wuhan) and Chinese hamster ovary cells CHO from negative control ATCC were seeded into a 96-well plate at 2500 cells/well. It was then incubated in a 5% C02 incubator overnight at 37°C. Half of the medium was removed from the cell plate on the next day. A 2x hIgG (negative control antibody, provided by Biointron), Vatelizumab, FS002-Al-vc-MMAE, FS002-A15-vc-MMAE, FS002-A36-vc-MMAE, Vatelizumab-vc-MMAE, hIgG1-vcMMAE (negative control ADC, provided by ChemPartner) was prepared with a complete culture medium, and then diluted at a 3-fold gradient with 11 specific concentration points in total. Serial dilutions of the above molecules were added to the appropriate wells, and it was then incubated in a 5% C02 incubator for 5 days at 37°C. After the incubation, 100 uL of Cell-Titer-Glo 2.0 reagent was added to the 96-well plate. It was then well mixed on a plate shaker for 2 minutes, and finally equilibrated at room temperature for 10 minutes. Readings were taken using a microplate reader. Finally, IC50 was used to compare the biological activity of the ADC against each cell line.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.08 nM	High ITGA2 expression (ITGA2 +++)
Method Description	Human bile duct cancer cells HuCC-T1 available from Zhejiang MeisenCTCC, human epidermal cancer cells A431 available from Procell Life Science&Technology Co.,Ltd. (Wuhan) and Chinese hamster ovary cells CHO from negative control ATCC were seeded into a 96-well plate at 2500 cells/well. It was then incubated in a 5% C02 incubator overnight at 37°C. Half of the medium was removed from the cell plate on the next day. A 2x hIgG (negative control antibody, provided by Biointron), Vatelizumab, FS002-Al-vc-MMAE, FS002-A15-vc-MMAE, FS002-A36-vc-MMAE, Vatelizumab-vc-MMAE, hIgG1-vcMMAE (negative control ADC, provided by ChemPartner) was prepared with a complete culture medium, and then diluted at a 3-fold gradient with 11 specific concentration points in total. Serial dilutions of the above molecules were added to the appropriate wells, and it was then incubated in a 5% C02 incubator for 5 days at 37°C. After the incubation, 100 uL of Cell-Titer-Glo 2.0 reagent was added to the 96-well plate. It was then well mixed on a plate shaker for 2 minutes, and finally equilibrated at room temperature for 10 minutes. Readings were taken using a microplate reader. Finally, IC50 was used to compare the biological activity of the ADC against each cell line.    Click to Show/Hide
In Vitro Model	Intrahepatic cholangiocarcinoma, Cholangiocarcinoma	HuCC-T1 cells		CVCL_0324

Experiment 1 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0201 nM	Positive HER2 expression (HER2+++/++)
Method Description	HCC 1954, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0513 nM	Positive HER2 expression (HER2+++/++)
Method Description	NCI-N87, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0937 nM	Positive HER2 expression (HER2+++/++)
Method Description	BT-474, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.2151 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-OV-3, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1.457 nM	Negative HER2 expression (HER2-)
Method Description	MCF-7, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1.457 nM	Negative HER2 expression (HER2-)
Method Description	MDA-MB-468, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.021 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Multiple myeloma	KMS-21 cells		CVCL_2991
Experiment 2 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.021 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600
Experiment 3 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.022 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma, Multiple myeloma	KMS-27 cells		CVCL_2993
Experiment 4 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma, Multiple myeloma	KMS-20 cells		CVCL_2990

Experiment 1 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0229 nM	Positive HER2 expression (HER2+++/++)
Method Description	HCC 1954, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0498 nM	Positive HER2 expression (HER2+++/++)
Method Description	NCI-N87, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	BT-474, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.2181 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-OV-3, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1.6314 nM	Negative HER2 expression (HER2-)
Method Description	MCF-7, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1.6314 nM	Negative HER2 expression (HER2-)
Method Description	MDA-MB-468, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0231 nM	Positive HER2 expression (HER2+++/++)
Method Description	HCC 1954, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0563 nM	Positive HER2 expression (HER2+++/++)
Method Description	NCI-N87, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0783 nM	Positive HER2 expression (HER2+++/++)
Method Description	BT-474, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1518 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-OV-3, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1.6495 nM	Negative HER2 expression (HER2-)
Method Description	MCF-7, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1.6495 nM	Negative HER2 expression (HER2-)
Method Description	MDA-MB-468, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0232 nM	Positive HER2 expression (HER2+++/++)
Method Description	HCC 1954, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0587 nM	Positive HER2 expression (HER2+++/++)
Method Description	NCI-N87, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1038 nM	Positive HER2 expression (HER2+++/++)
Method Description	BT-474, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.2372 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-OV-3, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1.6814 nM	Negative HER2 expression (HER2-)
Method Description	MCF-7, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1.6814 nM	Negative HER2 expression (HER2-)
Method Description	MDA-MB-468, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0242 nM	Positive HER2 expression (HER2+++/++)
Method Description	HCC 1954, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0523 nM	Positive HER2 expression (HER2+++/++)
Method Description	NCI-N87, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0777 nM	Positive HER2 expression (HER2+++/++)
Method Description	BT-474, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1627 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-OV-3, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1.659 nM	Negative HER2 expression (HER2-)
Method Description	MCF-7, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1.659 nM	Negative HER2 expression (HER2-)
Method Description	MDA-MB-468, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0258 nM	Positive HER2 expression (HER2+++/++)
Method Description	HCC 1954, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.0536 nM	Positive HER2 expression (HER2+++/++)
Method Description	NCI-N87, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1026 nM	Positive HER2 expression (HER2+++/++)
Method Description	BT-474, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.2074 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-OV-3, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 5 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1.5316 nM	Negative HER2 expression (HER2-)
Method Description	MCF-7, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 6 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1.5316 nM	Negative HER2 expression (HER2-)
Method Description	MDA-MB-468, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.026 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Multiple myeloma	KMS-21 cells		CVCL_2991
Experiment 2 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.027 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma	NCI-H929 cells		CVCL_1600
Experiment 3 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.028 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma, Multiple myeloma	KMS-27 cells		CVCL_2993
Experiment 4 Reporting the Activity Date of This ADC					[114]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.077 nM	High CD48 expression (CD48 +++)
Method Description	TheabilityoftheCD48ADCstoinhibitcellproliferationandsurvivalwasassessedusingthePromegaCelliter-Gloproliferationassay.Celllineswereculturedin mediathatisoptimalfortheirgrowthat5%C02,370Cinatissuecultureincubator.Priortoseedingfortheproliferationassaythecellsweresplitatleast2daysbeforetheassaytoensureoptimalgrowthdensity.Onthedayofseedingcellviabilityandcelldensityweredeterminedusingacellcounter (ViCellXRCellViabilityAnalyzerBeckmanCoulter).Cells withhigherthan85%viabilitywereseededinwhiteclearbottom384-wellTCtreatedplatesb (Corningcat.#3765).CellswereseededatadensityofI,000cellsperwellin45pLof standardgrowthmedia.Plateswereincubatedat5%C0 2 ,370Covernightinatissueculture incubator.ThenextdayCD48targetingMMAEADCsandnon-targetingisotypeADCs werepreparedatlOXinstandardgrowthmedia.ThepreparedCD48targetingandisotype matchednon targetingcontrolADCtreatmentswereaddedtothecellsresultinginfinalconcentrationsof0.001- 25nMandafinalvolumeof50pLperwell.Eachdrug concentrationwastestedinquadruplets.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma, Multiple myeloma	KMS-20 cells		CVCL_2990

Experiment 1 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.035 nM	Positive HER2 expression (HER2+++/++)
Method Description	SKBR3 8000 cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. For cell viability curves, serially diluted conjugates or naked payloads were added to the cells at final concentrations ranging from 100 nM to 5 pM and incubated for 3 days. To measure viability, cells were incubated with CCK8 (Dojindo) for the final 2 hours and the absorbance at 450 nm (OD450) was determined on a Victor (Perkin Elmer).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	NCI-H1975 8000 cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. For cell viability curves, serially diluted conjugates or naked payloads were added to the cells at final concentrations ranging from 100 nM to 5 pM and incubated for 3 days. To measure viability, cells were incubated with CCK8 (Dojindo) for the final 2 hours and the absorbance at 450 nm (OD450) was determined on a Victor (Perkin Elmer).    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511

Experiment 1 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 2 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.062 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.068 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.456 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 5 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.787 nM	High TROP2 expression (TROP2 +++)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Breast acantholytic squamous cell carcinoma	HCC-1806 cells		CVCL_1258
Experiment 6 Reporting the Activity Date of This ADC					[113]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	The Cell Counting Kit-8 (CCK-8) assay was performed to measure the in vitro efficiency of ADCs. TROP2-expression tumor cell lines (BXPC-3, HCI-441, Fadu, HCC1806, NCI-N87) and TROP2 negative tumor cell lines (Calu-6) were cultured in a 10 % 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. All ADCs were diluted 5-fold with RPMI 1640 medium from an initial concentration of 100 nmol/L, a total of nine concentration gradients. The ADC samples were added to three wells with every single concentration and the 96-well plates were cultured at 37 °C in a 5 % CO2 cell incubator for six days. Then CCK8 solution was added and incubated at 37 °C for 4 h. Optical density (OD) value was measured at 450 nm using a BioTek Epoch. IC50 values and the cell viability curve were calculated by GraphPad software.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.05 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.06 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.061 nM	High L1CAM expression (L1CAM +++)
Method Description	HeLa cells are cultured in DMEM complete medium (Corning, 10-013-CVR) containing 10% FBS (Gibco, 10099-141) and 100 U/mL penicillin-streptomycin mixture (Thermofisher, 15140122). When the cell coverage in the culture container reaches 80-90%, TrypLE (Thermofisher, 12604-013) is used to digest the HeLa cells from the culture container, and they are seeded in a 96-well cell culture plate (Greiner, 655098) at a density of 3.3X103 cells/mL, with 500 cells per well (145uL complete medium),and the 96-well plate is incubated at 37°C overnight. The next day, (ADC) is diluted in complete medium in a 4-fold serial dilution, with 9 concentration gradient points. Then, 5uL of dilution of the ADC molecule is added to each well in the 96-well cell culture plate, gently mixed, and the 96-well plate is incubated at 37°C for 6 days. Finally, 75 uL of CTG is added to each well, gently mixed, and the 96-well plate is incubated at room temperature for 10 minutes. Then the luminescence signal is detected using a multimode microplate reader (PerkinElmer Envision 2105). A dose-inhibition curve is generated, and the half-maximal inhibitory concentration (IC50) is calculated using non-linear regression with GraphPad software.    Click to Show/Hide
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030
Experiment 2 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	95 nM	Low L1CAM expression (L1CAM+)
Method Description	HeLa L1CAM-KO cells are cultured in DMEM complete medium (Corning, 10-013-CVR) containing 10% FBS (Gibco, 10099-141) and 100 U/mL penicillin-streptomycin mixture (Thermofisher, 15140122). When the cell coverage in the culture container reaches 80-90%, TrypLE (Thermofisher, 12604-013) is used to digest the HeLa L1CAM-KO cells from the culture container, and they are seeded in a 96-well cell culture plate (Greiner, 655098) at a density of 3.3X103 cells/mL, with 500 cells per well (145uL complete medium),and the 96-well plate is incubated at 37°C overnight. The next day, (ADC) is diluted in complete medium in a 4-fold serial dilution, with 9 concentration gradient points. Then, 5uL of dilution of the ADC molecule is added to each well in the 96-well cell culture plate, gently mixed, and the 96-well plate is incubated at 37°C for 6 days. Finally, 75 uL of CTG is added to each well, gently mixed, and the 96-well plate is incubated at room temperature for 10 minutes. Then the luminescence signal is detected using a multimode microplate reader (PerkinElmer Envision 2105). A dose-inhibition curve is generated, and the half-maximal inhibitory concentration (IC50) is calculated using non-linear regression with GraphPad software.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	HeLa cells (L1CAM KO)		CVCL_0030

Experiment 1 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.064 nM	Positive HER2 expression (HER2+++/++)
Method Description	BT-474, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	30.219 nM	Negative HER2 expression (HER2-)
Method Description	MCF-7, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.069 nM	Positive HER2 expression (HER2+++/++)
Method Description	BT-474, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 0.064 to 0.075 nmol/L. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	98.357 nM	Negative HER2 expression (HER2-)
Method Description	MCF-7, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to A431 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. A431cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[120]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07&#1770.00 nM	High TF expression (TF +++)
Method Description	Pancreatic cancer cell lines HPAF-II, BxPC-3, or PSN-1 were harvested on 96-well plates (Corning) and incubated at 37°C overnight. Payloads and ADCs were applied to each well at various concentrations, and the plates were incubated at 37°C for 6 days (n = 3). Cancer cell viability was measured using CCK-8 (Dojindo).
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[120]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.18&#1770.02 nM	Moderate TF expression (TF++)
Method Description	Pancreatic cancer cell lines HPAF-II, BxPC-3, or PSN-1 were harvested on 96-well plates (Corning) and incubated at 37°C overnight. Payloads and ADCs were applied to each well at various concentrations, and the plates were incubated at 37°C for 6 days (n = 3). Cancer cell viability was measured using CCK-8 (Dojindo).
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[120]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.65&#1770.01 nM	Low TF expression (TF+)
Method Description	Pancreatic cancer cell lines HPAF-II, BxPC-3, or PSN-1 were harvested on 96-well plates (Corning) and incubated at 37°C overnight. Payloads and ADCs were applied to each well at various concentrations, and the plates were incubated at 37°C for 6 days (n = 3). Cancer cell viability was measured using CCK-8 (Dojindo).
In Vitro Model	Pancreatic adenocarcinoma	PSN-1 cells		CVCL_1644

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.07 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[121]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.071 nM	Low HER2 expression (HER2+)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-453 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC					[121]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.091 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the nci-n87 cell.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.075 nM	Positive HER2 expression (HER2+++/++)
Method Description	BT-474, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[117]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	139.901 nM	Negative HER2 expression (HER2-)
Method Description	MCF-7, 1000cell/well was added to the designated 384-well cell culture plate in the appropriate growth media. The ADCs stock solution was diluted in series in a ratio of 1:3 to produce 10 diluted solutions with different concentrations (the compound stock solution was an L-His buffer salt solution with a concentration of about 2 mg/mL, which was diluted with PBS, and the initial maximum concentration at test point was about 500 mg/mL). 4ul of the compound diluted solutions with different concentrations was distributed into a 384-well plate. After 96 hours, the plate was taken from the incubator and equilibrated at room temperature for 10 minutes. 40uL of CellTiter-Glo reagent was added to each well to be tested (the ratio of CellTiter-Glo reagent to medium was 1:1).the plate was then placed at room temperature for 30 minutes, and then reading was carried out on an EnSpire reader for cell counting.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.08 nM	High ITGA2 expression (ITGA2 +++)
Method Description	Human bile duct cancer cells HuCC-T1 available from Zhejiang MeisenCTCC, human epidermal cancer cells A431 available from Procell Life Science&Technology Co.,Ltd. (Wuhan) and Chinese hamster ovary cells CHO from negative control ATCC were seeded into a 96-well plate at 2500 cells/well. It was then incubated in a 5% C02 incubator overnight at 37°C. Half of the medium was removed from the cell plate on the next day. A 2x hIgG (negative control antibody, provided by Biointron), Vatelizumab, FS002-Al-vc-MMAE, FS002-A15-vc-MMAE, FS002-A36-vc-MMAE, Vatelizumab-vc-MMAE, hIgG1-vcMMAE (negative control ADC, provided by ChemPartner) was prepared with a complete culture medium, and then diluted at a 3-fold gradient with 11 specific concentration points in total. Serial dilutions of the above molecules were added to the appropriate wells, and it was then incubated in a 5% C02 incubator for 5 days at 37°C. After the incubation, 100 uL of Cell-Titer-Glo 2.0 reagent was added to the 96-well plate. It was then well mixed on a plate shaker for 2 minutes, and finally equilibrated at room temperature for 10 minutes. Readings were taken using a microplate reader. Finally, IC50 was used to compare the biological activity of the ADC against each cell line.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.89 nM	High ITGA2 expression (ITGA2 +++)
Method Description	Human bile duct cancer cells HuCC-T1 available from Zhejiang MeisenCTCC, human epidermal cancer cells A431 available from Procell Life Science&Technology Co.,Ltd. (Wuhan) and Chinese hamster ovary cells CHO from negative control ATCC were seeded into a 96-well plate at 2500 cells/well. It was then incubated in a 5% C02 incubator overnight at 37°C. Half of the medium was removed from the cell plate on the next day. A 2x hIgG (negative control antibody, provided by Biointron), Vatelizumab, FS002-Al-vc-MMAE, FS002-A15-vc-MMAE, FS002-A36-vc-MMAE, Vatelizumab-vc-MMAE, hIgG1-vcMMAE (negative control ADC, provided by ChemPartner) was prepared with a complete culture medium, and then diluted at a 3-fold gradient with 11 specific concentration points in total. Serial dilutions of the above molecules were added to the appropriate wells, and it was then incubated in a 5% C02 incubator for 5 days at 37°C. After the incubation, 100 uL of Cell-Titer-Glo 2.0 reagent was added to the 96-well plate. It was then well mixed on a plate shaker for 2 minutes, and finally equilibrated at room temperature for 10 minutes. Readings were taken using a microplate reader. Finally, IC50 was used to compare the biological activity of the ADC against each cell line.    Click to Show/Hide
In Vitro Model	Intrahepatic cholangiocarcinoma, Cholangiocarcinoma	HuCC-T1 cells		CVCL_0324

Experiment 1 Reporting the Activity Date of This ADC					[120]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.08&#1770.00 nM	High TF expression (TF +++)
Method Description	Pancreatic cancer cell lines HPAF-II, BxPC-3, or PSN-1 were harvested on 96-well plates (Corning) and incubated at 37°C overnight. Payloads and ADCs were applied to each well at various concentrations, and the plates were incubated at 37°C for 6 days (n = 3). Cancer cell viability was measured using CCK-8 (Dojindo).
In Vitro Model	Pancreatic ductal adenocarcinoma	HPAF-II cells		CVCL_0313
Experiment 2 Reporting the Activity Date of This ADC					[120]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.09&#1770.00 nM	Moderate TF expression (TF++)
Method Description	Pancreatic cancer cell lines HPAF-II, BxPC-3, or PSN-1 were harvested on 96-well plates (Corning) and incubated at 37°C overnight. Payloads and ADCs were applied to each well at various concentrations, and the plates were incubated at 37°C for 6 days (n = 3). Cancer cell viability was measured using CCK-8 (Dojindo).
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 3 Reporting the Activity Date of This ADC					[120]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.12&#1770.18 nM	Low TF expression (TF+)
Method Description	Pancreatic cancer cell lines HPAF-II, BxPC-3, or PSN-1 were harvested on 96-well plates (Corning) and incubated at 37°C overnight. Payloads and ADCs were applied to each well at various concentrations, and the plates were incubated at 37°C for 6 days (n = 3). Cancer cell viability was measured using CCK-8 (Dojindo).
In Vitro Model	Pancreatic adenocarcinoma	PSN-1 cells		CVCL_1644

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.08 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[122]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.085 nM	Positive TROP2 expression (TROP2+++/++)
Method Description	Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[122]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.182 nM	Positive TROP2 expression (TROP2+++/++)
Method Description	Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.    Click to Show/Hide
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 3 Reporting the Activity Date of This ADC					[122]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.265 nM	Positive TROP2 expression (TROP2+++/++)
Method Description	Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[122]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.418 nM	Positive TROP2 expression (TROP2+++/++)
Method Description	Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 5 Reporting the Activity Date of This ADC					[122]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.945 nM	Positive TROP2 expression (TROP2+++/++)
Method Description	Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.    Click to Show/Hide
In Vitro Model	Breast acantholytic squamous cell carcinoma	HCC-1806 cells		CVCL_1258
Experiment 6 Reporting the Activity Date of This ADC					[122]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[121]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.091 nM	Low HER2 expression (HER2+)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-453 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-453 cells		CVCL_0418
Experiment 2 Reporting the Activity Date of This ADC					[121]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.331 nM	High HER2 expression (HER2+++; >300,000 HER2 molecules/cell)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the nci-n87 cell.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.092 nM	High L1CAM expression (L1CAM +++)
Method Description	HeLa cells are cultured in DMEM complete medium (Corning, 10-013-CVR) containing 10% FBS (Gibco, 10099-141) and 100 U/mL penicillin-streptomycin mixture (Thermofisher, 15140122). When the cell coverage in the culture container reaches 80-90%, TrypLE (Thermofisher, 12604-013) is used to digest the HeLa cells from the culture container, and they are seeded in a 96-well cell culture plate (Greiner, 655098) at a density of 3.3X103 cells/mL, with 500 cells per well (145uL complete medium),and the 96-well plate is incubated at 37°C overnight. The next day, (ADC) is diluted in complete medium in a 4-fold serial dilution, with 9 concentration gradient points. Then, 5uL of dilution of the ADC molecule is added to each well in the 96-well cell culture plate, gently mixed, and the 96-well plate is incubated at 37°C for 6 days. Finally, 75 uL of CTG is added to each well, gently mixed, and the 96-well plate is incubated at room temperature for 10 minutes. Then the luminescence signal is detected using a multimode microplate reader (PerkinElmer Envision 2105). A dose-inhibition curve is generated, and the half-maximal inhibitory concentration (IC50) is calculated using non-linear regression with GraphPad software.    Click to Show/Hide
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030
Experiment 2 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	90 nM	Low L1CAM expression (L1CAM+)
Method Description	HeLa L1CAM-KO cells are cultured in DMEM complete medium (Corning, 10-013-CVR) containing 10% FBS (Gibco, 10099-141) and 100 U/mL penicillin-streptomycin mixture (Thermofisher, 15140122). When the cell coverage in the culture container reaches 80-90%, TrypLE (Thermofisher, 12604-013) is used to digest the HeLa L1CAM-KO cells from the culture container, and they are seeded in a 96-well cell culture plate (Greiner, 655098) at a density of 3.3X103 cells/mL, with 500 cells per well (145uL complete medium),and the 96-well plate is incubated at 37°C overnight. The next day, (ADC) is diluted in complete medium in a 4-fold serial dilution, with 9 concentration gradient points. Then, 5uL of dilution of the ADC molecule is added to each well in the 96-well cell culture plate, gently mixed, and the 96-well plate is incubated at 37°C for 6 days. Finally, 75 uL of CTG is added to each well, gently mixed, and the 96-well plate is incubated at room temperature for 10 minutes. Then the luminescence signal is detected using a multimode microplate reader (PerkinElmer Envision 2105). A dose-inhibition curve is generated, and the half-maximal inhibitory concentration (IC50) is calculated using non-linear regression with GraphPad software.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	HeLa cells (L1CAM KO)		CVCL_0030

Experiment 1 Reporting the Activity Date of This ADC					[123]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.093&#1770.009 nM	Positive MSLN expression (MSLN+++/++)
Method Description	Oval-Citar-3-MSLN cells with good growth state were added to 96-well cell culture plates (5×104 cells /mL, 100uL/ well) and incubated overnight in a CO2 incubator at 37°C.
In Vitro Model	High grade ovarian serous adenocarcinoma	Oval-Citar-3-MSLN cells		CVCL_0465

Experiment 1 Reporting the Activity Date of This ADC					[124]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.1 nM	Positive HER2 expression (HER2+++/++)
Method Description	According to Vichai et al., (31) experiments were performed in 96-well plates (flat bottom, transparent plate, with lid; Corning-Falcon cat. n° 353072) using a CLARIOstar Plus plate-reader device (BMG LABTECH). Cells were seeded in a 96-well plate at a density of 2 × 103 cells in 100 uL per well, keeping a column of the plate without cells (background control), and allowed to recover for 24 h. Cells were treated live with 100 uL of various concentrations (final concentrations ranging from 0.003 to 100 nM) of trastuzumab conjugates (diluted in supplemented RPMI for HCC1954 and MDA-MB-231 cell lines and in DMEM for MCF7 cell line) or not (negative control = untreated cells; only supplemented with 100 uL of RPMI for HCC1954 and MDA-MB-231 cell lines or with 100 uL of DMEM for MCF7 cell line) in technical triplicates. Cells were incubated for 96 h at 37 °C and 5% CO2 under a humid atmosphere in an IncuCyteS3 (from Sartorius). Cells were fixed with an addition of 100 uL of cold 10% (w/v) trichloroacetic acid (TCA) to wells for 1 h at 4 °C, washed with tap water (×3), allowed to dry overnight at 25 °C, stained with 0.057% (w/v) SRB (in 1% (v/v) acetic acid) for 30 min at 25 °C, then quickly washed with 1% (v/v) acetic acid (×3) and allowed to dry overnight at 25 °C. After incubating the plate with 100 uL of cold 10 mM unbuffered Trizma base solution for 5 min at 25 °C under agitation, the Abs 530 nm was recorded. Final data were analyzed with Excel (Microsoft Corp.) and GraphPad Prism version 10.1.2 for Windows (GraphPad Software, Boston, Massachusetts USA). Mean Abs values and Normalized % cell viability (see below) were calculated. IC50 was calculated in performing a sigmoidal fit ([inhibitor] vs response-variable slope, GraphPad Prism v10.0.0). A minimum of three independent experiments (n = 3) was used. Normalized % cell viability [x] = [ (Mean Abs 530 nm conjugates [x] - Mean Abs 530 nm background control)/ (Mean Abs 530 nm negative control - Mean Abs 530 nm background control)] × 100; with [x] corresponding to the final conjugate's concentration.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[124]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	According to Vichai et al., (31) experiments were performed in 96-well plates (flat bottom, transparent plate, with lid; Corning-Falcon cat. n° 353072) using a CLARIOstar Plus plate-reader device (BMG LABTECH). Cells were seeded in a 96-well plate at a density of 2 × 103 cells in 100 uL per well, keeping a column of the plate without cells (background control), and allowed to recover for 24 h. Cells were treated live with 100 uL of various concentrations (final concentrations ranging from 0.003 to 100 nM) of trastuzumab conjugates (diluted in supplemented RPMI for HCC1954 and MDA-MB-231 cell lines and in DMEM for MCF7 cell line) or not (negative control = untreated cells; only supplemented with 100 uL of RPMI for HCC1954 and MDA-MB-231 cell lines or with 100 uL of DMEM for MCF7 cell line) in technical triplicates. Cells were incubated for 96 h at 37 °C and 5% CO2 under a humid atmosphere in an IncuCyteS3 (from Sartorius). Cells were fixed with an addition of 100 uL of cold 10% (w/v) trichloroacetic acid (TCA) to wells for 1 h at 4 °C, washed with tap water (×3), allowed to dry overnight at 25 °C, stained with 0.057% (w/v) SRB (in 1% (v/v) acetic acid) for 30 min at 25 °C, then quickly washed with 1% (v/v) acetic acid (×3) and allowed to dry overnight at 25 °C. After incubating the plate with 100 uL of cold 10 mM unbuffered Trizma base solution for 5 min at 25 °C under agitation, the Abs 530 nm was recorded. Final data were analyzed with Excel (Microsoft Corp.) and GraphPad Prism version 10.1.2 for Windows (GraphPad Software, Boston, Massachusetts USA). Mean Abs values and Normalized % cell viability (see below) were calculated. IC50 was calculated in performing a sigmoidal fit ([inhibitor] vs response-variable slope, GraphPad Prism v10.0.0). A minimum of three independent experiments (n = 3) was used. Normalized % cell viability [x] = [ (Mean Abs 530 nm conjugates [x] - Mean Abs 530 nm background control)/ (Mean Abs 530 nm negative control - Mean Abs 530 nm background control)] × 100; with [x] corresponding to the final conjugate's concentration.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[124]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	According to Vichai et al., (31) experiments were performed in 96-well plates (flat bottom, transparent plate, with lid; Corning-Falcon cat. n° 353072) using a CLARIOstar Plus plate-reader device (BMG LABTECH). Cells were seeded in a 96-well plate at a density of 2 × 103 cells in 100 uL per well, keeping a column of the plate without cells (background control), and allowed to recover for 24 h. Cells were treated live with 100 uL of various concentrations (final concentrations ranging from 0.003 to 100 nM) of trastuzumab conjugates (diluted in supplemented RPMI for HCC1954 and MDA-MB-231 cell lines and in DMEM for MCF7 cell line) or not (negative control = untreated cells; only supplemented with 100 uL of RPMI for HCC1954 and MDA-MB-231 cell lines or with 100 uL of DMEM for MCF7 cell line) in technical triplicates. Cells were incubated for 96 h at 37 °C and 5% CO2 under a humid atmosphere in an IncuCyteS3 (from Sartorius). Cells were fixed with an addition of 100 uL of cold 10% (w/v) trichloroacetic acid (TCA) to wells for 1 h at 4 °C, washed with tap water (×3), allowed to dry overnight at 25 °C, stained with 0.057% (w/v) SRB (in 1% (v/v) acetic acid) for 30 min at 25 °C, then quickly washed with 1% (v/v) acetic acid (×3) and allowed to dry overnight at 25 °C. After incubating the plate with 100 uL of cold 10 mM unbuffered Trizma base solution for 5 min at 25 °C under agitation, the Abs 530 nm was recorded. Final data were analyzed with Excel (Microsoft Corp.) and GraphPad Prism version 10.1.2 for Windows (GraphPad Software, Boston, Massachusetts USA). Mean Abs values and Normalized % cell viability (see below) were calculated. IC50 was calculated in performing a sigmoidal fit ([inhibitor] vs response-variable slope, GraphPad Prism v10.0.0). A minimum of three independent experiments (n = 3) was used. Normalized % cell viability [x] = [ (Mean Abs 530 nm conjugates [x] - Mean Abs 530 nm background control)/ (Mean Abs 530 nm negative control - Mean Abs 530 nm background control)] × 100; with [x] corresponding to the final conjugate's concentration.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[100]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.11 nM	Positive TF expression (TF+++/++)
Method Description	The TF-specific ADCs were added to A431 cells, with either a 72 h incubation or a 4 h incubation followed by removal of excess ADC and culture for another 68 h. A440cells were lysed in CTG assay reagent after treatment.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.12 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[126]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.125 nM
Method Description	IC50 Values (nM) of anti-TRBC1-MMAE in T-cell cancer cell lines in CML-T1 TRBC1
In Vitro Model	Chronic myelogenous leukemia, BCR-ABL1 positive, Chronic myeloid leukemia	CML-T1 TRBC1 cells		CVCL_1126
Experiment 2 Reporting the Activity Date of This ADC					[126]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.141 nM
Method Description	IC50 Values (nM) of anti-TRBC1-MMAE in T-cell cancer cell lines in Jurkat TRBC2
In Vitro Model	Childhood T acute lymphoblastic leukemia, Precursor T-cell acute lymphoblastic leukemia	Jurkat TRBC2 cells		CVCL_0065
Experiment 3 Reporting the Activity Date of This ADC					[126]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.144 nM
Method Description	IC50 Values (nM) of anti-TRBC1-MMAE in T-cell cancer cell lines in Jurkat TCR-KO
In Vitro Model	Childhood T acute lymphoblastic leukemia, Precursor T-cell acute lymphoblastic leukemia	Jurkat TCR-KO cells		CVCL_0065
Experiment 4 Reporting the Activity Date of This ADC					[126]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.145 nM
Method Description	IC50 Values (nM) of anti-TRBC1-MMAE in T-cell cancer cell lines in Jurkat TRBC1
In Vitro Model	Childhood T acute lymphoblastic leukemia, Precursor T-cell acute lymphoblastic leukemia	Jurkat TRBC1 cells		CVCL_0065
Experiment 5 Reporting the Activity Date of This ADC					[126]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.155 nM
Method Description	IC50 Values (nM) of anti-TRBC1-MMAE in T-cell cancer cell lines in HPB-ALL TRBC2
In Vitro Model	Childhood T acute lymphoblastic leukemia, Precursor T-cell acute lymphoblastic leukemia	HPB-ALL TRBC2 cells		CVCL_1820
Experiment 6 Reporting the Activity Date of This ADC					[126]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.156 nM
Method Description	IC50 Values (nM) of anti-TRBC1-MMAE in T-cell cancer cell lines in HPB-ALL TRBC1
In Vitro Model	Childhood T acute lymphoblastic leukemia, Precursor T-cell acute lymphoblastic leukemia	HPB-ALL TRBC1 cells		CVCL_1820
Experiment 7 Reporting the Activity Date of This ADC					[126]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.248 nM
Method Description	IC50 Values (nM) of anti-TRBC1-MMAE in T-cell cancer cell lines in SUP-T1 TRBC1
In Vitro Model	Childhood T lymphoblastic lymphoma, T-cell non-Hodgkin lymphoma	SUP-T1 TRBC1 cells		CVCL_1714
Experiment 8 Reporting the Activity Date of This ADC					[126]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.611 nM
Method Description	IC50 Values (nM) of anti-TRBC1-MMAE in T-cell cancer cell lines in H9 TRBC1
In Vitro Model	Sezary syndrome	H9 TRBC1 cells		CVCL_1240

Experiment 1 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.14 nM	High ITGA2 expression (ITGA2 +++)
Method Description	Human bile duct cancer cells HuCC-T1 available from Zhejiang MeisenCTCC, human epidermal cancer cells A431 available from Procell Life Science&Technology Co.,Ltd. (Wuhan) and Chinese hamster ovary cells CHO from negative control ATCC were seeded into a 96-well plate at 2500 cells/well. It was then incubated in a 5% C02 incubator overnight at 37°C. Half of the medium was removed from the cell plate on the next day. A 2x hIgG (negative control antibody, provided by Biointron), Vatelizumab, FS002-Al-vc-MMAE, FS002-A15-vc-MMAE, FS002-A36-vc-MMAE, Vatelizumab-vc-MMAE, hIgG1-vcMMAE (negative control ADC, provided by ChemPartner) was prepared with a complete culture medium, and then diluted at a 3-fold gradient with 11 specific concentration points in total. Serial dilutions of the above molecules were added to the appropriate wells, and it was then incubated in a 5% C02 incubator for 5 days at 37°C. After the incubation, 100 uL of Cell-Titer-Glo 2.0 reagent was added to the 96-well plate. It was then well mixed on a plate shaker for 2 minutes, and finally equilibrated at room temperature for 10 minutes. Readings were taken using a microplate reader. Finally, IC50 was used to compare the biological activity of the ADC against each cell line.    Click to Show/Hide
In Vitro Model	Intrahepatic cholangiocarcinoma, Cholangiocarcinoma	HuCC-T1 cells		CVCL_0324
Experiment 2 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.14 nM	High ITGA2 expression (ITGA2 +++)
Method Description	Human bile duct cancer cells HuCC-T1 available from Zhejiang MeisenCTCC, human epidermal cancer cells A431 available from Procell Life Science&Technology Co.,Ltd. (Wuhan) and Chinese hamster ovary cells CHO from negative control ATCC were seeded into a 96-well plate at 2500 cells/well. It was then incubated in a 5% C02 incubator overnight at 37°C. Half of the medium was removed from the cell plate on the next day. A 2x hIgG (negative control antibody, provided by Biointron), Vatelizumab, FS002-Al-vc-MMAE, FS002-A15-vc-MMAE, FS002-A36-vc-MMAE, Vatelizumab-vc-MMAE, hIgG1-vcMMAE (negative control ADC, provided by ChemPartner) was prepared with a complete culture medium, and then diluted at a 3-fold gradient with 11 specific concentration points in total. Serial dilutions of the above molecules were added to the appropriate wells, and it was then incubated in a 5% C02 incubator for 5 days at 37°C. After the incubation, 100 uL of Cell-Titer-Glo 2.0 reagent was added to the 96-well plate. It was then well mixed on a plate shaker for 2 minutes, and finally equilibrated at room temperature for 10 minutes. Readings were taken using a microplate reader. Finally, IC50 was used to compare the biological activity of the ADC against each cell line.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[122]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.144 nM	Positive TROP2 expression (TROP2+++/++)
Method Description	Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[122]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.224 nM	Positive TROP2 expression (TROP2+++/++)
Method Description	Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.    Click to Show/Hide
In Vitro Model	Lung papillary adenocarcinoma	NCI-H441 cells		CVCL_1561
Experiment 3 Reporting the Activity Date of This ADC					[122]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.338 nM	Positive TROP2 expression (TROP2+++/++)
Method Description	Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 4 Reporting the Activity Date of This ADC					[122]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.683 nM	Positive TROP2 expression (TROP2+++/++)
Method Description	Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 5 Reporting the Activity Date of This ADC					[122]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.027 nM	Positive TROP2 expression (TROP2+++/++)
Method Description	Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.    Click to Show/Hide
In Vitro Model	Breast acantholytic squamous cell carcinoma	HCC-1806 cells		CVCL_1258
Experiment 6 Reporting the Activity Date of This ADC					[122]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	Trop2 positive tumor cells FaDu, NCI-N87, BxPC-3, NCI-H441, HCC-1806, and Trop2 negative cell Calu-6 were inoculated into 96-well plates at a quantity of 5000 cells/well in 90 uL of media and incubated overnight at 37 °C in a 5% CO2 cell incubator. Each sample was diluted fivefold with PBS from an initial concentration of 1 mM, total of 9 concentration gradients were tested. 10 uL of each concentration was added into 3 repeat wells, and the 96-well plates were cultured in a cell incubator with 5% CO2 at 37 °C for 144 h. Original culture medium was discarded, 100 uL of CCK-8 solution was added and incubated at 37 °C for 2-4 h, and measured optical density (OD) values at 450 nm. The IC50 values and the cell viability curve were calculated by GraphPad Prism software.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	Calu-6 cells		CVCL_0236

Experiment 1 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.155 nM	High L1CAM expression (L1CAM +++)
Method Description	HeLa cells are cultured in DMEM complete medium (Corning, 10-013-CVR) containing 10% FBS (Gibco, 10099-141) and 100 U/mL penicillin-streptomycin mixture (Thermofisher, 15140122). When the cell coverage in the culture container reaches 80-90%, TrypLE (Thermofisher, 12604-013) is used to digest the HeLa cells from the culture container, and they are seeded in a 96-well cell culture plate (Greiner, 655098) at a density of 3.3X103 cells/mL, with 500 cells per well (145uL complete medium),and the 96-well plate is incubated at 37°C overnight. The next day, (ADC) is diluted in complete medium in a 4-fold serial dilution, with 9 concentration gradient points. Then, 5uL of dilution of the ADC molecule is added to each well in the 96-well cell culture plate, gently mixed, and the 96-well plate is incubated at 37°C for 6 days. Finally, 75 uL of CTG is added to each well, gently mixed, and the 96-well plate is incubated at room temperature for 10 minutes. Then the luminescence signal is detected using a multimode microplate reader (PerkinElmer Envision 2105). A dose-inhibition curve is generated, and the half-maximal inhibitory concentration (IC50) is calculated using non-linear regression with GraphPad software.    Click to Show/Hide
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030
Experiment 2 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	100 nM	Low L1CAM expression (L1CAM+)
Method Description	HeLa L1CAM-KO cells are cultured in DMEM complete medium (Corning, 10-013-CVR) containing 10% FBS (Gibco, 10099-141) and 100 U/mL penicillin-streptomycin mixture (Thermofisher, 15140122). When the cell coverage in the culture container reaches 80-90%, TrypLE (Thermofisher, 12604-013) is used to digest the HeLa L1CAM-KO cells from the culture container, and they are seeded in a 96-well cell culture plate (Greiner, 655098) at a density of 3.3X103 cells/mL, with 500 cells per well (145uL complete medium),and the 96-well plate is incubated at 37°C overnight. The next day, (ADC) is diluted in complete medium in a 4-fold serial dilution, with 9 concentration gradient points. Then, 5uL of dilution of the ADC molecule is added to each well in the 96-well cell culture plate, gently mixed, and the 96-well plate is incubated at 37°C for 6 days. Finally, 75 uL of CTG is added to each well, gently mixed, and the 96-well plate is incubated at room temperature for 10 minutes. Then the luminescence signal is detected using a multimode microplate reader (PerkinElmer Envision 2105). A dose-inhibition curve is generated, and the half-maximal inhibitory concentration (IC50) is calculated using non-linear regression with GraphPad software.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	HeLa cells (L1CAM KO)		CVCL_0030

Experiment 1 Reporting the Activity Date of This ADC					[127]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.16 nM	Positive GPC3 expression (GPC3+++/++)
Method Description	HuH7 2500cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added with a 3-fold dilution across 11 points, for the various ADCs. Cell proliferation was measured after 5 days exposure, 100ul Cell titer glo 2.0 to test IC50.
In Vitro Model	Adult hepatocellular carcinoma	HuH7 cells		CVCL_0336
Experiment 2 Reporting the Activity Date of This ADC					[127]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.61 nM	Positive GPC3 expression (GPC3+++/++)
Method Description	HepG2 2500cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added with a 3-fold dilution across 11 points, for the various ADCs. Cell proliferation was measured after 5 days exposure, 100ul Cell titer glo 2.0 to test IC50.
In Vitro Model	Hepatoblastoma	HepG2 cells		CVCL_0027
Experiment 3 Reporting the Activity Date of This ADC					[127]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 207 nM	Negative GPC3expression (GPC3-)
Method Description	CHO 2500cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added with a 3-fold dilution across 11 points, for the various ADCs. Cell proliferation was measured after 5 days exposure, 100ul Cell titer glo 2.0 to test IC50.
In Vitro Model	Normal	CHO cells		CVCL_0213

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.16 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.16 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[127]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.17 nM	Positive GPC3 expression (GPC3+++/++)
Method Description	HuH7 2500cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added with a 3-fold dilution across 11 points, for the various ADCs. Cell proliferation was measured after 5 days exposure, 100ul Cell titer glo 2.0 to test IC50.
In Vitro Model	Adult hepatocellular carcinoma	HuH7 cells		CVCL_0336
Experiment 2 Reporting the Activity Date of This ADC					[127]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.1 nM	Positive GPC3 expression (GPC3+++/++)
Method Description	HepG2 2500cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added with a 3-fold dilution across 11 points, for the various ADCs. Cell proliferation was measured after 5 days exposure, 100ul Cell titer glo 2.0 to test IC50.
In Vitro Model	Hepatoblastoma	HepG2 cells		CVCL_0027
Experiment 3 Reporting the Activity Date of This ADC					[127]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 207 nM	Negative GPC3expression (GPC3-)
Method Description	CHO 2500cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added with a 3-fold dilution across 11 points, for the various ADCs. Cell proliferation was measured after 5 days exposure, 100ul Cell titer glo 2.0 to test IC50.
In Vitro Model	Normal	CHO cells		CVCL_0213

Experiment 1 Reporting the Activity Date of This ADC					[127]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.17 nM	Positive GPC3 expression (GPC3+++/++)
Method Description	HuH7 2500cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added with a 3-fold dilution across 11 points, for the various ADCs. Cell proliferation was measured after 5 days exposure, 100ul Cell titer glo 2.0 to test IC50.
In Vitro Model	Adult hepatocellular carcinoma	HuH7 cells		CVCL_0336
Experiment 2 Reporting the Activity Date of This ADC					[127]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.63 nM	Positive GPC3 expression (GPC3+++/++)
Method Description	HepG2 2500cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added with a 3-fold dilution across 11 points, for the various ADCs. Cell proliferation was measured after 5 days exposure, 100ul Cell titer glo 2.0 to test IC50.
In Vitro Model	Hepatoblastoma	HepG2 cells		CVCL_0027
Experiment 3 Reporting the Activity Date of This ADC					[127]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 207 nM	Negative GPC3expression (GPC3-)
Method Description	CHO 2500cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added with a 3-fold dilution across 11 points, for the various ADCs. Cell proliferation was measured after 5 days exposure, 100ul Cell titer glo 2.0 to test IC50.
In Vitro Model	Normal	CHO cells		CVCL_0213

Experiment 1 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.2 nM	High ITGA2 expression (ITGA2 +++)
Method Description	Human bile duct cancer cells HuCC-T1 available from Zhejiang MeisenCTCC, human epidermal cancer cells A431 available from Procell Life Science&Technology Co.,Ltd. (Wuhan) and Chinese hamster ovary cells CHO from negative control ATCC were seeded into a 96-well plate at 2500 cells/well. It was then incubated in a 5% C02 incubator overnight at 37°C. Half of the medium was removed from the cell plate on the next day. A 2x hIgG (negative control antibody, provided by Biointron), Vatelizumab, FS002-Al-vc-MMAE, FS002-A15-vc-MMAE, FS002-A36-vc-MMAE, Vatelizumab-vc-MMAE, hIgG1-vcMMAE (negative control ADC, provided by ChemPartner) was prepared with a complete culture medium, and then diluted at a 3-fold gradient with 11 specific concentration points in total. Serial dilutions of the above molecules were added to the appropriate wells, and it was then incubated in a 5% C02 incubator for 5 days at 37°C. After the incubation, 100 uL of Cell-Titer-Glo 2.0 reagent was added to the 96-well plate. It was then well mixed on a plate shaker for 2 minutes, and finally equilibrated at room temperature for 10 minutes. Readings were taken using a microplate reader. Finally, IC50 was used to compare the biological activity of the ADC against each cell line.    Click to Show/Hide
In Vitro Model	Intrahepatic cholangiocarcinoma, Cholangiocarcinoma	HuCC-T1 cells		CVCL_0324
Experiment 2 Reporting the Activity Date of This ADC					[116]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.2 nM	High ITGA2 expression (ITGA2 +++)
Method Description	Human bile duct cancer cells HuCC-T1 available from Zhejiang MeisenCTCC, human epidermal cancer cells A431 available from Procell Life Science&Technology Co.,Ltd. (Wuhan) and Chinese hamster ovary cells CHO from negative control ATCC were seeded into a 96-well plate at 2500 cells/well. It was then incubated in a 5% C02 incubator overnight at 37°C. Half of the medium was removed from the cell plate on the next day. A 2x hIgG (negative control antibody, provided by Biointron), Vatelizumab, FS002-Al-vc-MMAE, FS002-A15-vc-MMAE, FS002-A36-vc-MMAE, Vatelizumab-vc-MMAE, hIgG1-vcMMAE (negative control ADC, provided by ChemPartner) was prepared with a complete culture medium, and then diluted at a 3-fold gradient with 11 specific concentration points in total. Serial dilutions of the above molecules were added to the appropriate wells, and it was then incubated in a 5% C02 incubator for 5 days at 37°C. After the incubation, 100 uL of Cell-Titer-Glo 2.0 reagent was added to the 96-well plate. It was then well mixed on a plate shaker for 2 minutes, and finally equilibrated at room temperature for 10 minutes. Readings were taken using a microplate reader. Finally, IC50 was used to compare the biological activity of the ADC against each cell line.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[128]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.2 nM	High HER2 expression (HER2 +++)
Method Description	The MTT (3- (4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assays were performed using WT ADC and positively charged ADC in three cell lines with varying HER2 expression levels: N87 (high), MCF-7 (low), and MDA-MB-468 (non-expressing). Cells were seeded at a density of 10,000 cells per well in 96-well plates and incubated for 24 h before treatment. ADCs were added at concentrations ranging from 0.01 nM to 1000 nM, and cells were incubated for an additional 96 h. Following treatment, 5 mg/mL MTT solution was added to each well and incubated for 4 h, after which 10% SDS-HCl solution was added to dissolve the formazan crystals. Absorbance was measured at 570 nm the next day. Cell viability (%) was calculated as (ODtreated/ (ODcontrol) × 100%. GraphPad Prism (version 10.4.1) was used for curve fitting of the sigmoidal dose-response curves (cell viability vs. ADC concentration) under the nonlinear regression option, and the half-maximal inhibitory concentration (IC50) values were determined.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[128]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	296 nM	Negative HER2 expression (HER2-)
Method Description	The MTT (3- (4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assays were performed using WT ADC and positively charged ADC in three cell lines with varying HER2 expression levels: N87 (high), MCF-7 (low), and MDA-MB-468 (non-expressing). Cells were seeded at a density of 10,000 cells per well in 96-well plates and incubated for 24 h before treatment. ADCs were added at concentrations ranging from 0.01 nM to 1000 nM, and cells were incubated for an additional 96 h. Following treatment, 5 mg/mL MTT solution was added to each well and incubated for 4 h, after which 10% SDS-HCl solution was added to dissolve the formazan crystals. Absorbance was measured at 570 nm the next day. Cell viability (%) was calculated as (ODtreated/ (ODcontrol) × 100%. GraphPad Prism (version 10.4.1) was used for curve fitting of the sigmoidal dose-response curves (cell viability vs. ADC concentration) under the nonlinear regression option, and the half-maximal inhibitory concentration (IC50) values were determined.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[128]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1603 nM	Low HER2 expression (HER2+)
Method Description	The MTT (3- (4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assays were performed using WT ADC and positively charged ADC in three cell lines with varying HER2 expression levels: N87 (high), MCF-7 (low), and MDA-MB-468 (non-expressing). Cells were seeded at a density of 10,000 cells per well in 96-well plates and incubated for 24 h before treatment. ADCs were added at concentrations ranging from 0.01 nM to 1000 nM, and cells were incubated for an additional 96 h. Following treatment, 5 mg/mL MTT solution was added to each well and incubated for 4 h, after which 10% SDS-HCl solution was added to dissolve the formazan crystals. Absorbance was measured at 570 nm the next day. Cell viability (%) was calculated as (ODtreated/ (ODcontrol) × 100%. GraphPad Prism (version 10.4.1) was used for curve fitting of the sigmoidal dose-response curves (cell viability vs. ADC concentration) under the nonlinear regression option, and the half-maximal inhibitory concentration (IC50) values were determined.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[129]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.211 nM	Positive HER2 expression (HER2+++/++)
Method Description	Having ADCs with cleavable and non-cleavable linkers in place, we next assessed there in vitro cytotoxicity activities using SSEA4-expressing ovarian SKVO3 cells and breast cancer cells SKBR3 with a negligible expression of SSEA4 and 293T cells as a control. SK-OV3, SKBR3, and 293T cells (2×103 cells/well) were incubated with ADC-1, ADC-2, and chMC-813-70 for 72 h and then treated with MTS at 37 °C. The conversion of the tetrazolium salt MTS (3- (4,5-dimethylthiazol-2-yl)-5- (3-carboxymethoxyphenyl)-2- (4-sulfophenyl)-2H-tetrazolium) to a purple formazan, as a measure of the percentage of viable cells, was measured by absorbance at 490 nm after 4 h. The untreated cells' absorbance was considered 100 % survival (Figure 4).    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[127]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.22 nM	Positive GPC3 expression (GPC3+++/++)
Method Description	HuH7 2500cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added with a 3-fold dilution across 11 points, for the various ADCs. Cell proliferation was measured after 5 days exposure, 100ul Cell titer glo 2.0 to test IC50.
In Vitro Model	Adult hepatocellular carcinoma	HuH7 cells		CVCL_0336
Experiment 2 Reporting the Activity Date of This ADC					[127]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.58 nM	Positive GPC3 expression (GPC3+++/++)
Method Description	HepG2 2500cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added with a 3-fold dilution across 11 points, for the various ADCs. Cell proliferation was measured after 5 days exposure, 100ul Cell titer glo 2.0 to test IC50.
In Vitro Model	Hepatoblastoma	HepG2 cells		CVCL_0027
Experiment 3 Reporting the Activity Date of This ADC					[127]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 207 nM	Negative GPC3expression (GPC3-)
Method Description	CHO 2500cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. 24 hours later, dosing solutions were added with a 3-fold dilution across 11 points, for the various ADCs. Cell proliferation was measured after 5 days exposure, 100ul Cell titer glo 2.0 to test IC50.
In Vitro Model	Normal	CHO cells		CVCL_0213

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.22 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.23 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.24&#1770.17 nM	High TROP2 expression (TROP2++)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.43&#1770.48 nM	Moderate TROP2 expression (TROP2++)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 3 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.68&#1770.31 nM	Moderate TROP2 expression (TROP2++)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Esophageal squamous cell carcinoma, Squamous cell carcinoma of the esophagus	KYSE150 cells		CVCL_1348
Experiment 4 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.73&#1770.21 nM	High TROP2 expression (TROP2++)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 5 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.22&#1770.48 nM	High TROP2 expression (TROP2++)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	T3M4 cells		CVCL_4056
Experiment 6 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.55&#1770.17 nM	Moderate TROP2 expression (TROP2++)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 7 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.81&#1770.06 nM	High TROP2 expression (TROP2++)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 8 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15.02&#1770.09 nM	Negative TROP2 expression (TROP2-)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Esophageal squamous cell carcinoma, Squamous cell carcinoma of the esophagus	Eca109 cells		CVCL_6898
Experiment 9 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15.86&#1770.51 nM	Low TROP2 expression (TROP2+)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 10 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	AsPC-1 cells		CVCL_0152
Experiment 11 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 12 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 13 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Colon carcinoma	HCT116 cells		CVCL_0291
Experiment 14 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Low TROP2 expression (TROP2+)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	SW480 cells		CVCL_0546
Experiment 15 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Lung large cell carcinoma	H460 cells		CVCL_0459
Experiment 16 Reporting the Activity Date of This ADC					[130]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative TROP2 expression (TROP2-)
Method Description	The cytotoxicity of hIMB1636-MMAE and free MMAE was evaluated by the Cell Counting Kit-8 (CCK-8) assay (Dojindo, Kyushu, Japan). Cells were plated at 2 × 103 to 8 × 103 cells/well in 100 uL culture medium into 96-well plates. Following an overnight incubation at 37 °C, the cells were cultured continuously for 48 h in 100 uL of medium containing various concentrations of drugs (100, 10, 1, 0.1, 0.01, and 0.001 nM). Then, the medium was replaced with 100 uL of fresh medium containing 10% CCK-8 reagent and incubated for 1 h. The absorbance was measured at 450 nm by a SpectraMax i3x Multi-Mode microplate reader (Molecular Devices, LLC, USA). The half-maximal inhibitory concentration (IC50) of the samples was calculated by Prism GraphPad 6.0 (GraphPad Software, San Diego, CA). The data are presented as the mean ± SD for three independent experiments.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	A549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.32 nM	High L1CAM expression (L1CAM +++)
Method Description	HeLa cells are cultured in DMEM complete medium (Corning, 10-013-CVR) containing 10% FBS (Gibco, 10099-141) and 100 U/mL penicillin-streptomycin mixture (Thermofisher, 15140122). When the cell coverage in the culture container reaches 80-90%, TrypLE (Thermofisher, 12604-013) is used to digest the HeLa cells from the culture container, and they are seeded in a 96-well cell culture plate (Greiner, 655098) at a density of 3.3X103 cells/mL, with 500 cells per well (145uL complete medium),and the 96-well plate is incubated at 37°C overnight. The next day, (ADC) is diluted in complete medium in a 4-fold serial dilution, with 9 concentration gradient points. Then, 5uL of dilution of the ADC molecule is added to each well in the 96-well cell culture plate, gently mixed, and the 96-well plate is incubated at 37°C for 6 days. Finally, 75 uL of CTG is added to each well, gently mixed, and the 96-well plate is incubated at room temperature for 10 minutes. Then the luminescence signal is detected using a multimode microplate reader (PerkinElmer Envision 2105). A dose-inhibition curve is generated, and the half-maximal inhibitory concentration (IC50) is calculated using non-linear regression with GraphPad software.    Click to Show/Hide
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030
Experiment 2 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	91 nM	Low L1CAM expression (L1CAM+)
Method Description	HeLa L1CAM-KO cells are cultured in DMEM complete medium (Corning, 10-013-CVR) containing 10% FBS (Gibco, 10099-141) and 100 U/mL penicillin-streptomycin mixture (Thermofisher, 15140122). When the cell coverage in the culture container reaches 80-90%, TrypLE (Thermofisher, 12604-013) is used to digest the HeLa L1CAM-KO cells from the culture container, and they are seeded in a 96-well cell culture plate (Greiner, 655098) at a density of 3.3X103 cells/mL, with 500 cells per well (145uL complete medium),and the 96-well plate is incubated at 37°C overnight. The next day, (ADC) is diluted in complete medium in a 4-fold serial dilution, with 9 concentration gradient points. Then, 5uL of dilution of the ADC molecule is added to each well in the 96-well cell culture plate, gently mixed, and the 96-well plate is incubated at 37°C for 6 days. Finally, 75 uL of CTG is added to each well, gently mixed, and the 96-well plate is incubated at room temperature for 10 minutes. Then the luminescence signal is detected using a multimode microplate reader (PerkinElmer Envision 2105). A dose-inhibition curve is generated, and the half-maximal inhibitory concentration (IC50) is calculated using non-linear regression with GraphPad software.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	HeLa cells (L1CAM KO)		CVCL_0030

Experiment 1 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.33 nM	Moderate SORT1 expression (SORT1++)
Method Description	The in vitro cell-killing assay was carried out using MDA-MB-231, MCF-7, MCF-10A, and T47D. Cells were plated in 96-well plates (5000 cells/well). After 1 h incubation, ADCs were added in a serial of concentrations with three replicates per concentration. The concentration of ADCs against MDA-MB-231, MCF-7, and MCF-10A ranged from 300 nM to 137 pM, while the range of concentration was from 100 nM to 46 pM for T47D. This was followed by another 72 h of culture. Cell viability was detected using the Cell Counting Kit 8 (APExBIO, Houston, TX, USA).    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma of no special type	T47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.3 nM	Moderate SORT1 expression (SORT1++)
Method Description	The in vitro cell-killing assay was carried out using MDA-MB-231, MCF-7, MCF-10A, and T47D. Cells were plated in 96-well plates (5000 cells/well). After 1 h incubation, ADCs were added in a serial of concentrations with three replicates per concentration. The concentration of ADCs against MDA-MB-231, MCF-7, and MCF-10A ranged from 300 nM to 137 pM, while the range of concentration was from 100 nM to 46 pM for T47D. This was followed by another 72 h of culture. Cell viability was detected using the Cell Counting Kit 8 (APExBIO, Houston, TX, USA).    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[131]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.3 nM	Moderate SORT1 expression (SORT1++)
Method Description	The in vitro cell-killing assay was carried out using MDA-MB-231, MCF-7, MCF-10A, and T47D. Cells were plated in 96-well plates (5000 cells/well). After 1 h incubation, ADCs were added in a serial of concentrations with three replicates per concentration. The concentration of ADCs against MDA-MB-231, MCF-7, and MCF-10A ranged from 300 nM to 137 pM, while the range of concentration was from 100 nM to 46 pM for T47D. This was followed by another 72 h of culture. Cell viability was detected using the Cell Counting Kit 8 (APExBIO, Houston, TX, USA).    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[132]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.363&#1770.02 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					[132]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 10 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					[132]
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					[119]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.395 nM	High L1CAM expression (L1CAM +++)
Method Description	HeLa cells are cultured in DMEM complete medium (Corning, 10-013-CVR) containing 10% FBS (Gibco, 10099-141) and 100 U/mL penicillin-streptomycin mixture (Thermofisher, 15140122). When the cell coverage in the culture container reaches 80-90%, TrypLE (Thermofisher, 12604-013) is used to digest the HeLa cells from the culture container, and they are seeded in a 96-well cell culture plate (Greiner, 655098) at a density of 3.3X103 cells/mL, with 500 cells per well (145uL complete medium),and the 96-well plate is incubated at 37°C overnight. The next day, (ADC) is diluted in complete medium in a 4-fold serial dilution, with 9 concentration gradient points. Then, 5uL of dilution of the ADC molecule is added to each well in the 96-well cell culture plate, gently mixed, and the 96-well plate is incubated at 37°C for 6 days. Finally, 75 uL of CTG is added to each well, gently mixed, and the 96-well plate is incubated at room temperature for 10 minutes. Then the luminescence signal is detected using a multimode microplate reader (PerkinElmer Envision 2105). A dose-inhibition curve is generated, and the half-maximal inhibitory concentration (IC50) is calculated using non-linear regression with GraphPad software.    Click to Show/Hide
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030
Experiment 2 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	44 nM	Low L1CAM expression (L1CAM+)
Method Description	HeLa L1CAM-KO cells are cultured in DMEM complete medium (Corning, 10-013-CVR) containing 10% FBS (Gibco, 10099-141) and 100 U/mL penicillin-streptomycin mixture (Thermofisher, 15140122). When the cell coverage in the culture container reaches 80-90%, TrypLE (Thermofisher, 12604-013) is used to digest the HeLa L1CAM-KO cells from the culture container, and they are seeded in a 96-well cell culture plate (Greiner, 655098) at a density of 3.3X103 cells/mL, with 500 cells per well (145uL complete medium),and the 96-well plate is incubated at 37°C overnight. The next day, (ADC) is diluted in complete medium in a 4-fold serial dilution, with 9 concentration gradient points. Then, 5uL of dilution of the ADC molecule is added to each well in the 96-well cell culture plate, gently mixed, and the 96-well plate is incubated at 37°C for 6 days. Finally, 75 uL of CTG is added to each well, gently mixed, and the 96-well plate is incubated at room temperature for 10 minutes. Then the luminescence signal is detected using a multimode microplate reader (PerkinElmer Envision 2105). A dose-inhibition curve is generated, and the half-maximal inhibitory concentration (IC50) is calculated using non-linear regression with GraphPad software.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	HeLa cells (L1CAM KO)		CVCL_0030

Experiment 1 Reporting the Activity Date of This ADC					[133]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.4&#1777.2 nM	Positive ET expression (ET+++/++)
Method Description	Cell cytotoxicity was monitored using a specific assay (Abcam, Cambridge, UK- Cat # 112118). This cytotoxicity assay is based on the measurement of mitochondrial dehydrogenase activity using a specific dye. This assay evaluates the metabolic activity of viable cells. Cells were plated at 1500 cells/well in 100 ul culture medium. The following day, 100 ul of increasing concentrations of mAb, diluted in culture medium, were added to each well. Cells were incubated for 96 h at 37 °C in a 5% CO2 incubator. The OD570/OD605 nm ratio was used to determine cell viability in each well in triplicate according to the instructions. Data were analyzed using Prism 9.4 (GraphPad Software San Diego, CA, USA) to determine the half maximal inhibitory concentration (IC50) using the variable slope model after checking that we had a normal distribution of these data by a D'Agostino & Pearson test.    Click to Show/Hide
In Vitro Model	Melanoma	UACC-257 cells		CVCL_1779

Experiment 1 Reporting the Activity Date of This ADC					[134]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.425 nM	High FOLH1 expression (FOLH1 +++)
Method Description	In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	C4-2 cells		CVCL_4782

Experiment 1 Reporting the Activity Date of This ADC					[128]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.46 nM	High HER2 expression (HER2 +++)
Method Description	The MTT (3- (4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assays were performed using WT ADC and positively charged ADC in three cell lines with varying HER2 expression levels: N87 (high), MCF-7 (low), and MDA-MB-468 (non-expressing). Cells were seeded at a density of 10,000 cells per well in 96-well plates and incubated for 24 h before treatment. ADCs were added at concentrations ranging from 0.01 nM to 1000 nM, and cells were incubated for an additional 96 h. Following treatment, 5 mg/mL MTT solution was added to each well and incubated for 4 h, after which 10% SDS-HCl solution was added to dissolve the formazan crystals. Absorbance was measured at 570 nm the next day. Cell viability (%) was calculated as (ODtreated/ (ODcontrol) × 100%. GraphPad Prism (version 10.4.1) was used for curve fitting of the sigmoidal dose-response curves (cell viability vs. ADC concentration) under the nonlinear regression option, and the half-maximal inhibitory concentration (IC50) values were determined.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[128]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5.01 nM	Negative HER2 expression (HER2-)
Method Description	The MTT (3- (4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assays were performed using WT ADC and positively charged ADC in three cell lines with varying HER2 expression levels: N87 (high), MCF-7 (low), and MDA-MB-468 (non-expressing). Cells were seeded at a density of 10,000 cells per well in 96-well plates and incubated for 24 h before treatment. ADCs were added at concentrations ranging from 0.01 nM to 1000 nM, and cells were incubated for an additional 96 h. Following treatment, 5 mg/mL MTT solution was added to each well and incubated for 4 h, after which 10% SDS-HCl solution was added to dissolve the formazan crystals. Absorbance was measured at 570 nm the next day. Cell viability (%) was calculated as (ODtreated/ (ODcontrol) × 100%. GraphPad Prism (version 10.4.1) was used for curve fitting of the sigmoidal dose-response curves (cell viability vs. ADC concentration) under the nonlinear regression option, and the half-maximal inhibitory concentration (IC50) values were determined.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[128]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	81.4 nM	Low HER2 expression (HER2+)
Method Description	The MTT (3- (4, 5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assays were performed using WT ADC and positively charged ADC in three cell lines with varying HER2 expression levels: N87 (high), MCF-7 (low), and MDA-MB-468 (non-expressing). Cells were seeded at a density of 10,000 cells per well in 96-well plates and incubated for 24 h before treatment. ADCs were added at concentrations ranging from 0.01 nM to 1000 nM, and cells were incubated for an additional 96 h. Following treatment, 5 mg/mL MTT solution was added to each well and incubated for 4 h, after which 10% SDS-HCl solution was added to dissolve the formazan crystals. Absorbance was measured at 570 nm the next day. Cell viability (%) was calculated as (ODtreated/ (ODcontrol) × 100%. GraphPad Prism (version 10.4.1) was used for curve fitting of the sigmoidal dose-response curves (cell viability vs. ADC concentration) under the nonlinear regression option, and the half-maximal inhibitory concentration (IC50) values were determined.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[134]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.52 nM	High FOLH1 expression (FOLH1 +++)
Method Description	In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	C4-2 cells		CVCL_4782

Experiment 1 Reporting the Activity Date of This ADC					[134]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.542 nM	High FOLH1 expression (FOLH1 +++)
Method Description	In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	C4-2 cells		CVCL_4782

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.61 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.635 nM	High L1CAM expression (L1CAM +++)
Method Description	HeLa cells are cultured in DMEM complete medium (Corning, 10-013-CVR) containing 10% FBS (Gibco, 10099-141) and 100 U/mL penicillin-streptomycin mixture (Thermofisher, 15140122). When the cell coverage in the culture container reaches 80-90%, TrypLE (Thermofisher, 12604-013) is used to digest the HeLa cells from the culture container, and they are seeded in a 96-well cell culture plate (Greiner, 655098) at a density of 3.3X103 cells/mL, with 500 cells per well (145uL complete medium),and the 96-well plate is incubated at 37°C overnight. The next day, (ADC) is diluted in complete medium in a 4-fold serial dilution, with 9 concentration gradient points. Then, 5uL of dilution of the ADC molecule is added to each well in the 96-well cell culture plate, gently mixed, and the 96-well plate is incubated at 37°C for 6 days. Finally, 75 uL of CTG is added to each well, gently mixed, and the 96-well plate is incubated at room temperature for 10 minutes. Then the luminescence signal is detected using a multimode microplate reader (PerkinElmer Envision 2105). A dose-inhibition curve is generated, and the half-maximal inhibitory concentration (IC50) is calculated using non-linear regression with GraphPad software.    Click to Show/Hide
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030
Experiment 2 Reporting the Activity Date of This ADC					[119]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	100 nM	Low L1CAM expression (L1CAM+)
Method Description	HeLa L1CAM-KO cells are cultured in DMEM complete medium (Corning, 10-013-CVR) containing 10% FBS (Gibco, 10099-141) and 100 U/mL penicillin-streptomycin mixture (Thermofisher, 15140122). When the cell coverage in the culture container reaches 80-90%, TrypLE (Thermofisher, 12604-013) is used to digest the HeLa L1CAM-KO cells from the culture container, and they are seeded in a 96-well cell culture plate (Greiner, 655098) at a density of 3.3X103 cells/mL, with 500 cells per well (145uL complete medium),and the 96-well plate is incubated at 37°C overnight. The next day, (ADC) is diluted in complete medium in a 4-fold serial dilution, with 9 concentration gradient points. Then, 5uL of dilution of the ADC molecule is added to each well in the 96-well cell culture plate, gently mixed, and the 96-well plate is incubated at 37°C for 6 days. Finally, 75 uL of CTG is added to each well, gently mixed, and the 96-well plate is incubated at room temperature for 10 minutes. Then the luminescence signal is detected using a multimode microplate reader (PerkinElmer Envision 2105). A dose-inhibition curve is generated, and the half-maximal inhibitory concentration (IC50) is calculated using non-linear regression with GraphPad software.    Click to Show/Hide
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	HeLa cells (L1CAM KO)		CVCL_0030

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.64 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.72 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.78 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.0- 9.9 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 21 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma, Small cell lung cancer	NCI-H69 cells (+NE)		CVCL_1579
Experiment 2 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	10- 99 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 21 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma, Small cell lung cancer	NCI-H69 cells (-NE)		CVCL_1579
Experiment 3 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Activity Concentration at -50% (AC50)	1.0- 9.9 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (HT29: 1200 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 34 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	HT29 cells (+NE)		CVCL_0320
Experiment 4 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Activity Concentration at -50% (AC50)	1.0- 9.9 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 29 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma, Multiple myeloma	NCI-H929 cells (+NE)		CVCL_1600
Experiment 5 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Activity Concentration at -50% (AC50)	10- 99 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 31 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Renal cell carcinoma	786-O cells (+NE)		CVCL_1051
Experiment 6 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Activity Concentration at -50% (AC50)	100- 999 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (HT29: 1200 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 14 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	HT29 cells (-NE)		CVCL_0320
Experiment 7 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Activity Concentration at -50% (AC50)	> 1000 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 31 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Renal cell carcinoma	786-O cells (-NE)		CVCL_1051
Experiment 8 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Activity Concentration at -50% (AC50)	> 1000 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 29 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma, Multiple myeloma	NCI-H929 cells (-NE)		CVCL_1600

Experiment 1 Reporting the Activity Date of This ADC					[136]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1 nM	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.09 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.28 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[137]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.69&#1770.31 nM
Method Description	Human thyroid cancer cells were seeded in a 96-well plate at a density of 3000 cells per well overnight. The cell culture medium was replaced with the medium containing either chemo drugs (maximum concentration: 117.11 umol/L) or ICAM1-ADCs at serial diluted concentrations (maximum concentration: 0.67 umol/L). After 96h, cell cytotoxicity was determined by using a CCK-8 kit (KeyGEN Biotech, China) following the manufacturer's protocol. The absorbance at 450 nm was measured with an ELISA browser (Bio-Tek EL 800, USA). The experiments were repeated three times.    Click to Show/Hide
In Vitro Model	Differentiated thyroid carcinoma, Thyroid gland papillary carcinoma	IHH4 cells		CVCL_2960
Experiment 2 Reporting the Activity Date of This ADC					[137]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	7.35&#1771.45 nM
Method Description	Human thyroid cancer cells were seeded in a 96-well plate at a density of 3000 cells per well overnight. The cell culture medium was replaced with the medium containing either chemo drugs (maximum concentration: 117.11 umol/L) or ICAM1-ADCs at serial diluted concentrations (maximum concentration: 0.67 umol/L). After 96h, cell cytotoxicity was determined by using a CCK-8 kit (KeyGEN Biotech, China) following the manufacturer's protocol. The absorbance at 450 nm was measured with an ELISA browser (Bio-Tek EL 800, USA). The experiments were repeated three times.    Click to Show/Hide
In Vitro Model	Thyroid gland anaplastic carcinoma	8505C cells		CVCL_1054
Experiment 3 Reporting the Activity Date of This ADC					[137]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15.59&#1774.18 nM
Method Description	Human thyroid cancer cells were seeded in a 96-well plate at a density of 3000 cells per well overnight. The cell culture medium was replaced with the medium containing either chemo drugs (maximum concentration: 117.11 umol/L) or ICAM1-ADCs at serial diluted concentrations (maximum concentration: 0.67 umol/L). After 96h, cell cytotoxicity was determined by using a CCK-8 kit (KeyGEN Biotech, China) following the manufacturer's protocol. The absorbance at 450 nm was measured with an ELISA browser (Bio-Tek EL 800, USA). The experiments were repeated three times.    Click to Show/Hide
In Vitro Model	Thyroid gland anaplastic carcinoma, Anaplastic thyroid carcinoma	TCO1 cells		CVCL_M839
Experiment 4 Reporting the Activity Date of This ADC					[137]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	68.6&#17711.2 nM
Method Description	Human thyroid cancer cells were seeded in a 96-well plate at a density of 3000 cells per well overnight. The cell culture medium was replaced with the medium containing either chemo drugs (maximum concentration: 117.11 umol/L) or ICAM1-ADCs at serial diluted concentrations (maximum concentration: 0.67 umol/L). After 96h, cell cytotoxicity was determined by using a CCK-8 kit (KeyGEN Biotech, China) following the manufacturer's protocol. The absorbance at 450 nm was measured with an ELISA browser (Bio-Tek EL 800, USA). The experiments were repeated three times.    Click to Show/Hide
In Vitro Model	Thyroid carcinoma	BCPAP cells		CVCL_0153

Experiment 1 Reporting the Activity Date of This ADC					[138]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.8 nM	Positive MUC1-C expression (MUC1-C+++/++)
Method Description	Cells were seeded at a density of 1500-3500 cells per well in 96-well plates. The next day, the cells were treated with different concentrations of the drug. Cell viability and proliferation were assessed using the Alamar Blue Reagent (cat# DAL1100, Thermo Fisher Scientific) following the company protocol. The IC50 values were determined by nonlinear regression of the dose-response data using Prism 10.0 (SCR_002798, GraphPad Software). Fluorescence intensity (560 nm excitation/590 nm emission) was measured in at least triplicate wells.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma of no special type	MCF-7 cells (ER (D538G))		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[138]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	6.3 nM	Positive MUC1-C expression (MUC1-C+++/++)
Method Description	Cells were seeded at a density of 1500-3500 cells per well in 96-well plates. The next day, the cells were treated with different concentrations of the drug. Cell viability and proliferation were assessed using the Alamar Blue Reagent (cat# DAL1100, Thermo Fisher Scientific) following the company protocol. The IC50 values were determined by nonlinear regression of the dose-response data using Prism 10.0 (SCR_002798, GraphPad Software). Fluorescence intensity (560 nm excitation/590 nm emission) was measured in at least triplicate wells.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[138]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	27 nM	Positive MUC1-C expression (MUC1-C+++/++)
Method Description	Cells were seeded at a density of 1500-3500 cells per well in 96-well plates. The next day, the cells were treated with different concentrations of the drug. Cell viability and proliferation were assessed using the Alamar Blue Reagent (cat# DAL1100, Thermo Fisher Scientific) following the company protocol. The IC50 values were determined by nonlinear regression of the dose-response data using Prism 10.0 (SCR_002798, GraphPad Software). Fluorescence intensity (560 nm excitation/590 nm emission) was measured in at least triplicate wells.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma of no special type	MCF-7 cells (ER (Y537S))		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2 nM
Method Description	Tumor cells (RPMI-7951+p97) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Malignant melanoma	RPMI-7951 cells		CVCL_1666
Experiment 2 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2 nM
Method Description	Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 3 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2 nM
Method Description	Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 4 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5 nM	Moderate MELTF expression (MELTF++)
Method Description	Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 5 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM
Method Description	Tumor cells (RPMI-7951) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Malignant melanoma	RPMI-7951 cells		CVCL_1666

Experiment 1 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2 nM
Method Description	Tumor cells (RPMI-7951+p97) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Malignant melanoma	RPMI-7951 cells		CVCL_1666
Experiment 2 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	7 nM
Method Description	Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 3 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	100 nM
Method Description	Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 4 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	718 nM	Moderate MELTF expression (MELTF++)
Method Description	Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 5 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM
Method Description	Tumor cells (RPMI-7951) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Malignant melanoma	RPMI-7951 cells		CVCL_1666

Experiment 1 Reporting the Activity Date of This ADC					[139]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2 nM	High cMET expression (cMET +++)
Method Description	SNU-5 (1750 cells/well, 12.5 uL), A549 cells (750 cells/well, 12.5 uL), HT-29 (1000 cells/well, 12.5 uL) and SK-BR-3 (1000 cells/well, 12.5 uL) were seeded in a white flat-bottom 384-well plate (3570, Corning) at least 4-8 h before drug treatment for SNU-5 and 16-24 h for all the adherent cells. 2× working stock of the anti-cMET FDC (200 nM) or ADC (20-200 nM) were initially prepared in the cell growth media which were subsequently serially diluted in the corresponding media 3-fold. Following this, 12.5 uL of each of the serially diluted drug conjugates were added into the 384-well plate containing the cells. In a similar manner, replicates of 12.5 uL each of either a 2 uM Staurosporine (S1421, Selleck Chemicals) or media only was added into the wells to serve as the 100% cell killing and 0% cell killing, respectively. For the combination treatment, cells were treated with a 3-fold serial dilution of the anti-cMET IgG starting at 50 nM (final concentration in the well) while holding the FDC concentration constant at the approximate IC50 of 2 nM. After 96 h incubation at 37°C with 5% CO2, 25 uL of room temperature CellTiterGlo2.0 reagent (G9241, Promega) was added to each well using a multichannel pipette followed by a 2-min shaking using an orbital shaker (500 rpm), and then a 10-min incubation at room temperature. Afterwards, the plate was read using plate reader capable of reading luminescence in multi-well plates (Tecan Spark). Data were analyzed using GraphPad Prism software.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	SNU-5 cells		CVCL_0078

Experiment 1 Reporting the Activity Date of This ADC					[140]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.028&#1770.4680 nM	Positive SLCA2 expression (SLCA2+++/++)
Method Description	The MTT assay was performed to determin the in vitro efficacy of the 19G4-MMAE ADC. Cells were seeded in 96-well plates at a density of 5000 cells/well for SCC15, NPC/HK1, FADU, C666-1 at 37 °C and 5% CO2 overnight. Dilutions of PBS, 19G4, IgG-MMAE, and 19G4-MMAE solutions were added to cells for 72 h incubation at 37 °C. Cell viability were evaluated in triplicate by MTT assay. The IC50 was determined using Graphpad Prism version 9 (GraphPad Software, Inc.).    Click to Show/Hide
In Vitro Model	Squamous cell carcinoma of the oral tongue, Tongue squamous cell carcinoma	SCC15 cells		CVCL_1681
Experiment 2 Reporting the Activity Date of This ADC					[140]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	205.1 nM	Positive SLCA2 expression (SLCA2+++/++)
Method Description	The MTT assay was performed to determin the in vitro efficacy of the 19G4-MMAE ADC. Cells were seeded in 96-well plates at a density of 5000 cells/well for SCC15, NPC/HK1, FADU, C666-1 at 37 °C and 5% CO2 overnight. Dilutions of PBS, 19G4, IgG-MMAE, and 19G4-MMAE solutions were added to cells for 72 h incubation at 37 °C. Cell viability were evaluated in triplicate by MTT assay. The IC50 was determined using Graphpad Prism version 9 (GraphPad Software, Inc.).    Click to Show/Hide
In Vitro Model	Nasopharyngeal carcinoma	NPC/HK1 cells		CVCL_7084
Experiment 3 Reporting the Activity Date of This ADC					[140]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	235.4 nM	Positive SLCA2 expression (SLCA2+++/++)
Method Description	The MTT assay was performed to determin the in vitro efficacy of the 19G4-MMAE ADC. Cells were seeded in 96-well plates at a density of 5000 cells/well for SCC15, NPC/HK1, FADU, C666-1 at 37 °C and 5% CO2 overnight. Dilutions of PBS, 19G4, IgG-MMAE, and 19G4-MMAE solutions were added to cells for 72 h incubation at 37 °C. Cell viability were evaluated in triplicate by MTT assay. The IC50 was determined using Graphpad Prism version 9 (GraphPad Software, Inc.).    Click to Show/Hide
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 4 Reporting the Activity Date of This ADC					[140]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	344.4 nM	Negative SLCA2 expression (SLCA2-)
Method Description	The MTT assay was performed to determin the in vitro efficacy of the 19G4-MMAE ADC. Cells were seeded in 96-well plates at a density of 5000 cells/well for SCC15, NPC/HK1, FADU, C666-1 at 37 °C and 5% CO2 overnight. Dilutions of PBS, 19G4, IgG-MMAE, and 19G4-MMAE solutions were added to cells for 72 h incubation at 37 °C. Cell viability were evaluated in triplicate by MTT assay. The IC50 was determined using Graphpad Prism version 9 (GraphPad Software, Inc.).    Click to Show/Hide
In Vitro Model	Nasopharyngeal carcinoma	C666-1 cells		CVCL_7949

Experiment 1 Reporting the Activity Date of This ADC					[141]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.04 nM	Positive CADM1 expression (CADM1+++/++)
Method Description	Killing of endometrial adenocarcinoma cells by h3E1-MMAE ADC. Endometrial adenocarcinoma cells were cultured in a 96-well plate at 30% confluence, and either hIgG-MMAE or h3E1-MMAE ADC was added at indicated concentrations. After 5 days, cell viability was calculated by WST-8 assays in triplicate. The mean is plotted in a line graph, with a thin vertical line indicating the standard deviation. a and b, P-value <.05 and .01, respectively, when compared with the value of h3E1-MMAE ADC at the identical concentration. IC50 (ug/ml and nM) is calculated.    Click to Show/Hide
In Vitro Model	Type II endometrial adenocarcinoma	HEC-50B cells		CVCL_2929
Experiment 2 Reporting the Activity Date of This ADC					[141]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	12.02 nM	Positive CADM1 expression (CADM1+++/++)
Method Description	Killing of endometrial adenocarcinoma cells by h3E1-MMAE ADC. Endometrial adenocarcinoma cells were cultured in a 96-well plate at 30% confluence, and either hIgG-MMAE or h3E1-MMAE ADC was added at indicated concentrations. After 5 days, cell viability was calculated by WST-8 assays in triplicate. The mean is plotted in a line graph, with a thin vertical line indicating the standard deviation. a and b, P-value <.05 and .01, respectively, when compared with the value of h3E1-MMAE ADC at the identical concentration. IC50 (ug/ml and nM) is calculated.    Click to Show/Hide
In Vitro Model	Endometrial adenocarcinoma	HEC-1B cells		CVCL_0294
Experiment 3 Reporting the Activity Date of This ADC					[141]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	13.03 nM	Positive CADM1 expression (CADM1+++/++)
Method Description	Killing of endometrial adenocarcinoma cells by h3E1-MMAE ADC. Endometrial adenocarcinoma cells were cultured in a 96-well plate at 30% confluence, and either hIgG-MMAE or h3E1-MMAE ADC was added at indicated concentrations. After 5 days, cell viability was calculated by WST-8 assays in triplicate. The mean is plotted in a line graph, with a thin vertical line indicating the standard deviation. a and b, P-value <.05 and .01, respectively, when compared with the value of h3E1-MMAE ADC at the identical concentration. IC50 (ug/ml and nM) is calculated.    Click to Show/Hide
In Vitro Model	Uveal melanoma	OCM-2 cells		CVCL_6936
Experiment 4 Reporting the Activity Date of This ADC					[141]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	24.32 nM	Positive CADM1 expression (CADM1+++/++)
Method Description	Killing of endometrial adenocarcinoma cells by h3E1-MMAE ADC. Endometrial adenocarcinoma cells were cultured in a 96-well plate at 30% confluence, and either hIgG-MMAE or h3E1-MMAE ADC was added at indicated concentrations. After 5 days, cell viability was calculated by WST-8 assays in triplicate. The mean is plotted in a line graph, with a thin vertical line indicating the standard deviation. a and b, P-value <.05 and .01, respectively, when compared with the value of h3E1-MMAE ADC at the identical concentration. IC50 (ug/ml and nM) is calculated.    Click to Show/Hide
In Vitro Model	Endometrial adenocarcinoma	JHUM-3 cells		CVCL_4657
Experiment 5 Reporting the Activity Date of This ADC					[141]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM	Negative CADM1 expression (CADM1 -)
Method Description	Killing of endometrial adenocarcinoma cells by h3E1-MMAE ADC. Endometrial adenocarcinoma cells were cultured in a 96-well plate at 30% confluence, and either hIgG-MMAE or h3E1-MMAE ADC was added at indicated concentrations. After 5 days, cell viability was calculated by WST-8 assays in triplicate. The mean is plotted in a line graph, with a thin vertical line indicating the standard deviation. a and b, P-value <.05 and .01, respectively, when compared with the value of h3E1-MMAE ADC at the identical concentration. IC50 (ug/ml and nM) is calculated.    Click to Show/Hide
In Vitro Model	Endometrial adenocarcinoma	HHUA cells		CVCL_3866

Experiment 1 Reporting the Activity Date of This ADC					[136]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.3 nM	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[142]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	2.88 nM	High ROR1 expression ( ROR1 +++)
Method Description	In each ultra-low attachment U bottom 384-well transparent plate patient-derived lung cancer cells AMB-LC-0003T were dispensed in triplicate at 500 cells/well in 40 p1l of M10018 (Aimedbio) media. After centrifugation at 250 g for 2 minutes, reaction was carried out at 37°C and 5% Co 2 for 24 hours. Thereafter, each antibody-drug conjugate was serially diluted 3-fold from 500 nM to 0.314 pM and the cells were treated therewith. The plate was reacted again at 37°C and 5% Co2 for 6 days. After a total of 7 days of reaction, spheroids were formed by the cells in the 384-well plate, so images of spheroids in each well were captured using Operetta CLS (PerkinElmer) according to a high-content screening method. To maintain the spheroid form of the cells in each well, washing was not performed before analysis. The captured images were converted into volume through additional analysis, and the spheroid volume values by concentration were standardized based on the spheroid treated with the lowest concentration of drug. Graphs were created with a log (inhibitor) vs. normalized response - Variable slope using GraphPad Prism 9.3.1, and IC5 o values were obtained.    Click to Show/Hide
In Vitro Model	lung cancer	AMB-LC-0003T cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[142]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	162.1 nM	Low ROR1 expression (ROR1+)
Method Description	In each ultra-low attachment U bottom 384-well transparent plate patient-derived lung cancer cells AMB-LC-0003T were dispensed in triplicate at 500 cells/well in 40 p1l of M10018 (Aimedbio) media. After centrifugation at 250 g for 2 minutes, reaction was carried out at 37°C and 5% Co 2 for 24 hours. Thereafter, each antibody-drug conjugate was serially diluted 3-fold from 500 nM to 0.314 pM and the cells were treated therewith. The plate was reacted again at 37°C and 5% Co2 for 6 days. After a total of 7 days of reaction, spheroids were formed by the cells in the 384-well plate, so images of spheroids in each well were captured using Operetta CLS (PerkinElmer) according to a high-content screening method. To maintain the spheroid form of the cells in each well, washing was not performed before analysis. The captured images were converted into volume through additional analysis, and the spheroid volume values by concentration were standardized based on the spheroid treated with the lowest concentration of drug. Graphs were created with a log (inhibitor) vs. normalized response - Variable slope using GraphPad Prism 9.3.1, and IC5 o values were obtained.    Click to Show/Hide
In Vitro Model	lung cancer	AMB-LC-0003T cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3 nM
Method Description	Tumor cells (RPMI-7951+p97) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Malignant melanoma	RPMI-7951 cells		CVCL_1666
Experiment 2 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3 nM
Method Description	Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 3 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5 nM
Method Description	Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 4 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	12 nM	Moderate MELTF expression (MELTF++)
Method Description	Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 5 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM
Method Description	Tumor cells (RPMI-7951) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Malignant melanoma	RPMI-7951 cells		CVCL_1666

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[118]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 3 nM	Positive HER2 expression (HER2+++/++)
Method Description	SK-BR-3 cells (a HER2-positive cell line) were seeded at 2000 cells/well in a 96-well plate and incubated overnight at 37°C in a humidified atmosphere containing 5% CO2. The cells were treated with serially diluted homogeneous ADCs and incubated for 4 days at 37°C in a humidified atmosphere containing 5% CO2. The cytotoxicity was evaluated using the Cell Counting Kit SF (Nacalai Tesque). Each dose-response curve was fitted by 4-parameter logistic model with same upper/lower asymptotes using GraphPad prism 7 software, and calculated IC50 of homogeneous ADCs    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4 nM
Method Description	Tumor cells (RPMI-7951+p97) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Malignant melanoma	RPMI-7951 cells		CVCL_1666
Experiment 2 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	6 nM
Method Description	Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 3 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	55 nM
Method Description	Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 4 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	444 nM	Moderate MELTF expression (MELTF++)
Method Description	Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 5 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM
Method Description	Tumor cells (RPMI-7951) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Malignant melanoma	RPMI-7951 cells		CVCL_1666

Experiment 1 Reporting the Activity Date of This ADC					[143]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.27 nM	Positive PD-L1 expression (PD-L1+++/++)
Method Description	The starting point of the small molecule drug was 500 nM, and the drug was diluted 5 times sequentially, for a total of eight concentration points. Cells were laid on 96-well plate at 4000 cells/well, cultured overnight and were added with diluted drugs, in the incubator for 72 h. All cells incubated with the drug were tested for cell viability using Cell Counting Kit-8 (CCK-8) kit (Meilunbio, Dalian, China).    Click to Show/Hide
In Vitro Model	Glioblastoma	U87 cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[142]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5.38 nM	High ROR1 expression ( ROR1 +++)
Method Description	In each ultra-low attachment U bottom 384-well transparent plate patient-derived lung cancer cells AMB-LC-0003T were dispensed in triplicate at 500 cells/well in 40 p1l of M10018 (Aimedbio) media. After centrifugation at 250 g for 2 minutes, reaction was carried out at 37°C and 5% Co 2 for 24 hours. Thereafter, each antibody-drug conjugate was serially diluted 3-fold from 500 nM to 0.314 pM and the cells were treated therewith. The plate was reacted again at 37°C and 5% Co2 for 6 days. After a total of 7 days of reaction, spheroids were formed by the cells in the 384-well plate, so images of spheroids in each well were captured using Operetta CLS (PerkinElmer) according to a high-content screening method. To maintain the spheroid form of the cells in each well, washing was not performed before analysis. The captured images were converted into volume through additional analysis, and the spheroid volume values by concentration were standardized based on the spheroid treated with the lowest concentration of drug. Graphs were created with a log (inhibitor) vs. normalized response - Variable slope using GraphPad Prism 9.3.1, and IC5 o values were obtained.    Click to Show/Hide
In Vitro Model	lung cancer	AMB-LC-0003T cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[142]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	122.4 nM	Low ROR1 expression (ROR1+)
Method Description	In each ultra-low attachment U bottom 384-well transparent plate patient-derived lung cancer cells AMB-LC-0003T were dispensed in triplicate at 500 cells/well in 40 p1l of M10018 (Aimedbio) media. After centrifugation at 250 g for 2 minutes, reaction was carried out at 37°C and 5% Co 2 for 24 hours. Thereafter, each antibody-drug conjugate was serially diluted 3-fold from 500 nM to 0.314 pM and the cells were treated therewith. The plate was reacted again at 37°C and 5% Co2 for 6 days. After a total of 7 days of reaction, spheroids were formed by the cells in the 384-well plate, so images of spheroids in each well were captured using Operetta CLS (PerkinElmer) according to a high-content screening method. To maintain the spheroid form of the cells in each well, washing was not performed before analysis. The captured images were converted into volume through additional analysis, and the spheroid volume values by concentration were standardized based on the spheroid treated with the lowest concentration of drug. Graphs were created with a log (inhibitor) vs. normalized response - Variable slope using GraphPad Prism 9.3.1, and IC5 o values were obtained.    Click to Show/Hide
In Vitro Model	lung cancer	AMB-LC-0003T cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[144]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	7.81&#1772.31 nM
Method Description	Cells were seeded into 96-well plates (5000 cells/well) and incubated for 24 h at 37°C in 5% CO2. To investigate the effect of NECTIN4-targeted ADC, cells were incubated with medium containing enfortumab or enfortumab-MMAE conjugate. After 72 h of incubation, 10 uL of CCK-8 solution was added to each well and incubated for 3 h at 37°C. Then, absorbance at 450 nm was measured using a microplate reader (Bio-Rad Laboratories Inc.). The IC50 of the NECTIN4-targeted ADC was calculated using GraphPad Prism 7 software (GraphPad Software, San Diego, CA, USA).    Click to Show/Hide
In Vitro Model	Extramammary Paget disease	KS-EMPD-1 cells		CVCL_C4LP

Experiment 1 Reporting the Activity Date of This ADC					[143]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	8.01 nM	Positive PD-L1 expression (PD-L1+++/++)
Method Description	The starting point of the small molecule drug was 500 nM, and the drug was diluted 5 times sequentially, for a total of eight concentration points. Cells were laid on 96-well plate at 4000 cells/well, cultured overnight and were added with diluted drugs, in the incubator for 72 h. All cells incubated with the drug were tested for cell viability using Cell Counting Kit-8 (CCK-8) kit (Meilunbio, Dalian, China).    Click to Show/Hide
In Vitro Model	Glioblastoma	U87 cells		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 10 nM	High ROR1 expression (ROR1+++);ROR1 MFI=79464.6
Method Description	A total of 250-1500cells (MDA-MB-231) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 10 nM	High ROR1 expression (ROR1+++);ROR1 MFI=70456.2
Method Description	A total of 250-1500cells (NCI-N87) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 10 nM	High ROR1 expression (ROR1+++);ROR1 MFI=97567.9
Method Description	A total of 250-1500cells (NCI-H446) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma	NCI-H446 cells		CVCL_1562
Experiment 4 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 10 nM	High ROR1 expression (ROR1+++);ROR1 MFI=128559.5
Method Description	A total of 250-1500cells (HT-29) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Colon cancer	HT29 cells		CVCL_A8EZ
Experiment 5 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 10 nM	High ROR1 expression (ROR1+++);ROR1 MFI=87015.2
Method Description	A total of 250-1500cells (HCC827) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 6 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	< 10 nM	High ROR1 expression (ROR1+++);ROR1 MFI=111495.8
Method Description	A total of 250-1500cells (HCC1187) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	HCC1187 cells		CVCL_1247
Experiment 7 Reporting the Activity Date of This ADC					[96]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Low ROR1 expression (ROR1+);ROR1 MFI=6610.4
Method Description	A total of 250-1500cells (MCF-7) were plated in 150ul cell culture medium per well of a 96-well flat plate in the appropriate growth media. After 3-5h, add ADC at different concentrations respectively. Set 2-4 replicate wells for each drug concentration, as well as corresponding vehicle control and blank control wells. After 5-6 days of treatment (according to the cell growth rate to ensure sufficient cell division), pour off the culture medium, add CCK8 reaction solution (purchased from MCE, cat#HY - K0301), 100 uL per well. Incubate at 37°C until the expected color intensity is reached, and measure the cell viability (OD450nm) of each group.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	10- 99 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 22 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma, Small cell lung cancer	NCI-H69 cells (-NE)		CVCL_1579
Experiment 2 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	10- 99 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H69: 2000 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 22 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Lung small cell carcinoma, Small cell lung cancer	NCI-H69 cells (+NE)		CVCL_1579
Experiment 3 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Activity Concentration at -50% (AC50)	1.0- 9.9 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (HT29: 1200 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 35 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	HT29 cells (+NE)		CVCL_0320
Experiment 4 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Activity Concentration at -50% (AC50)	1.0- 9.9 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 30 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma, Multiple myeloma	NCI-H929 cells (+NE)		CVCL_1600
Experiment 5 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Activity Concentration at -50% (AC50)	10- 99 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (HT29: 1200 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 15 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	HT29 cells (-NE)		CVCL_0320
Experiment 6 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Activity Concentration at -50% (AC50)	100- 999 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone, whereas to the second set the test compound and 5nM hum.neutrophil elastase were added followed by a 96 h incubation in an incubator at 37°C and 32 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Renal cell carcinoma	786-O cells (+NE)		CVCL_1051
Experiment 7 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Activity Concentration at -50% (AC50)	> 1000 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (786-0: 1500 cells/ well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 32 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Renal cell carcinoma	786-O cells (-NE)		CVCL_1051
Experiment 8 Reporting the Activity Date of This ADC					[135]
Efficacy Data	Activity Concentration at -50% (AC50)	> 1000 nM
Method Description	After cell counting a defined cell number was sowed into a 96-well culture plate with white bottom (from Costar #3610) (NCI H292: 2500 cells/well) in total volume 100 uL. The cells (except MOLM-13 cells, these cells were directly treated) were then incubated in an incubator at 37°C and 5 % carbon dioxide. After 48 h, the medium was replaced. The treatment started by adding the test compounds in 10 uL of culture medium to the cells in triplicates. Concentrations ranging from 10-5 M to 10-13 M were chosen. Two identical treated sets of samples were prepared. One set was treated with the test compound alone and was added followed by a 96 h incubation in an incubator at 37°C and 30 % carbon dioxide.    Click to Show/Hide
In Vitro Model	Plasma cell myeloma, Multiple myeloma	NCI-H929 cells (-NE)		CVCL_1600

Experiment 1 Reporting the Activity Date of This ADC					[134]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	10.2 nM	High FOLH1 expression (FOLH1 +++)
Method Description	In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	C4-2 cells		CVCL_4782

Experiment 1 Reporting the Activity Date of This ADC					[142]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	10.62 nM	High ROR1 expression ( ROR1 +++)
Method Description	In each ultra-low attachment U bottom 384-well transparent plate patient-derived lung cancer cells AMB-LC-0003T were dispensed in triplicate at 500 cells/well in 40 p1l of M10018 (Aimedbio) media. After centrifugation at 250 g for 2 minutes, reaction was carried out at 37°C and 5% Co 2 for 24 hours. Thereafter, each antibody-drug conjugate was serially diluted 3-fold from 500 nM to 0.314 pM and the cells were treated therewith. The plate was reacted again at 37°C and 5% Co2 for 6 days. After a total of 7 days of reaction, spheroids were formed by the cells in the 384-well plate, so images of spheroids in each well were captured using Operetta CLS (PerkinElmer) according to a high-content screening method. To maintain the spheroid form of the cells in each well, washing was not performed before analysis. The captured images were converted into volume through additional analysis, and the spheroid volume values by concentration were standardized based on the spheroid treated with the lowest concentration of drug. Graphs were created with a log (inhibitor) vs. normalized response - Variable slope using GraphPad Prism 9.3.1, and IC5 o values were obtained.    Click to Show/Hide
In Vitro Model	lung cancer	AMB-LC-0003T cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[142]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	159.5 nM	Low ROR1 expression (ROR1+)
Method Description	In each ultra-low attachment U bottom 384-well transparent plate patient-derived lung cancer cells AMB-LC-0003T were dispensed in triplicate at 500 cells/well in 40 p1l of M10018 (Aimedbio) media. After centrifugation at 250 g for 2 minutes, reaction was carried out at 37°C and 5% Co 2 for 24 hours. Thereafter, each antibody-drug conjugate was serially diluted 3-fold from 500 nM to 0.314 pM and the cells were treated therewith. The plate was reacted again at 37°C and 5% Co2 for 6 days. After a total of 7 days of reaction, spheroids were formed by the cells in the 384-well plate, so images of spheroids in each well were captured using Operetta CLS (PerkinElmer) according to a high-content screening method. To maintain the spheroid form of the cells in each well, washing was not performed before analysis. The captured images were converted into volume through additional analysis, and the spheroid volume values by concentration were standardized based on the spheroid treated with the lowest concentration of drug. Graphs were created with a log (inhibitor) vs. normalized response - Variable slope using GraphPad Prism 9.3.1, and IC5 o values were obtained.    Click to Show/Hide
In Vitro Model	lung cancer	AMB-LC-0003T cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[134]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	11.3 nM	High FOLH1 expression (FOLH1 +++)
Method Description	In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	C4-2 cells		CVCL_4782

Experiment 1 Reporting the Activity Date of This ADC					[134]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	12.5 nM	High FOLH1 expression (FOLH1 +++)
Method Description	In Vitro Potency Studies - In vitro potency of anti-PSMA ADCs is determined using a metastatic castration-resistant prostate cancer (mCRPC) representative cell-line, C4-2. The cell culture is incubated with antibody drug conjugates for 96 hours at 37C. Cell viability is analyzed using Cell Titer GlO (Promega, USA). Anti-proliferative activity is represented by potency, ICso, the concentration at which 50% of the maximum activity is achieved and cell killing, and Emax, the maximum level of growth inhibition. Table 5 summarizes the cell killing and in vitro potency of the anti-PSMA ADCs.    Click to Show/Hide
In Vitro Model	Prostate carcinoma	C4-2 cells		CVCL_4782

Experiment 1 Reporting the Activity Date of This ADC					[145]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	13.18 nM	High B7-H3 expression (B7-H3 +++)
Method Description	Cancer cell lines U87, U251, U87/B7-H3 KO cells (3000 cells per well) at logarithmic growth stage were seeded in 96-well plates and allowed to adhere overnight at 37 °C in a humidified incubator of 5% CO2. After that, ADCs, 401 and MMAE were diluted at a certain concentration gradient and added to cell plates in triplicate, the cells were treated at 37 °C with 5% CO2 for 72 h. In addition, the complete medium without cells served as the blank and the cells cultured in medium alone served as vehicle control.    Click to Show/Hide
In Vitro Model	Glioblastoma	U87 cells		CVCL_0022
Experiment 2 Reporting the Activity Date of This ADC					[145]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	35.48 nM	High B7-H3 expression (B7-H3 +++)
Method Description	Cancer cell lines U87, U251, U87/B7-H3 KO cells (3000 cells per well) at logarithmic growth stage were seeded in 96-well plates and allowed to adhere overnight at 37 °C in a humidified incubator of 5% CO2. After that, ADCs, 401 and MMAE were diluted at a certain concentration gradient and added to cell plates in triplicate, the cells were treated at 37 °C with 5% CO2 for 72 h. In addition, the complete medium without cells served as the blank and the cells cultured in medium alone served as vehicle control.    Click to Show/Hide
In Vitro Model	Astrocytoma	U251 cells		CVCL_0021
Experiment 3 Reporting the Activity Date of This ADC					[145]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	239.88 nM	High B7-H3 expression (B7-H3 +++)
Method Description	Cancer cell lines U87, U251, U87/B7-H3 KO cells (3000 cells per well) at logarithmic growth stage were seeded in 96-well plates and allowed to adhere overnight at 37 °C in a humidified incubator of 5% CO2. After that, ADCs, 401 and MMAE were diluted at a certain concentration gradient and added to cell plates in triplicate, the cells were treated at 37 °C with 5% CO2 for 72 h. In addition, the complete medium without cells served as the blank and the cells cultured in medium alone served as vehicle control.    Click to Show/Hide
In Vitro Model	Glioblastoma	U87 cells (B7-H3 KO)		CVCL_0022

Experiment 1 Reporting the Activity Date of This ADC					[146]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	14.27 nM	Moderate 5T4 expression (5T4++)
Method Description	Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[146]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	16.32 nM	Moderate 5T4 expression (5T4++)
Method Description	Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.    Click to Show/Hide
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 3 Reporting the Activity Date of This ADC					[146]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	46.71 nM	High 5T4 expression (5T4 +++)
Method Description	Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 4 Reporting the Activity Date of This ADC					[146]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	51.22 nM	High 5T4 expression (5T4 +++)
Method Description	Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 5 Reporting the Activity Date of This ADC					[146]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	61.98 nM	Moderate 5T4 expression (5T4++)
Method Description	Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 6 Reporting the Activity Date of This ADC					[146]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM	High 5T4 expression (5T4 +++)
Method Description	Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 7 Reporting the Activity Date of This ADC					[146]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM	Low 5T4 expression (5T4+)
Method Description	Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.    Click to Show/Hide
In Vitro Model	Normal	FCHO cells		CVCL_U424

Experiment 1 Reporting the Activity Date of This ADC					[146]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	14.57 nM	Moderate 5T4 expression (5T4++)
Method Description	Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.    Click to Show/Hide
In Vitro Model	Ovarian mixed germ cell tumor	PA-1 cells		CVCL_0479
Experiment 2 Reporting the Activity Date of This ADC					[146]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	16.01 nM	Moderate 5T4 expression (5T4++)
Method Description	Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[146]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	23.5 nM	High 5T4 expression (5T4 +++)
Method Description	Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 4 Reporting the Activity Date of This ADC					[146]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	41.82 nM	High 5T4 expression (5T4 +++)
Method Description	Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 5 Reporting the Activity Date of This ADC					[146]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	45.43 nM	Moderate 5T4 expression (5T4++)
Method Description	Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 6 Reporting the Activity Date of This ADC					[146]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM	High 5T4 expression (5T4 +++)
Method Description	Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	PANC-1 cells		CVCL_0480
Experiment 7 Reporting the Activity Date of This ADC					[146]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM	Low 5T4 expression (5T4+)
Method Description	Cytotoxicity assays performed in the presence of n501-MMAE and n501-alphaHSA-MMAE and their antibody control was assessed using cells plated at 5000 cells per well in medium with in flat bottom 96-well cell culture plates (NEST Biotechnology, China). After 12 h, tumor cells were added with serial dilutions of n501-alphaHSA-MMAE or n501-MMAE in triplicate wells and incubated for 72 h at 37°C in a humidified 5% CO2 atmosphere. After mixing CCK8 reagent and complete medium at a ratio of 1:9, the cell culture medium was removed and CCK8 working solution was added for another 1-3 h. The absorbance was measured by a microplate reader at 450 nm, and the cell viability ratio (%) was calculated using the following formula: (A sample - A blank)/ (A control - A blank) × 100%.    Click to Show/Hide
In Vitro Model	Normal	FCHO cells		CVCL_U424

Experiment 1 Reporting the Activity Date of This ADC					[143]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	15.88 nM	Moderate PD-L1 expression (PD-L1++)
Method Description	The starting point of the small molecule drug was 500 nM, and the drug was diluted 5 times sequentially, for a total of eight concentration points. Cells were laid on 96-well plate at 4000 cells/well, cultured overnight and were added with diluted drugs, in the incubator for 72 h. All cells incubated with the drug were tested for cell viability using Cell Counting Kit-8 (CCK-8) kit (Meilunbio, Dalian, China).    Click to Show/Hide
In Vitro Model	Colon carcinoma	HCT116 cells		CVCL_0291
Experiment 2 Reporting the Activity Date of This ADC					[143]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	25.55 nM	Moderate PD-L1 expression (PD-L1++)
Method Description	The starting point of the small molecule drug was 500 nM, and the drug was diluted 5 times sequentially, for a total of eight concentration points. Cells were laid on 96-well plate at 4000 cells/well, cultured overnight and were added with diluted drugs, in the incubator for 72 h. All cells incubated with the drug were tested for cell viability using Cell Counting Kit-8 (CCK-8) kit (Meilunbio, Dalian, China).    Click to Show/Hide
In Vitro Model	Colon carcinoma	HCT116 cells		CVCL_0291
Experiment 3 Reporting the Activity Date of This ADC					[143]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	25.7 nM	Positive PD-L1 expression (PD-L1+++/++)
Method Description	The starting point of the small molecule drug was 500 nM, and the drug was diluted 5 times sequentially, for a total of eight concentration points. Cells were laid on 96-well plate at 4000 cells/well, cultured overnight and were added with diluted drugs, in the incubator for 72 h. All cells incubated with the drug were tested for cell viability using Cell Counting Kit-8 (CCK-8) kit (Meilunbio, Dalian, China).    Click to Show/Hide
In Vitro Model	Glioblastoma	U87 cells		CVCL_0022
Experiment 4 Reporting the Activity Date of This ADC					[143]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	68.49 nM	Moderate PD-L1 expression (PD-L1++)
Method Description	The starting point of the small molecule drug was 500 nM, and the drug was diluted 5 times sequentially, for a total of eight concentration points. Cells were laid on 96-well plate at 4000 cells/well, cultured overnight and were added with diluted drugs, in the incubator for 72 h. All cells incubated with the drug were tested for cell viability using Cell Counting Kit-8 (CCK-8) kit (Meilunbio, Dalian, China).    Click to Show/Hide
In Vitro Model	Colon carcinoma	HCT116 cells		CVCL_0291

Experiment 1 Reporting the Activity Date of This ADC					[147]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	16.9 nM	Moderate CD276 expression (CD276 ++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-468 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[147]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	18.8 nM	Moderate CD276 expression (CD276 ++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-231 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 3 Reporting the Activity Date of This ADC					[147]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	40.8 nM	High CD276expression (CD276 +++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the 4T1 cell.
In Vitro Model	Mammary carcinoma	4T1 cells		CVCL_0125

Experiment 1 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	17 nM
Method Description	Tumor cells (RPMI-7951+p97) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Malignant melanoma	RPMI-7951 cells		CVCL_1666
Experiment 2 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	114 nM
Method Description	Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 3 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	305 nM
Method Description	Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 4 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	780 nM	Moderate MELTF expression (MELTF++)
Method Description	Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 5 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM
Method Description	Tumor cells (RPMI-7951) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Malignant melanoma	RPMI-7951 cells		CVCL_1666

Experiment 1 Reporting the Activity Date of This ADC					[136]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 25 nM	Positive HER2 expression (HER2+++/++)
Method Description	To investigate the cytotoxicity of the unconjugated small-molecule TOP1 inhibitors and ADCs, respective cells were incubated for 4 days (small molecules) and 7 days (ADCs) with increasing concentrations of small molecules (0.015-1,000 nmol/L) and ADCs (0.05-3 ug/mL) to generate a dose-response curve. Killing was analyzed using resazurin cell viability dye at a final concentration of 55 umol/L (Merck) by dividing the fluorescence from control cells in medium by the fluorescence of ADC-treated cells. Fluorescence emission at 590 nmol/L was measured on a microplate reader Infinite 200 Pro (Tecan Group Ltd.).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

Experiment 1 Reporting the Activity Date of This ADC					[148]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	25.6 nM	Low CEACAM5 expression (CEACAM5+)
Method Description	Logarithmically growing cell lines MKN-45, BxPC-3, LS174T, and FCHO were seeded in a 96 well cell culture plate at 5000 cells/well for 12 h. After the culture supernatant was discarded, the 200 uL three-fold diluted UdADC was added to cells, with native antibody B9 and free payload vcMMAE used as control. The concentration of each group started from 1 uM and was repeated in triplicate. Cells were cultured for 72 h at 37 °C, then the culture medium was removed and 100 uL CCK8 solution (10 uL CCK8 + 90 uL medium) was added into each well, using CCK8 solution without cells as reference wells. After cells were incubated at 37 °C for 1-3 h, absorbance was measured at 450 nm using a 96-well microplate reader. Cell viability (%) = [ (ODtreated - ODreference well)/ (ODnon-treated - ODreference well)] × 100%.    Click to Show/Hide
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC					[148]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	38.14 nM	High CEACAM5 expression (CEACAM5 +++)
Method Description	Logarithmically growing cell lines MKN-45, BxPC-3, LS174T, and FCHO were seeded in a 96 well cell culture plate at 5000 cells/well for 12 h. After the culture supernatant was discarded, the 200 uL three-fold diluted UdADC was added to cells, with native antibody B9 and free payload vcMMAE used as control. The concentration of each group started from 1 uM and was repeated in triplicate. Cells were cultured for 72 h at 37 °C, then the culture medium was removed and 100 uL CCK8 solution (10 uL CCK8 + 90 uL medium) was added into each well, using CCK8 solution without cells as reference wells. After cells were incubated at 37 °C for 1-3 h, absorbance was measured at 450 nm using a 96-well microplate reader. Cell viability (%) = [ (ODtreated - ODreference well)/ (ODnon-treated - ODreference well)] × 100%.    Click to Show/Hide
In Vitro Model	Gastric adenocarcinoma	MKN-45 cells		CVCL_0434
Experiment 3 Reporting the Activity Date of This ADC					[148]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	101.4 nM	High CEACAM5 expression (CEACAM5 +++)
Method Description	Logarithmically growing cell lines MKN-45, BxPC-3, LS174T, and FCHO were seeded in a 96 well cell culture plate at 5000 cells/well for 12 h. After the culture supernatant was discarded, the 200 uL three-fold diluted UdADC was added to cells, with native antibody B9 and free payload vcMMAE used as control. The concentration of each group started from 1 uM and was repeated in triplicate. Cells were cultured for 72 h at 37 °C, then the culture medium was removed and 100 uL CCK8 solution (10 uL CCK8 + 90 uL medium) was added into each well, using CCK8 solution without cells as reference wells. After cells were incubated at 37 °C for 1-3 h, absorbance was measured at 450 nm using a 96-well microplate reader. Cell viability (%) = [ (ODtreated - ODreference well)/ (ODnon-treated - ODreference well)] × 100%.    Click to Show/Hide
In Vitro Model	Colon adenocarcinoma	LS174T cells		CVCL_1384

Experiment 1 Reporting the Activity Date of This ADC					[149]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	29.65 Nm
Method Description	A cell line expressing doppel, HCT116, was selected and cultured with increasing concentrations of ADC. After 72 hours, viability of each culture was assessed. ICso values were calculated by logistic non-linear regression and reported as nM.
In Vitro Model	Colon carcinoma	HCT116 cells		CVCL_0291

Experiment 1 Reporting the Activity Date of This ADC					[142]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	34.56 nM	High ROR1 expression ( ROR1 +++)
Method Description	In each ultra-low attachment U bottom 384-well transparent plate patient-derived lung cancer cells AMB-LC-0003T were dispensed in triplicate at 500 cells/well in 40 p1l of M10018 (Aimedbio) media. After centrifugation at 250 g for 2 minutes, reaction was carried out at 37°C and 5% Co 2 for 24 hours. Thereafter, each antibody-drug conjugate was serially diluted 3-fold from 500 nM to 0.314 pM and the cells were treated therewith. The plate was reacted again at 37°C and 5% Co2 for 6 days. After a total of 7 days of reaction, spheroids were formed by the cells in the 384-well plate, so images of spheroids in each well were captured using Operetta CLS (PerkinElmer) according to a high-content screening method. To maintain the spheroid form of the cells in each well, washing was not performed before analysis. The captured images were converted into volume through additional analysis, and the spheroid volume values by concentration were standardized based on the spheroid treated with the lowest concentration of drug. Graphs were created with a log (inhibitor) vs. normalized response - Variable slope using GraphPad Prism 9.3.1, and IC5 o values were obtained.    Click to Show/Hide
In Vitro Model	lung cancer	AMB-LC-0003T cells		Homo sapiens
Experiment 2 Reporting the Activity Date of This ADC					[142]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	165.2 nM	Low ROR1 expression (ROR1+)
Method Description	In each ultra-low attachment U bottom 384-well transparent plate patient-derived lung cancer cells AMB-LC-0003T were dispensed in triplicate at 500 cells/well in 40 p1l of M10018 (Aimedbio) media. After centrifugation at 250 g for 2 minutes, reaction was carried out at 37°C and 5% Co 2 for 24 hours. Thereafter, each antibody-drug conjugate was serially diluted 3-fold from 500 nM to 0.314 pM and the cells were treated therewith. The plate was reacted again at 37°C and 5% Co2 for 6 days. After a total of 7 days of reaction, spheroids were formed by the cells in the 384-well plate, so images of spheroids in each well were captured using Operetta CLS (PerkinElmer) according to a high-content screening method. To maintain the spheroid form of the cells in each well, washing was not performed before analysis. The captured images were converted into volume through additional analysis, and the spheroid volume values by concentration were standardized based on the spheroid treated with the lowest concentration of drug. Graphs were created with a log (inhibitor) vs. normalized response - Variable slope using GraphPad Prism 9.3.1, and IC5 o values were obtained.    Click to Show/Hide
In Vitro Model	lung cancer	AMB-LC-0003T cells		Homo sapiens

Experiment 1 Reporting the Activity Date of This ADC					[149]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	39.32 Nm
Method Description	A cell line expressing doppel, HCT116, was selected and cultured with increasing concentrations of ADC. After 72 hours, viability of each culture was assessed. ICso values were calculated by logistic non-linear regression and reported as nM.
In Vitro Model	Colon carcinoma	HCT116 cells		CVCL_0291

Experiment 1 Reporting the Activity Date of This ADC					[150]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	44.63 nM	Low NECTIN4 expression (NECTIN4+)
Method Description	Cells in the exponential growth phase were harvested and seeded at a density of 4 × 103 cells per well into 96-well plates, followed by overnight incubation. The 96-well plate was filled with gradient dilutions of the NDC along with complete growth medium. Cells were incubated at 37 °C for 96 h. 20 uL of cell counting Kit-8 (Dojindo) was administered to the cells, which were then incubated at 37 °C for 4 h. After shaking the 96-well plates, absorbance was measured at 450 nm using an enzyme marker. Inhibition % = (1 - absorbance of experimental group) / average absorbance of blank group × 100. IC50 values were ascertained by non-linear regression analysis utilizing GraphPad Prism version 8.0.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 2 Reporting the Activity Date of This ADC					[150]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.04 nM	Low NECTIN4 expression (NECTIN4+)
Method Description	Cells in the exponential growth phase were harvested and seeded at a density of 4 × 103 cells per well into 96-well plates, followed by overnight incubation. The 96-well plate was filled with gradient dilutions of the NDC along with complete growth medium. Cells were incubated at 37 °C for 96 h. 20 uL of cell counting Kit-8 (Dojindo) was administered to the cells, which were then incubated at 37 °C for 4 h. After shaking the 96-well plates, absorbance was measured at 450 nm using an enzyme marker. Inhibition % = (1 - absorbance of experimental group) / average absorbance of blank group × 100. IC50 values were ascertained by non-linear regression analysis utilizing GraphPad Prism version 8.0.    Click to Show/Hide
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603

Experiment 1 Reporting the Activity Date of This ADC					[147]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	50.7 nM	Moderate CD276 expression (CD276 ++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-468 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[147]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	125.4 nM	High CD276expression (CD276 +++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the 4T1 cell.
In Vitro Model	Mammary carcinoma	4T1 cells		CVCL_0125
Experiment 3 Reporting the Activity Date of This ADC					[147]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	175 nM	Moderate CD276 expression (CD276 ++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-231 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[151]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	73.56 nM
Method Description	The in vitro antitumor efficacy of BsADC was assessed using the SNU899 cell.
In Vitro Model	Laryngeal squamous cell carcinoma, Squamous cell carcinoma of the larynx	SNU899 cells		CVCL_5105
Experiment 2 Reporting the Activity Date of This ADC					[151]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	115.4 nM
Method Description	The in vitro antitumor efficacy of BsADC was assessed using the SNU46 cell.
In Vitro Model	Laryngeal squamous cell carcinoma, Squamous cell carcinoma of the larynx	SNU46 cells		CVCL_5063

Experiment 1 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Positive HER2 expression (HER2+++/++)
Method Description	SKBR3 8000 cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. For cell viability curves, serially diluted conjugates or naked payloads were added to the cells at final concentrations ranging from 100 nM to 5 pM and incubated for 3 days. To measure viability, cells were incubated with CCK8 (Dojindo) for the final 2 hours and the absorbance at 450 nm (OD450) was determined on a Victor (Perkin Elmer).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[115]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Negative HER2 expression (HER2-)
Method Description	NCI-H1975 8000 cell/well were plated at set initial densities in 96 well flat bottom plates in the appropriate growth media. For cell viability curves, serially diluted conjugates or naked payloads were added to the cells at final concentrations ranging from 100 nM to 5 pM and incubated for 3 days. To measure viability, cells were incubated with CCK8 (Dojindo) for the final 2 hours and the absorbance at 450 nm (OD450) was determined on a Victor (Perkin Elmer).    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511

Experiment 1 Reporting the Activity Date of This ADC					[120]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 nM	Moderate TF expression (TF++)
Method Description	Pancreatic cancer cell lines HPAF-II, BxPC-3, or PSN-1 were harvested on 96-well plates (Corning) and incubated at 37°C overnight. Payloads and ADCs were applied to each well at various concentrations, and the plates were incubated at 37°C for 6 days (n = 3). Cancer cell viability was measured using CCK-8 (Dojindo).
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[152]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	253 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					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM	Moderate MELTF expression (MELTF++)
Method Description	Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 2 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM
Method Description	Tumor cells (RPMI-7951) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Malignant melanoma	RPMI-7951 cells		CVCL_1666
Experiment 3 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM
Method Description	Tumor cells (RPMI-7951+p97) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Malignant melanoma	RPMI-7951 cells		CVCL_1666
Experiment 4 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM
Method Description	Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 5 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM
Method Description	Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527

Experiment 1 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM	Moderate MELTF expression (MELTF++)
Method Description	Tumor cells (A2058) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Melanoma	A2058 cells		CVCL_1059
Experiment 2 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM
Method Description	Tumor cells (RPMI-7951) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Malignant melanoma	RPMI-7951 cells		CVCL_1666
Experiment 3 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM
Method Description	Tumor cells (RPMI-7951+p97) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Malignant melanoma	RPMI-7951 cells		CVCL_1666
Experiment 4 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM
Method Description	Tumor cells (SK-MEL-5) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527
Experiment 5 Reporting the Activity Date of This ADC					[112]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 1000 nM
Method Description	Tumor cells (SK-MEL-28) were incubated with CD228 ADCs for 96-144 hours at 37°C. Cell viability was measured using Cell Titer Glo according to manufacturer'sinstructions.
In Vitro Model	Cutaneous melanoma	SK-MEL-5 cells		CVCL_0527

Experiment 1 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	17 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 2 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3124 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 1 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	18 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 2 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3260 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 1 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	29 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 2 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3674 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 1 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	31 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 2 Reporting the Activity Date of This ADC					[105]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3592 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 1 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	111.1 ng/mL	Moderate Claudin 18.2 expression (Claudin 18.2++)
Method Description	LT-1C8 at 5000 or 10000 cells/well, 0.7mg/ml ADCs were added and incubated for 96 hours, then CCK-8 or Presto-Blue detection reagent was added to each well, and a microplate reader was used for detection and four parameter fitting was carried out.
In Vitro Model	Lung lymphangioleiomyomatosis, Lymphangioleiomyomatosis	LT-1C8 cells		CVCL_8891
Experiment 2 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	155.5 ng/mL	High Claudin 18.2 expression (Claudin 18.2 +++)
Method Description	LI-M11 cells at 5000 cells/well, 0.7mg/ml ADCs were added and incubated for 96 hours, then CCK-8 or Presto-Blue detection reagent was added to each well, and a microplate reader was used for detection and four parameter fitting was carried out.
In Vitro Model	Lung lymphangioleiomyomatosis, Lymphangioleiomyomatosis	LI-M11 cells		CVCL_8891
Experiment 3 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4045 ng/mL	Negative Claudin 18.2 expression (Claudin 18.2-)
Method Description	BxPC-3 at 3000 cells/well, 0.7mg/ml ADCs were added and incubated for 96 hours, then CCK-8 or Presto-Blue detection reagent was added to each well, and a microplate reader was used for detection and four parameter fitting was carried out.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	200.3 ng/mL	High Claudin 18.2 expression (Claudin 18.2 +++)
Method Description	LI-M11 cells at 5000 cells/well, 1.0mg/ml ADCs were added and incubated for 96 hours, then CCK-8 or Presto-Blue detection reagent was added to each well, and a microplate reader was used for detection and four parameter fitting was carried out.
In Vitro Model	Lung lymphangioleiomyomatosis, Lymphangioleiomyomatosis	LI-M11 cells		CVCL_8891
Experiment 2 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	520.5 ng/mL	Moderate Claudin 18.2 expression (Claudin 18.2++)
Method Description	LT-1C8 at 5000 or 10000 cells/well, 1.0mg/ml ADCs were added and incubated for 96 hours, then CCK-8 or Presto-Blue detection reagent was added to each well, and a microplate reader was used for detection and four parameter fitting was carried out.
In Vitro Model	Lung lymphangioleiomyomatosis, Lymphangioleiomyomatosis	LT-1C8 cells		CVCL_8891
Experiment 3 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	5295 ng/mL	Negative Claudin 18.2 expression (Claudin 18.2-)
Method Description	BxPC-3 at 3000 cells/well, 1.0mg/ml ADCs were added and incubated for 96 hours, then CCK-8 or Presto-Blue detection reagent was added to each well, and a microplate reader was used for detection and four parameter fitting was carried out.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[153]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	285 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					[153]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	306 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					[103]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	349.6 ng/mL	High Claudin 18.2 expression (Claudin 18.2 +++)
Method Description	LI-M11 cells at 5000 cells/well, 0.9mg/ml ADCs were added and incubated for 96 hours, then CCK-8 or Presto-Blue detection reagent was added to each well, and a microplate reader was used for detection and four parameter fitting was carried out.
In Vitro Model	Lung lymphangioleiomyomatosis, Lymphangioleiomyomatosis	LI-M11 cells		CVCL_8891
Experiment 2 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	615.1 ng/mL	Moderate Claudin 18.2 expression (Claudin 18.2++)
Method Description	LT-1C8 at 5000 or 10000 cells/well, 0.9mg/ml ADCs were added and incubated for 96 hours, then CCK-8 or Presto-Blue detection reagent was added to each well, and a microplate reader was used for detection and four parameter fitting was carried out.
In Vitro Model	Lung lymphangioleiomyomatosis, Lymphangioleiomyomatosis	LT-1C8 cells		CVCL_8891
Experiment 3 Reporting the Activity Date of This ADC					[103]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4237 ng/mL	Negative Claudin 18.2 expression (Claudin 18.2-)
Method Description	BxPC-3 at 3000 cells/well, 0.9mg/ml ADCs were added and incubated for 96 hours, then CCK-8 or Presto-Blue detection reagent was added to each well, and a microplate reader was used for detection and four parameter fitting was carried out.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[154]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.54 uM	Moderate HER2 expression (HER2++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the BxPc-3 cell.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 2 Reporting the Activity Date of This ADC					[154]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.54 uM	Low HER2 expression (HER2+)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-468 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[154]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.85 uM	Low HER2 expression (HER2+)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-231 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062
Experiment 4 Reporting the Activity Date of This ADC					[154]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3.8 uM	Low HER2 expression (HER2+)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the AsPc1 cell.
In Vitro Model	Pancreatic ductal adenocarcinoma	AsPc1 cells		CVCL_0152
Experiment 5 Reporting the Activity Date of This ADC					[154]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	10.79 uM	Moderate HER2 expression (HER2++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the CFPAC cell.
In Vitro Model	Cystic fibrosis, Pancreatic ductal adenocarcinoma	CFPAC cells		CVCL_1119
Experiment 6 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.01 ug/mL	High EGFR expression (EGFR +++)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 7 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 ug/mL	High EGFR expression (EGFR +++)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 8 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 ug/mL	High EGFR expression (EGFR +++)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 9 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.05 ug/mL	Moderate EGFR expression (EGFR++)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Pancreatic adenocarcinoma	Panc_02_03 cells		CVCL_1633
Experiment 10 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.12 ug/mL	Moderate EGFR expression (EGFR++)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 11 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.18 ug/mL	Negative EGFR expression (EGFR-)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Lung squamous cell carcinoma	NCI-H520 cells		CVCL_1566

Experiment 1 Reporting the Activity Date of This ADC					[147]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	6.9 uM	Moderate CD276 expression (CD276 ++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-468 cell.
In Vitro Model	Mammary carcinoma	4T1 cells		CVCL_0125
Experiment 2 Reporting the Activity Date of This ADC					[147]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	7.7 uM	Moderate CD276 expression (CD276 ++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the MDA-MB-231 cell.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[147]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	13.1 uM	High CD276expression (CD276 +++)
Method Description	The in vitro antitumor efficacy of ADC was assessed using the 4T1 cell.
In Vitro Model	Mammary carcinoma	4T1 cells		CVCL_0125

Experiment 1 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 ug/mL	High HER2 expression (HER2 +++); Moderate EGFR expression (EGFR++)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04 ug/mL	Moderate HER2 expression (HER2++); High EGFR expression (EGFR +++)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 3 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.05 ug/mL	Low HER2 expression (HER2+); High EGFR expression (EGFR +++)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 4 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.05 ug/mL	Moderate HER2 expression (HER2++); High EGFR expression (EGFR +++)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 5 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.29 ug/mL	Low HER2 expression (HER2+); Moderate EGFR expression (EGFR++)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Pancreatic adenocarcinoma	Panc_02_03 cells		CVCL_1633
Experiment 6 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.16 ug/mL	Negative HER2 expression (HER2-); Negative EGFR expression (EGFR-)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Lung squamous cell carcinoma	NCI-H520 cells		CVCL_1566

Experiment 1 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.02 ug/mL	High HER2 expression (HER2 +++)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3.7 ug/mL	Moderate HER2 expression (HER2++)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1650 cells		CVCL_1483
Experiment 3 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	3.93 ug/mL	Moderate HER2 expression (HER2++)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 4 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.73 ug/mL	Low HER2 expression (HER2+)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 5 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	4.91 ug/mL	Low HER2 expression (HER2+)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Pancreatic adenocarcinoma	Panc_02_03 cells		CVCL_1633
Experiment 6 Reporting the Activity Date of This ADC					[155]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	9.12 ug/mL	Negative HER2 expression (HER2-)
Method Description	A-431 was inoculated at 6 × 103 cells/well, NCI-H1650 at 5 × 103 cells/well, SK-OV-3, Panc 02.03, and NCI-H520 at 4 × 103 cells/well, and NCI-H1975 at 3 × 103 cells/well in fresh complete medium and cultured overnight. Antibodies were diluted with a complete medium and added to the cells. The 96-well plates were placed in IncuCyte for incubation and were photographed at 4-h intervals for 4 days under phase conditions. This allowed for the analysis of cell viability by measuring the confluence of the cells in each well.    Click to Show/Hide
In Vitro Model	Lung squamous cell carcinoma	NCI-H520 cells		CVCL_1566

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.6996 ug/ml
Method Description	Series diluted ADCs (maximum concentration: 20 ug/mL, 3-fold dilutions, 10 gradients)were used to treat human lung squamous carcinoma NCI-H226 5000cells cultured in a cellculture plate, and the killing activity was detected after 72 hours of incubation in IncuCyte (Sartorius AG, IncuCytee S3).
In Vitro Model	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	1.138 ug/ml
Method Description	Series diluted ADCs (maximum concentration: 20 ug/mL, 3-fold dilutions, 10 gradients)were used to treat human lung squamous carcinoma NCI-H226 5000cells cultured in a cellculture plate, and the killing activity was detected after 72 hours of incubation in IncuCyte (Sartorius AG, IncuCytee S3).
In Vitro Model	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544

Experiment 1 Reporting the Activity Date of This ADC					[91]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	> 100 ug/ml
Method Description	Series diluted ADCs (maximum concentration: 20 ug/mL, 3-fold dilutions, 10 gradients)were used to treat human lung squamous carcinoma NCI-H226 5000cells cultured in a cellculture plate, and the killing activity was detected after 72 hours of incubation in IncuCyte (Sartorius AG, IncuCytee S3).
In Vitro Model	Pleural epithelioid mesothelioma	NCI-H226 cells		CVCL_1544

Experiment 1 Reporting the Activity Date of This ADC					[156]
Efficacy Data	Half Maximal Effective Concentration (EC50)	61&#1779 pM	Positive HER2 expression (HER2+++/++)
Method Description	Proliferation assays revealed EC50 values in double-digit picomolar range for all constructs on high HER2 expressing cell line SK-BR-3 (Figure 3a, Table 2) which was found to be comparable or significantly lower than for Cp-bearing ADCs found in literature
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[156]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2940&#1771674 pM	Positive HER2 expression (HER2+++/++)
Method Description	Proliferation assays revealed EC50 values in double-digit picomolar range for all constructs on high HER2 expressing cell line SK-BR-3 (Figure 3a, Table 2) which was found to be comparable or significantly lower than for Cp-bearing ADCs found in literature
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077
Experiment 3 Reporting the Activity Date of This ADC					[156]
Efficacy Data	Half Maximal Effective Concentration (EC50)	10370&#1776865 pM	Moderate HER2 expression (HER2++)
Method Description	Proliferation assays revealed EC50 values in double-digit picomolar range for all constructs on high HER2 expressing cell line SK-BR-3 (Figure 3a, Table 2) which was found to be comparable or significantly lower than for Cp-bearing ADCs found in literature
In Vitro Model	Bladder carcinoma	RT112 cells		CVCL_1670

Experiment 1 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.022 nM	High HER2 expression (HER2+++)
Method Description	IC50 (in nM) cell-based assays of tested entities on breast cancer cell lines MDA-MB-231 (HER2-low)
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells (HER2 low)		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Effective Concentration (EC50)	312.1 nM	Low HER2 expression (HER2+)
Method Description	IC50 (in nM) cell-based assays of tested entities on breast cancer cell lines MDA-MB-231 (HER2-low)
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells (HER2 low)		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.029 nM	High HER2 expression (HER2+++)
Method Description	IC50 (in nM) cell-based assays of tested entities on breast cancer cell lines MDA-MB-231 (HER2-low)
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells (HER2 low)		CVCL_0062
Experiment 2 Reporting the Activity Date of This ADC					[157]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Low HER2 expression (HER2+)
Method Description	IC50 (in nM) cell-based assays of tested entities on breast cancer cell lines MDA-MB-231 (HER2-low)
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells (HER2 low)		CVCL_0062

Experiment 1 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.038 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 0.1 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.1 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to BT474-HDR cells under 0.1 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	21.32 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 toBT474-HDR cells under 20 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	42.79 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 20 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.063 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 0.1 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.19 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to BT474-HDR cells under 0.1 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	66.8 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 20 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 4 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	109.1 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 toBT474-HDR cells under 20 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.1 nM	Positive TCRA6 expression (TCRA6+++/++)
Method Description	Cytotoxic effects of aTCRA6 DAR2 and aTCRA6 DAR52-8 ADCs were estimated by exposing Jurkat WT and Jurkat TCRA6 T cells to different ADC concentrations. Cell viability was analyzed 72 h post ADC addition by a fluorometric method using CellTiter-Blue Cell Viability Assay (Promega, Wisconsin, USA) according to the manufacturer's instructions. Briefly, cells were seeded in a 96-well plate (1 × 104 cells/well) with the desired ADC concentrations ranging from 0.06-400 nM (for DAR2 ADC) or 0.005-30 nM (for DAR52-8 ADC) in a serial dilution. After 72 h, redox dye (resazurin) was added to the cells, and the plate was incubated for 3-4 h. Fluorescence of resorufin (560Ex/590Em) was recorded using CLARIOstar plus microplate reader (BMG LABTECH, Offenburg, Germany). Cell proliferation was normalized to untreated control cell fluorescence values. The resulting curves were fitted with a variable slope four-parameter fit, and EC50s were calculated using GraphPad Prism.    Click to Show/Hide
In Vitro Model	Childhood T acute lymphoblastic leukemia, Precursor T-cell acute lymphoblastic leukemia	Jurkat cells (TCRA6+)		CVCL_0065
Experiment 2 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Negative TCRA6 expression (TCRA6-)
Method Description	Cytotoxic effects of aTCRA6 DAR2 and aTCRA6 DAR52-8 ADCs were estimated by exposing Jurkat WT and Jurkat TCRA6 T cells to different ADC concentrations. Cell viability was analyzed 72 h post ADC addition by a fluorometric method using CellTiter-Blue Cell Viability Assay (Promega, Wisconsin, USA) according to the manufacturer's instructions. Briefly, cells were seeded in a 96-well plate (1 × 104 cells/well) with the desired ADC concentrations ranging from 0.06-400 nM (for DAR2 ADC) or 0.005-30 nM (for DAR52-8 ADC) in a serial dilution. After 72 h, redox dye (resazurin) was added to the cells, and the plate was incubated for 3-4 h. Fluorescence of resorufin (560Ex/590Em) was recorded using CLARIOstar plus microplate reader (BMG LABTECH, Offenburg, Germany). Cell proliferation was normalized to untreated control cell fluorescence values. The resulting curves were fitted with a variable slope four-parameter fit, and EC50s were calculated using GraphPad Prism.    Click to Show/Hide
In Vitro Model	Childhood T acute lymphoblastic leukemia, Precursor T-cell acute lymphoblastic leukemia	Jurkat cells (TCRA6-)		CVCL_0065

Experiment 1 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.12 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 0.1 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.34 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to BT474-HDR cells under 0.1 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	6.15 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 toBT474-HDR cells under 20 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	26.65 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 20 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.14 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 0.1 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 2 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.39 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to BT474-HDR cells under 0.1 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 3 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	16.25 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 toBT474-HDR cells under 20 % O2
In Vitro Model	Invasive breast carcinoma of no special type	BT474-HDR cells		CVCL_0179
Experiment 4 Reporting the Activity Date of This ADC					[102]
Efficacy Data	Half Maximal Effective Concentration (EC50)	43.77 nM	High HER2 expression (HER2+++)
Method Description	Cytotoxicity of AZO-ADC-0/4/6/8 to SKOV-3 cells under 20 % O2
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532

Experiment 1 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.2 nM	High HER2 expression (HER2 +++)
Method Description	Cells were seeded in a 96-well white opaque plate at a density of 5 × 103/well (CHO, ATCC, CCL-61) or 1 × 104/well (MCF7 (ATCC, HTB-22), SK-BR-3 (ATCC, HTB-30), SK-OV-3 (ATCC, HTB-77) or JIMT-1 (Beyotime, C6453)). Cells were allowed to attach for 24 h at 37 °C and 5% CO2 in humidified atmosphere. Cells were then treated with serial dilutions of Tra-CAST, Tra-CAST-MMAE and SBA-MMAE or Tra-CASTi, Tra-CASTi-MMAE and DBCO-MMAE for 96 h (BT474, MCF7, SK-BR-3). Cell viability was determined using CellTiter Glo reagents (G7571) and was normalized to the control cells. Data was analyzed by Graphpad software, and the half-maximal effective concentration (EC50) value was calculated by fitting with the log (inhibitor) vs. response module.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.2 nM	High HER2 expression (HER2 +++)
Method Description	Cells were seeded in a 96-well white opaque plate at a density of 5 × 103/well (CHO, ATCC, CCL-61) or 1 × 104/well (MCF7 (ATCC, HTB-22), SK-BR-3 (ATCC, HTB-30), SK-OV-3 (ATCC, HTB-77) or JIMT-1 (Beyotime, C6453)). Cells were allowed to attach for 24 h at 37 °C and 5% CO2 in humidified atmosphere. Cells were then treated with serial dilutions of Tra-CAST, Tra-CAST-MMAE and SBA-MMAE or Tra-CASTi, Tra-CASTi-MMAE and DBCO-MMAE for 96 h (BT474, MCF7, SK-BR-3). Cell viability was determined using CellTiter Glo reagents (G7571) and was normalized to the control cells. Data was analyzed by Graphpad software, and the half-maximal effective concentration (EC50) value was calculated by fitting with the log (inhibitor) vs. response module.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	SKOV-3 cells		CVCL_0532
Experiment 3 Reporting the Activity Date of This ADC					[159]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.7 nM	Positive HER2 expression ( HER2+++/++)
Method Description	Cells were seeded in a 96-well white opaque plate at a density of 5 × 103/well (CHO, ATCC, CCL-61) or 1 × 104/well (MCF7 (ATCC, HTB-22), SK-BR-3 (ATCC, HTB-30), SK-OV-3 (ATCC, HTB-77) or JIMT-1 (Beyotime, C6453)). Cells were allowed to attach for 24 h at 37 °C and 5% CO2 in humidified atmosphere. Cells were then treated with serial dilutions of Tra-CAST, Tra-CAST-MMAE and SBA-MMAE or Tra-CASTi, Tra-CASTi-MMAE and DBCO-MMAE for 96 h (BT474, MCF7, SK-BR-3). Cell viability was determined using CellTiter Glo reagents (G7571) and was normalized to the control cells. Data was analyzed by Graphpad software, and the half-maximal effective concentration (EC50) value was calculated by fitting with the log (inhibitor) vs. response module.    Click to Show/Hide
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

Experiment 1 Reporting the Activity Date of This ADC					[160]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.66 nM
Method Description	Cytotoxic effects of aIgM ADCs were evaluated by exposing IgM+ lymphoma B cells or off-target (IgM-) cells to different ADC concentrations. Cell viability was analyzed 72 h post ADC addition by a colorimetric method using CellTiter 96® AQueous One Solution Cell Proliferation Assay (Promega). Briefly, cells were seeded (1x104 cells/well) in a 96-well plate with the desired antibody concentrations ranging from 0.014-90 nM in a serial dilution. After 72 h, MTS solution was added to the cells and plate was incubated for 2 h. Absorption was measured at 490 nm using CLARIOstar plus microplate reader (BMG LABTECH). Cell proliferation was normalized to untreated control cell absorption values. The resulting curves were fitted with a variable slope four-parameter fit and EC50s were calculated using GraphPad Prism.    Click to Show/Hide
In Vitro Model	Burkitt lymphoma	Ramos cells		CVCL_0597

Experiment 1 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.7 nM	Positive HER2 expression (HER2+++/++)
Method Description	6000 cells/well were seeded in a U bottom 96 well plate in 90 uL of medium (Table S 2) and incubated over night at 37 °C and 5% CO2. Jurkat cells utilized for this assay were derived from mechanism-of-action (MOA)-based bioassay core kit to measure FcGammaRIIIa (V158) function (Promega GmbH, Walldorf, Germany). The next day, 10 uL of a dilution row of each sample was added and cells were incubated for 3 days at 37°C and 5% CO2. To evaluate viability, cellular viability assay was performed utilizing CellTiter-Blue® (Promega GmbH, Walldorf, Germany) following the instructions if the supplier. Fluorescence measurement was conducted with a CLARIOstar Plus (BMG Labtech, Ortenberg, Germany) plate reader. Experiments with SKBR3, A431 and Ramos were conducted in at least two biological replicates with three technical replicates each. Assays on Jurkat cells were performed in technical triplicates.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3 nM	Negative HER2 expression (HER2-)
Method Description	6000 cells/well were seeded in a U bottom 96 well plate in 90 uL of medium (Table S 2) and incubated over night at 37 °C and 5% CO2. Jurkat cells utilized for this assay were derived from mechanism-of-action (MOA)-based bioassay core kit to measure FcGammaRIIIa (V158) function (Promega GmbH, Walldorf, Germany). The next day, 10 uL of a dilution row of each sample was added and cells were incubated for 3 days at 37°C and 5% CO2. To evaluate viability, cellular viability assay was performed utilizing CellTiter-Blue® (Promega GmbH, Walldorf, Germany) following the instructions if the supplier. Fluorescence measurement was conducted with a CLARIOstar Plus (BMG Labtech, Ortenberg, Germany) plate reader. Experiments with SKBR3, A431 and Ramos were conducted in at least two biological replicates with three technical replicates each. Assays on Jurkat cells were performed in technical triplicates.    Click to Show/Hide
In Vitro Model	Adenocarcinoma of the rat mammary gland	Jurkat Fc-GammaIIIa++ cells		CVCL_3475
Experiment 3 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Half Maximal Effective Concentration (EC50)	5.5 nM	Low HER2 expression (HER2+)
Method Description	6000 cells/well were seeded in a U bottom 96 well plate in 90 uL of medium (Table S 2) and incubated over night at 37 °C and 5% CO2. Jurkat cells utilized for this assay were derived from mechanism-of-action (MOA)-based bioassay core kit to measure FcGammaRIIIa (V158) function (Promega GmbH, Walldorf, Germany). The next day, 10 uL of a dilution row of each sample was added and cells were incubated for 3 days at 37°C and 5% CO2. To evaluate viability, cellular viability assay was performed utilizing CellTiter-Blue® (Promega GmbH, Walldorf, Germany) following the instructions if the supplier. Fluorescence measurement was conducted with a CLARIOstar Plus (BMG Labtech, Ortenberg, Germany) plate reader. Experiments with SKBR3, A431 and Ramos were conducted in at least two biological replicates with three technical replicates each. Assays on Jurkat cells were performed in technical triplicates.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Half Maximal Effective Concentration (EC50)	2 nM	Positive HER2 expression (HER2+++/++)
Method Description	6000 cells/well were seeded in a U bottom 96 well plate in 90 uL of medium (Table S 2) and incubated over night at 37 °C and 5% CO2. Jurkat cells utilized for this assay were derived from mechanism-of-action (MOA)-based bioassay core kit to measure FcGammaRIIIa (V158) function (Promega GmbH, Walldorf, Germany). The next day, 10 uL of a dilution row of each sample was added and cells were incubated for 3 days at 37°C and 5% CO2. To evaluate viability, cellular viability assay was performed utilizing CellTiter-Blue® (Promega GmbH, Walldorf, Germany) following the instructions if the supplier. Fluorescence measurement was conducted with a CLARIOstar Plus (BMG Labtech, Ortenberg, Germany) plate reader. Experiments with SKBR3, A431 and Ramos were conducted in at least two biological replicates with three technical replicates each. Assays on Jurkat cells were performed in technical triplicates.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Half Maximal Effective Concentration (EC50)	7.2 nM	Low HER2 expression (HER2+)
Method Description	6000 cells/well were seeded in a U bottom 96 well plate in 90 uL of medium (Table S 2) and incubated over night at 37 °C and 5% CO2. Jurkat cells utilized for this assay were derived from mechanism-of-action (MOA)-based bioassay core kit to measure FcGammaRIIIa (V158) function (Promega GmbH, Walldorf, Germany). The next day, 10 uL of a dilution row of each sample was added and cells were incubated for 3 days at 37°C and 5% CO2. To evaluate viability, cellular viability assay was performed utilizing CellTiter-Blue® (Promega GmbH, Walldorf, Germany) following the instructions if the supplier. Fluorescence measurement was conducted with a CLARIOstar Plus (BMG Labtech, Ortenberg, Germany) plate reader. Experiments with SKBR3, A431 and Ramos were conducted in at least two biological replicates with three technical replicates each. Assays on Jurkat cells were performed in technical triplicates.    Click to Show/Hide
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[161]
Efficacy Data	Half Maximal Effective Concentration (EC50)	7.6 nM	Negative HER2 expression (HER2-)
Method Description	6000 cells/well were seeded in a U bottom 96 well plate in 90 uL of medium (Table S 2) and incubated over night at 37 °C and 5% CO2. Jurkat cells utilized for this assay were derived from mechanism-of-action (MOA)-based bioassay core kit to measure FcGammaRIIIa (V158) function (Promega GmbH, Walldorf, Germany). The next day, 10 uL of a dilution row of each sample was added and cells were incubated for 3 days at 37°C and 5% CO2. To evaluate viability, cellular viability assay was performed utilizing CellTiter-Blue® (Promega GmbH, Walldorf, Germany) following the instructions if the supplier. Fluorescence measurement was conducted with a CLARIOstar Plus (BMG Labtech, Ortenberg, Germany) plate reader. Experiments with SKBR3, A431 and Ramos were conducted in at least two biological replicates with three technical replicates each. Assays on Jurkat cells were performed in technical triplicates.    Click to Show/Hide
In Vitro Model	Adenocarcinoma of the rat mammary gland	Jurkat Fc-GammaIIIa++ cells		CVCL_3475

Experiment 1 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Half Maximal Effective Concentration (EC50)	3.6 nM	Positive TCRA6 expression (TCRA6+++/++)
Method Description	Cytotoxic effects of aTCRA6 DAR2 and aTCRA6 DAR52-8 ADCs were estimated by exposing Jurkat WT and Jurkat TCRA6 T cells to different ADC concentrations. Cell viability was analyzed 72 h post ADC addition by a fluorometric method using CellTiter-Blue Cell Viability Assay (Promega, Wisconsin, USA) according to the manufacturer's instructions. Briefly, cells were seeded in a 96-well plate (1 × 104 cells/well) with the desired ADC concentrations ranging from 0.06-400 nM (for DAR2 ADC) or 0.005-30 nM (for DAR52-8 ADC) in a serial dilution. After 72 h, redox dye (resazurin) was added to the cells, and the plate was incubated for 3-4 h. Fluorescence of resorufin (560Ex/590Em) was recorded using CLARIOstar plus microplate reader (BMG LABTECH, Offenburg, Germany). Cell proliferation was normalized to untreated control cell fluorescence values. The resulting curves were fitted with a variable slope four-parameter fit, and EC50s were calculated using GraphPad Prism.    Click to Show/Hide
In Vitro Model	Childhood T acute lymphoblastic leukemia, Precursor T-cell acute lymphoblastic leukemia	Jurkat cells (TCRA6+)		CVCL_0065
Experiment 2 Reporting the Activity Date of This ADC					[158]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 100 nM	Negative TCRA6 expression (TCRA6-)
Method Description	Cytotoxic effects of aTCRA6 DAR2 and aTCRA6 DAR52-8 ADCs were estimated by exposing Jurkat WT and Jurkat TCRA6 T cells to different ADC concentrations. Cell viability was analyzed 72 h post ADC addition by a fluorometric method using CellTiter-Blue Cell Viability Assay (Promega, Wisconsin, USA) according to the manufacturer's instructions. Briefly, cells were seeded in a 96-well plate (1 × 104 cells/well) with the desired ADC concentrations ranging from 0.06-400 nM (for DAR2 ADC) or 0.005-30 nM (for DAR52-8 ADC) in a serial dilution. After 72 h, redox dye (resazurin) was added to the cells, and the plate was incubated for 3-4 h. Fluorescence of resorufin (560Ex/590Em) was recorded using CLARIOstar plus microplate reader (BMG LABTECH, Offenburg, Germany). Cell proliferation was normalized to untreated control cell fluorescence values. The resulting curves were fitted with a variable slope four-parameter fit, and EC50s were calculated using GraphPad Prism.    Click to Show/Hide
In Vitro Model	Childhood T acute lymphoblastic leukemia, Precursor T-cell acute lymphoblastic leukemia	Jurkat cells (TCRA6-)		CVCL_0065

Experiment 1 Reporting the Activity Date of This ADC					[162]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	Ntera-2 cell at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.    Click to Show/Hide
In Vitro Model	Embryonal carcinoma	Ntera-2 cells		CVCL_0034
Experiment 2 Reporting the Activity Date of This ADC					[162]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 nM	Negative ROR1 expression (ROR1-)
Method Description	MCF-7 cells at 625 cells/25 pL were seeded in a 384-well plat. ADCs were formulated at 2x starting concentration. Filter sterilized samples were serial diluted (1:3) under sterile conditions and added onto cells in triplicates. For cell viability measurement, 30 microliter of Cell Titer-Glo@ reagent (Promega Corp, Madison, WI) was added into each well, and plates processed as per product instructions.    Click to Show/Hide
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 nM	Negative ROR1 expression (ROR1-)
Method Description	The cell killing EC5o and Span for RORI ADCs conjugated to different linker warheads at different DARs on RORI positive Ntera-2 cell and RORI negative MCF-7 cells
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[163]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10 nM	Positive ROR1 expression (ROR1+++/++)
Method Description	The cell killing EC5o and Span for RORI ADCs conjugated to different linker warheads at different DARs on RORI positive Ntera-2 cell and RORI negative MCF-7 cells
In Vitro Model	Embryonal carcinoma	Ntera-2 cells		CVCL_0034

Experiment 1 Reporting the Activity Date of This ADC					[164]
Efficacy Data	Half Maximal Effective Concentration (EC50)	575.8 nM	High FAP expression (+++)
Method Description	the half-maximal inhibitory concentration (IC50) of NAPC-ADC against 4T1-FAP cells
In Vitro Model	Malignant neoplasms of the mouse mammary gland	4T1-FAP cells		CVCL_0125

Experiment 1 Reporting the Activity Date of This ADC					[165]
Efficacy Data	Partial Response (PR)	15.90 33.30 %
Patients Enrolled	Patients with platinum-resistant ovarian cancer (OC), metastatic triple negative breast cancer (TNBC) and received median 3 prior regimens.
Administration Dosage	0.15, 0.17, 0.18 mg/kg day1 and day15; q28d.
Related Clinical Trial
NCT Number	NCT04740398	Phase Status	Phase 1
Clinical Description	A phase 1a/1b, open-label, multi-center, first in human and expansion study to assess the safety, tolerance, and pharmacokinetics of the novel antitumor agent CBP-1008 in patients with advanced solid tumors.