Antibody ID	ANI0GYJQM
Antibody Name	Cetuximab
Brand Name	ERBITUX
Organization	Bristol-Myers Squibb; Merck & Co., Inc.
Indication	Colorectal cancer; Head and neck squamous cell carcinoma; Esophageal cancer
Approval Date	Feb. 2004
Synonyms	Fab C225; IMC-225; ABP-494; C225; C-225; CETUXIMAB CETUXIMAB BIOSIMILAR (ABP-494); CETUXIMAB (GENETICAL RECOMBINATION); CMAB009; CMAB-009; IMC-C225; MOAB C225    Click to Show/Hide
Antibody Type	Monoclonal antibody (mAb)
Antibody Subtype	Chimeric IgG1-kappa
Antigen Name	Epidermal growth factor receptor (EGFR)					Antigen Info
ChEMBI ID	CHEMBL1201577
PDB ID	1yy8 , 1yy9 , 4gw1 , 4gw5 , 4kro , 4krp , 5esq , 5hpm , 5hyq , 5icx , 5icy , 5icz , 5id0 , 5id1
DrugBank ID	DB00002
Drug Central ID	4954
Click to Show/Hide the Sequence Information of This Antibody
Heavy Chain Sequence	QVQLKQSGPGLVQPSQSLSITCTVSGFSLTNYGVHWVRQSPGKGLEWLGVIWSGGNTDYN TPFTSRLSINKDNSKSQVFFKMNSLQSNDTAIYYCARALTYYDYEFAYWGQGTLVTVSAA STKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSSG LYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRVEPKSPKSCDKTHTCPPCPAPELL GGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQ YNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSR DELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKS RWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK     Click to Show/Hide
Heavy Chain Varible Domain	QVQLKQSGPGLVQPSQSLSITCTVSGFSLTNYGVHWVRQSPGKGLEWLGVIWSGGNTDYN TPFTSRLSINKDNSKSQVFFKMNSLQSNDTAIYYCARALTYYDYEFAYWGQGTLVTVSA     Click to Show/Hide
Heavy Chain Constant Domain 1	ASTKGPSVFPLAPSSKSTSGGTAALGCLVKDYFPEPVTVSWNSGALTSGVHTFPAVLQSS GLYSLSSVVTVPSSSLGTQTYICNVNHKPSNTKVDKRV     Click to Show/Hide
Heavy Chain Constant Domain 2	APELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTK PREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAK     Click to Show/Hide
Heavy Chain Constant Domain 3	GQPREPQVYTLPPSREEMTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDS DGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK     Click to Show/Hide
Heavy Chain Hinge Region	EPKSCDKTHTCPPCP     Click to Show/Hide
Heavy Chain CDR 1	GFSLTNYG     Click to Show/Hide
Heavy Chain CDR 2	IWSGGNT     Click to Show/Hide
Heavy Chain CDR 3	ARALTYYDYEFAY     Click to Show/Hide
Light Chain Sequence	DILLTQSPVILSVSPGERVSFSCRASQSIGTNIHWYQQRTNGSPRLLIKYASESISGIPS RFSGSGSGTDFTLSINSVESEDIADYYCQQNNNWPTTFGAGTKLELKRTVAAPSVFIFPP SDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQDSKDSTYSLSSTLT LSKADYEKHKVYACEVTHQGLSSPVTKSFNRGA     Click to Show/Hide
Light Chain Varible Domain	DILLTQSPVILSVSPGERVSFSCRASQSIGTNIHWYQQRTNGSPRLLIKYASESISGIPS RFSGSGSGTDFTLSINSVESEDIADYYCQQNNNWPTTFGAGTKLELK     Click to Show/Hide
Light Chain Constant Domain	RTVAAPSVFIFPPSDEQLKSGTASVVCLLNNFYPREAKVQWKVDNALQSGNSQESVTEQD SKDSTYSLSSTLTLSKADYEKHKVYACEVTHQGLSSPVTKSFNRGEC     Click to Show/Hide
Light Chain CDR 1	QSIGTN     Click to Show/Hide
Light Chain CDR 2	YAS     Click to Show/Hide
Light Chain CDR 3	QQNNNWPTT     Click to Show/Hide

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 72.17%	Positive EGFR expression (EGFR +++/++)
Method Description	When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
In Vivo Model	Lung adenocarcinoma PDX model (PDX: PDX1)
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 91.89%	Positive EGFR expression (EGFR +++/++)
Method Description	When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
In Vivo Model	Lung adenocarcinoma PDX model (PDX: PDX1)

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 12.39%	Negative EGFR expression (EGFR -)
Method Description	When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
In Vivo Model	H520 CDX model
In Vitro Model	Lung squamous cell carcinoma	NCI-H520 cells		CVCL_1566
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 64%	Positive EGFR expression (EGFR +++/++)
Method Description	When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 93.80%	Positive EGFR expression (EGFR +++/++)
Method Description	When subcutaneous xenograft tumors reached 1.5 cm3, they were serially passaged in NSG mice by subcutaneous transplant (0.10-0.12 g, 2x2 mm) under general anesthesia. Mouse treatment was performed by intraperitoneal injection of vehicle (PBS), 50 mg/kg Cet-TPL in <300 uL PBS twice/week for about 2-3 weeks.
In Vivo Model	SCC6 CDX model
In Vitro Model	Squamous cell carcinoma	UM-SCC-6 cells		CVCL_7773

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6.25 ug/mL - 12.50 ug/mL ug/mL	Positive EGFR expression (EGFR +++/++)
Method Description	For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
In Vitro Model	Squamous cell carcinoma	UM-SCC-6 cells		CVCL_7773
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.5 ug/mL	Positive EGFR expression (EGFR +++/++)
Method Description	For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
In Vitro Model	Lung large cell carcinoma	NCI-H1299 cells		CVCL_0060
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	12.5 ug/mL	Positive EGFR expression (EGFR +++/++)
Method Description	For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 4 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 ug/mL	Negative EGFR expression (EGFR -)
Method Description	For proliferation assay, cells were seeded in 96-well plates in four to six replicates at densities of 2000 cells per well; after 24 h, 3.125-100 ug/mL IgG, Cet, and Cet-TPL were added to wells, respectively, and further incubated with cells for 72 h.
In Vitro Model	Lung squamous cell carcinoma	NCI-H520 cells		CVCL_1566

Experiment 1 Reporting the Activity Date of This ADC					[2]
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					[2]
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					[2]
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					[2]
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					[2]
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					[2]
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					[2]
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					[2]
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					[3]
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					[3]
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					[3]
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					[3]
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					[3]
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					[3]
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					[3]
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					[3]
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					[3]
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					[3]
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					[3]
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					[3]
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					[3]
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					[3]
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					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 42.79%	High EGFR expression (EGFR+++)
Method Description	The inhibitory activity of Cetuximab-(FGX16-11) 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	Colon cancer CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 2 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.01%	High EGFR expression (EGFR+++)
Method Description	The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 5 mg/kg.
In Vivo Model	Colon cancer CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 3 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 92.22%	High EGFR expression (EGFR+++)
Method Description	The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 10 mg/kg.
In Vivo Model	Colon cancer CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 4 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 99.98%	High EGFR expression (EGFR+++)
Method Description	The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 20 mg/kg.
In Vivo Model	Colon cancer CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724
Experiment 5 Reporting the Activity Date of This ADC					[4]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High EGFR expression (EGFR+++)
Method Description	The inhibitory activity of Cetuximab-(FGX16-11) against cancer cell growth was evaluated in various human cancer cell lines in vivo. The cells were treated with 40 mg/kg.
In Vivo Model	Colon cancer CDX model
In Vitro Model	Colon adenocarcinoma	SW48 cells		CVCL_1724

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 84.20%	Positive EGFR expression (EGFR+++/++)
Method Description	MMAU ADCs (3 mg/kg, intravenously four times at seven day intervals) induces efficient tumor cell killing in cell line-derived models of HSC-2 cells with EGFR expression with high expression.
In Vivo Model	HSC-2 CDX model
In Vitro Model	Oral cavity squamous cell carcinoma	HSC-2 cells		CVCL_1287
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 86.30%	Positive EGFR expression (EGFR+++/++)
Method Description	MMAU ADCs (10 mg/kg, intravenously four times at seven day intervals) induces efficient tumor cell killing in cell line-derived models of HSC-2 cells with EGFR expression with high expression.
In Vivo Model	HSC-2 CDX model
In Vitro Model	Oral cavity squamous cell carcinoma	HSC-2 cells		CVCL_1287

Experiment 1 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	25 pM	Low EGFR expression (EGFR+)
Method Description	Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO2 for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model	Non-small cell lung carcinoma	NCI-H522 cells		CVCL_1567
Experiment 2 Reporting the Activity Date of This ADC					[5]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	30 pM	High EGFR expression (EGFR+++)
Method Description	Cells were seeded in a culture-treated 96-well clear plate and incubated at 37°C under 5% CO2 for 24h. Serially diluted samples (50L) were added to each well and the plate was incubated at 37°C for 72h.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 85%	Positive EGFR expression (EGFR +++/++)
Method Description	Mice were injected intraperitoneally with 3 mg/kg of ITcetuximab, and 2days later,2 h after the administration of NPe6 (5 mg/kg) via the tail vein, the tumors were irradiated with a 664 nm laser at a dose of 30 J/cm2 from the diode laser unit.
In Vivo Model	A549 CDX model
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023

Experiment 1 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.36 nM	High EGFR expression (EGFR +++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 was evaluated from the sigmoid curve obtained using the curvefitting tool of the ImageJ software.
In Vitro Model	Skin squamous cell carcinoma	A-431 cells		CVCL_0037
Experiment 2 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.77 nM	Positive EGFR expression (EGFR +++/++)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 was evaluated from the sigmoid curve obtained using the curvefitting tool of the ImageJ software.
In Vitro Model	Lung adenocarcinoma	A-549 cells		CVCL_0023
Experiment 3 Reporting the Activity Date of This ADC					[6]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 nM	Low EGFR expression (EGFR +)
Method Description	Cancer cell lines were incubated with compounds for 72 h. IC50 was evaluated from the sigmoid curve obtained using the curvefitting tool of the ImageJ software.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Tumor Growth Inhibition value (TGI)	90.30%	High EGFR expression (EGFR+++)
Method Description	To test the effect of STING ADCs in vivo, we used a mouse tumor model in which the C57BL/6J mice were implanted subcutaneously with B16F10 melanoma cells stably expressing human EGFR (B16-EGFR). After the tumors grew to ~100 mm 3 , STING ADCs were administered to the mice through intraperitoneal injection three times (200 g each time on day 5, 8, and 11 after tumor cell inoculation).    Click to Show/Hide
In Vivo Model	Melanoma CDX model
In Vitro Model	Mouse melanoma	B16-F10 cells		CVCL_0159

Experiment 1 Reporting the Activity Date of This ADC					[7]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10 uM	Negative EGFR expression (EGFR-)
Method Description	Serial dilutions of IMSA172 or its conjugates with the indicated antibodies (ADCs) were incubated with THP1-ISG-Luc or this cell line stably expressing human EGFR (THP1-ISG-luc-EGFR; B and D) for 16 h, and the interferon response was measured by luciferase assay.
In Vitro Model	Acute monocytic leukemia	THP1-Lucia ISG cells		CVCL_X587

Experiment 1 Reporting the Activity Date of This ADC					[8]
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					[8]
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					[8]
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					[8]
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					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.66 pM	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	Biphasic synovial sarcoma	Aska-SS cells		CVCL_6C43
Experiment 2 Reporting the Activity Date of This ADC					[9]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	10.57 pM	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	Monophasic synovial sarcoma	HS-SY-2 cells		CVCL_8719

Experiment 1 Reporting the Activity Date of This ADC					[10]
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 1 Reporting the Activity Date of This ADC					[11]
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					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 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					[12]
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					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.11 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					[13]
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					[12]
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					[12]
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					[13]
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					[13]
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					[14]
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					[14]
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					[19]
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					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.47 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					[12]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.3 nM	High 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	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[12]
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					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.47 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					[13]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.3 nM	High 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	Skin squamous cell carcinoma	A431 cells		CVCL_0037
Experiment 3 Reporting the Activity Date of This ADC					[13]
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					[2]
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					[2]
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					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.85 nM	High EGFR expression (EGFR+++/++)
Method Description	HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model	HCC1954/TDR CDX model (CDX: C#19)
In Vitro Model	Breast ductal carcinoma	HCC1954 T-DM1R (T-DM1 resistance) cells		CVCL_1259
Experiment 2 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.85 nM	High EGFR expression (EGFR+++/++)
Method Description	HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model	HCC1954/TDR CDX model (CDX: C#10)
In Vitro Model	Breast ductal carcinoma	HCC1954 T-DM1R (T-DM1 resistance) cells		CVCL_1259
Experiment 3 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	1.41 nM	High EGFR expression (EGFR+++/++)
Method Description	HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vitro Model	Breast ductal carcinoma	HCC1954 cells		CVCL_1259
Experiment 4 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3.52 nM	High EGFR expression (EGFR+++/++)
Method Description	HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model	HCC1954/TDR CDX model (CDX: C#20)
In Vitro Model	Breast ductal carcinoma	HCC1954 T-DM1R (T-DM1 resistance) cells		CVCL_1259
Experiment 5 Reporting the Activity Date of This ADC					[15]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	7.68 nM	High EGFR expression (EGFR+++/++)
Method Description	HCC1954 cells (20,000) were plated in 150 mm dishes and treated with 1 nM T-DM1 (media replaced weekly). Resistant HCC1954 T-DM1R clones (HCC-TDM1R#) were obtained by single-cell cloning and continuously cultured in the presence of 1 nM T-DM1 for a total period of 5 months.
In Vivo Model	HCC1954/TDR CDX model (CDX: C#29)
In Vitro Model	Breast ductal carcinoma	HCC1954 T-DM1R (T-DM1 resistance) cells		CVCL_1259

Experiment 1 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.11 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179
Experiment 2 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	5.02 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	4.15 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the MDA-MB-468 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[16]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	8.54 nM	Positive HER2 expression (EPHA2+++/++)
Method Description	Potency of compounds and ADCs was evaluated using the BT474 cells. Cells were plated in a 96-well flat bottom tissue culture-treated clear polystyrene plate at ~100,000 cells per well in 200 uL with the indicated concentration of the compound or ADC.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

Experiment 1 Reporting the Activity Date of This ADC					[17]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	27.7 nM	Positive EGFR expression (EGFR +++/++)
Method Description	Cells were treated with different concentrations of drugs for 72 h. The viability was determined using the MTT assay.
In Vitro Model	Colon carcinoma	GEO cells (Cetuximab-resistant)		CVCL_0271

Experiment 1 Reporting the Activity Date of This ADC					[18]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	37.42 ug/mL	High EGFR expression (EGFR+++)
Method Description	Cells were seeded into 6-well plates, 500,000 cells/well. One day (24 hours) before treatment, MDA-MB-231 cells are being fasted from FBS. Cells are divided into five different doses of conjugate (5 ug/mL; 10 ug/mL; 20 ug/mL; 40 ug/mL; 80 ug/mL) and one untreated group. They were incubated for 48 hours.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Effective Concentration (EC50)	11.56 ng/mL	Positive EGFR expression (EGFR +++/++)
Method Description	Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Esophageal squamous cell carcinoma	KYSE-520 cells		CVCL_1355

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Effective Concentration (EC50)	18.17 ng/mL	Positive EGFR expression (EGFR +++/++)
Method Description	Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Esophageal squamous cell carcinoma	KYSE-520 cells		CVCL_1355

Experiment 1 Reporting the Activity Date of This ADC					[20]
Efficacy Data	Half Maximal Effective Concentration (EC50)	29.21 ng/mL	Positive EGFR expression (EGFR +++/++)
Method Description	Conjugate in various concentrations was added to cells in a 96 well plate at 1,000 cells per well in 100 pL in complete RPMI medium.
In Vitro Model	Esophageal squamous cell carcinoma	KYSE-520 cells		CVCL_1355

Experiment 1 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.04 nM	Low MUC1 expression (MUC1+);Low EGFR expression (EGFR+)
Method Description	A total of 625 cells (NCI-H292) were plated in 90 ul cell culture medium per well of a 96-well black/clear flat bottom TC-treated imaging microplate and cultured overnight. A ten-fold starting concentration of ADCs, a respective serial dilution (1:4) were prepared in cell culture medium briefly before use. Wells were supplied with 10 ul ADC or compound solution. Treatment was performed in technical triplicates. The plates were subsequently incubated for 144h. For subsequent cell viability measurement, 100 ul Cell Titer-Glo reagent was pipetted in each well, and plates were further processed according the manufacturer's instructions.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511
Experiment 2 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.06 nM	Low MUC1 expression (MUC1+);High EGFR expression (EGFR+++)
Method Description	A total of 625 cells (NCI-H292) were plated in 90 ul cell culture medium per well of a 96-well black/clear flat bottom TC-treated imaging microplate and cultured overnight. A ten-fold starting concentration of ADCs, a respective serial dilution (1:4) were prepared in cell culture medium briefly before use. Wells were supplied with 10 ul ADC or compound solution. Treatment was performed in technical triplicates. The plates were subsequently incubated for 144h. For subsequent cell viability measurement, 100 ul Cell Titer-Glo reagent was pipetted in each well, and plates were further processed according the manufacturer's instructions.    Click to Show/Hide
In Vitro Model	Lung adenocarcinoma	HCC827 cells		CVCL_2063
Experiment 3 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.13 nM	Moderate MUC1 expression (MUC1++);Low EGFR expression (EGFR+)
Method Description	A total of 625 cells (OVCAR-3) in a volume of 25 uL were seeded in a 384-well flat bottom white polystyrene plate the day before the actual assay started. ADC and free drugs were formulated at 2x starting concentration in cell culture medium and filtered through 0.22um cellulose acetate filtered 2 ml centrifuge tubes. Filter sterilized samples were serial diluted (1:3) under sterile conditions and 25 uL of each dilution was added onto cells in triplicates. Plates were cultured at 37 °C in a C02 incubator for 120 hours. For cell viability measurement, 30 uL of Cell Titer-Glo@ reagent (PromegaT M Corp, Madison, WI) was added into each well, and plates processed as per product instructions. Relative luminescence was measured.    Click to Show/Hide
In Vitro Model	Ovarian serous adenocarcinoma	OVCAR-3 cells		CVCL_0465
Experiment 4 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.15 nM	Low MUC1 expression (MUC1+);High EGFR expression (EGFR+++)
Method Description	A total of 625 cells (MDA-MB-468) in a volume of 25 uL were seeded in a 384-well flat bottom white polystyrene plate the day before the actual assay started. ADC and free drugs were formulated at 2x starting concentration in cell culture medium and filtered through 0.22um cellulose acetate filtered 2 ml centrifuge tubes. Filter sterilized samples were serial diluted (1:3) under sterile conditions and 25 uL of each dilution was added onto cells in triplicates. Plates were cultured at 37 °C in a C02 incubator for 120 hours. For cell viability measurement, 30 uL of Cell Titer-Glo@ reagent (PromegaT M Corp, Madison, WI) was added into each well, and plates processed as per product instructions. Relative luminescence was measured.    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 5 Reporting the Activity Date of This ADC					[21]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.17 nM	Low MUC1 expression (MUC1+);Moderate EGFR expression (EGFR++)
Method Description	A total of 625 cells (NCI-H292) were plated in 90 ul cell culture medium per well of a 96-well black/clear flat bottom TC-treated imaging microplate and cultured overnight. A ten-fold starting concentration of ADCs, a respective serial dilution (1:4) were prepared in cell culture medium briefly before use. Wells were supplied with 10 ul ADC or compound solution. Treatment was performed in technical triplicates. The plates were subsequently incubated for 144h. For subsequent cell viability measurement, 100 ul Cell Titer-Glo reagent was pipetted in each well, and plates were further processed according the manufacturer's instructions.    Click to Show/Hide
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455

Experiment 1 Reporting the Activity Date of This ADC					[22]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.79 nM	Low HER2 expression (HER2+)
Method Description	To measure cell viability, 5,000 cells per well were plated in 96-well plates and incubated with cetuximab, isotype ADC, ADC, or free inhibitor for 96 hours at 37°C. Cell viabilities were detected by CellTiter 96 AQueous One Solution Cell Proliferation Assay (Promega) according to the manufacturer's instructions. Optical absorbance was read on a FLUOstar Omega spectrophotometer (BMG Labtech; RRID:SCR_025024).    Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.00149 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0104 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.00183 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	1.35 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.00204 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	3.06 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0028 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.386 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.00317 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	4.83 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.00466 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.00669 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.00488 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.158 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.00542 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	1.5 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.00724 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0295 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.00776 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0671 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.00904 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.104 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0113 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.372 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0151 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.122 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0152 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.358 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0169 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	2.56 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0205 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.31 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0236 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0908 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0239 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	1.45 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0421 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.251 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0479 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	97.5 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0499 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	6.84-08 M	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0621 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	44.9 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0669 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.175 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0769 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.116 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0791 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	500 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0913 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.163 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.0922 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	10.9 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.1 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	15.4 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.109 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.716 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.127 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.132 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.142 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.957 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.218 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	500 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.241 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	9.19 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.247 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	56.9 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.295 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	500 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	0.603 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	500 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	1.15 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 2 Reporting the Activity Date of This ADC					[23]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)Human PBMC	26.6 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Tables 1b and 1c below set out the IC50 values for representative working examples from this assay
In Vitro Model	Liver and intrahepatic bile duct epithelial neoplasm	SK-HEP-1 cells		CVCL_0525

Experiment 1 Reporting the Activity Date of This ADC					[24]
Efficacy Data	Half Maximal inhibitory Concentration (IC50)	0.027 nM	Positive CD30 expression (CD30+++/++)
Method Description	Karpas-299 cells (ECACC), which are CD30 antigen-positiveand HER2 antigen-negative,were cultured in RPMI 1640 (GIBCO)containing 30%fetal bovine serum (MP Biomedicals) (hereinafter,referred to as "culture medium A" in this test).
In Vitro Model	ALK-positive anaplastic large cell lymphoma	Karpas-299 cells		CVCL_1324

Ref 1	Cetuximab-Triptolide Conjugate Suppresses the Growth of EGFR-Overexpressing Lung Cancers through Targeting RNA Polymerase II. Mol Ther Oncolytics. 2020 Jul 6;18:304-316. doi: 10.1016/j.omto.2020.07.001. eCollection 2020 Sep 25.
Ref 2	Divinylsulfonamides enable the construction of homogeneous antibody-drug conjugates. Bioorg Med Chem. 2020 Dec 1;28(23):115793. doi: 10.1016/j.bmc.2020.115793. Epub 2020 Oct 6.
Ref 3	Two engineered site-specific antibody-drug conjugates, HLmD4 and HLvM4, have potent therapeutic activity in two DLL4-positive tumour xenograft models. Am J Cancer Res. 2020 Aug 1;10(8):2387-2408. eCollection 2020.
Ref 4	DNA sequence-selective G-A cross-linking ADC payloads for use in solid tumour therapies. Commun Biol. 2022 Jul 29;5(1):741.
Ref 5	Hydrophilic Auristatin Glycoside Payload Enables Improved Antibody-Drug Conjugate Efficacy and Biocompatibility. Antibodies (Basel). 2018 Mar 22;7(2):15. doi: 10.3390/antib7020015.
Ref 6	Development of a new minimally invasive phototherapy for lung cancer using antibody-toxin conjugate. Thorac Cancer. 2023 Mar;14(7):645-653. doi: 10.1111/1759-7714.14776. Epub 2023 Jan 19.
Ref 7	Tumor-targeted delivery of a STING agonist improvescancer immunotherapy. Proc Natl Acad Sci U S A. 2022 Dec 6;119(49):e2214278119.
Ref 8	Balancing Selectivity and Efficacy of Bispecific Epidermal Growth Factor Receptor (EGFR) c-MET Antibodies and Antibody-Drug Conjugates. J Biol Chem. 2016 Nov 25;291(48):25106-25119. doi: 10.1074/jbc.M116.753491. Epub 2016 Sep 30.
Ref 9	Neodegrader conjugates; 2021-10-07.
Ref 10	MAbs. 2023 Jan-Dec;15(1):2149057. doi: 10.1080/19420862.2022.2149057.
Ref 11	Radiation Cleaved Drug-Conjugate Linkers Enable Local Payload Release. Bioconjug Chem. 2022 Aug 17;33(8):1474-1484.
Ref 12	Conjugates comprising self-immolative groups and methods related thereto.
Ref 13	Antibody-drug conjugates comprising branched linkers and methods related thereto; 2017-06-01.
Ref 14	EGFR binding Fc domain-drug conjugates: stable and highly potent cytotoxic molecules mediate selective cell killing. Biol Chem. 2021 Sep 20;403(5-6):525-534.
Ref 15	An anti-EGFR antibody-drug conjugate overcomes resistance to HER2-targeted drugs. Cancer Lett. 2023 Feb 1;554:216024.
Ref 16	Camptothecin derivative and ligand-drug conjugate thereof; 2022-04-21.
Ref 17	A Novel EGFR Targeted Immunotoxin Based on Cetuximab and Type 1 RIP Quinoin Overcomes the Cetuximab Resistance in Colorectal Cancer Cells. Toxins (Basel). 2023 Jan 9;15(1):57. doi: 10.3390/toxins15010057.
Ref 18	Conjugation of Cetuximab - Puromycin and Its Target-Specific Effect on Triple Negative Breast Cancer Cell Lines. Asian Pac J Cancer Prev. 2022 May 1;23(5):1803-1812.
Ref 19	Discovery of STRO-002, a Novel Homogeneous ADC Targeting Folate Receptor Alpha, for the Treatment of Ovarian and Endometrial Cancers. Mol Cancer Ther. 2023 Feb 1;22(2):155-167.
Ref 20	Bioactive substance conjugate, preparation method therefor and use thereof; 2022-08-18.
Ref 21	Bispecific antibody-drug conjugates targeting EGFR and MUC1 and uses thereof
Ref 22	Anti-EGFR Antibody-Drug Conjugate Carrying an Inhibitor Targeting CDK Restricts Triple-Negative Breast Cancer Growth
Ref 23	Antibody drug conjugates with enzymatically cleavable groups
Ref 24	Antibody-drug complexes containing hemiasterlin derivatives