Antibody ID	ANI0ARFWM
Antibody Name	Anti-EGFR mAb
Antibody Type	Monoclonal antibody (mAb)
Antibody Subtype	Humanized IgG1-kappa
Antigen Name	Epidermal growth factor receptor (EGFR)					Antigen Info
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Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High EGFR expression (EGFR+++)
Method Description	Treatment of SCID mice bearing FaDu subcutaneous SCCHN xenografts (H-Score 225), with ADC14aat a single i.v. dose of 14.9 mg/kg.
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High EGFR expression (EGFR+++)
Method Description	Treatment of SCID mice bearing FaDu subcutaneous SCCHN xenografts (H-Score 225), with ADC14aat a single i.v. dose of 7.4 mg/kg.
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100%	High EGFR expression (EGFR+++)
Method Description	Treatment of SCID mice bearing FaDu subcutaneous SCCHN xenografts (H-Score 225), with ADC 14a at a single i.v. dose of 3.7 mg/kg.
In Vitro Model	Hypopharyngeal squamous cell carcinoma	FaDu cells		CVCL_1218

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.3 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model	Oral cavity squamous cell carcinoma	HSC-2 cells		CVCL_1287
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 3 nM	Negative EGFR expression (EGFR-)
Method Description	Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model	Lung non-small cell carcinoma	NCI-H2110 cells		CVCL_1530
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	3 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model	Oral cavity squamous cell carcinoma	HSC-2 cells		CVCL_1287
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	40 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.1 nM	Negative EGFR expression (EGFR-)
Method Description	Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model	Lung non-small cell carcinoma	NCI-H2110 cells		CVCL_1530

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	6 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model	Oral cavity squamous cell carcinoma	HSC-2 cells		CVCL_1287
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	30 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model	Human papillomavirus-related endocervical adenocarcinoma	KB cells		CVCL_0372
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.3 nM	Negative EGFR expression (EGFR-)
Method Description	Conjugates or free drug compounds were diluted in RPMI-1640 supplemented with heat-inactivated 10% FBS and 0.1 mg/ml gentamycin , and added to the plated cells. To determine specificity of cytotoxic activity of the conjugates an excess of unconjugated antibody was added to a separate set of diluted conjugates.
In Vitro Model	Lung non-small cell carcinoma	NCI-H2110 cells		CVCL_1530

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	4.7 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Tongue squamous cell carcinoma	SAS cells		CVCL_1675
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	12 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	13 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Lung adenocarcinoma	PC-9 cells		CVCL_B260
Experiment 4 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	14 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Oral cavity squamous cell carcinoma	HSC-2 cells		CVCL_1287
Experiment 5 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	39 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 6 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	99 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511

Experiment 1 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	6.1 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Tongue squamous cell carcinoma	SAS cells		CVCL_1675
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	7.5 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Oral cavity squamous cell carcinoma	HSC-2 cells		CVCL_1287
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	11 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Lung mucoepidermoid carcinoma	NCI-H292 cells		CVCL_0455
Experiment 4 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	17 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Lung adenocarcinoma	PC-9 cells		CVCL_B260
Experiment 5 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	45 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186
Experiment 6 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	93 pM	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were incubated with a serial dilution of conjugate, and a mixture of conjugate and excess, unconjugated anti-EGFR (0.35 M) or anti-FR antibody (1 M), respectively (blocking). After 4 days of continuous treatment with conjugates, cell viability was determined using Cell Titer Glo reagent.
In Vitro Model	Lung adenocarcinoma	NCI-H1975 cells		CVCL_1511

Experiment 1 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.112 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were cultured in a 5% CO2 cell incubator at 37°C for 24 hours. Cytotoxicity test contains about 10000 cells when 100uL is added to each well.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.126 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were cultured in a 5% CO2 cell incubator at 37°C for 24 hours. Cytotoxicity test contains about 10000 cells when 101uL is added to each well.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Experiment 1 Reporting the Activity Date of This ADC					[3]
Efficacy Data	Half Maximal inhibitory Concentration (lC50)	0.267 nM	Positive EGFR expression (EGFR+++/++)
Method Description	Cells were cultured in a 5% CO2 cell incubator at 37°C for 24 hours. Cytotoxicity test contains about 10000 cells when 102uL is added to each well.
In Vitro Model	Pancreatic ductal adenocarcinoma	BxPC-3 cells		CVCL_0186

Ref 1	Synthesis of Highly Potent N-10 Amino-Linked DNA-Alkylating Indolinobenzodiazepine Antibody-Drug Conjugates (ADCs). ACS Med Chem Lett. 2019 Jul 22;10(8):1211-1215. doi: 10.1021/acsmedchemlett.9b00254. eCollection 2019 Aug 8.
Ref 2	Optimizing Lysosomal Activation of Antibody-Drug Conjugates (ADCs) by Incorporation of Novel Cleavable Dipeptide Linkers. Mol Pharm. 2019 Dec 2;16(12):4817-4825. doi: 10.1021/acs.molpharmaceut.9b00696. Epub 2019 Oct 29.
Ref 3	Conjugates and antibody-drug conjugates prepared therefrom