Linker ID	LIN0FCNGM
Linker Name	Gly3-Val-Cit-PABC
Linker Type	Sortase-based site-specific conjugation linker; Cathepsin-cleavable linker
Antibody-Linker Relation	Cleavable
Structure
	3D MOL			2D MOL
Formula	C27H44N8O7
Isosmiles	C=CC.CC(C)C(NC(=O)CNC(=O)CNC(=O)CN)C(=O)NC(CCCNC(N)=O)C(=O)Nc1ccc(CO)cc1
InChI	InChI=1S/C24H38N8O7.C3H6/c1-14(2)21(32-20(36)12-29-19(35)11-28-18(34)10-25)23(38)31-17(4-3-9-27-24(26)39)22(37)30-16-7-5-15(13-33)6-8-16;1-3-2/h5-8,14,17,21,33H,3-4,9-13,25H2,1-2H3,(H,28,34)(H,29,35)(H,30,37)(H,31,38)(H,32,36)(H3,26,27,39);3H,1H2,2H3
InChIKey	QQGQLPHYBLWMAT-UHFFFAOYSA-N
Pharmaceutical Properties	Molecule Weight		592.698	Polar area		246.87
	Complexity		42	xlogp Value		-1.4251
	Heavy Count		42	Rot Bonds		16
	Hbond acc		8	Hbond Donor		9

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.18±0.03 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of Fcab-1-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of Fcab-1-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.40 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of Fcab-1-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.19±0.05 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of Fcab-2-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of Fcab-2-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.40 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of Fcab-2-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.22±0.01 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of Fcab-3-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of Fcab-3-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.40 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of Fcab-3-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[1]
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					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 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					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.40 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					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.78±0.03 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of C-Fab-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of C-Fab-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.40 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of C-Fab-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100.00 nM	Negative EGFR expression (EGFR-)
Method Description	The inhibitory activity of huFc-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Invasive breast carcinoma	MCF-7 cells		CVCL_0031
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 300.00 nM	High EGFR expression (EGFR+++/++)
Method Description	The inhibitory activity of huFc-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419
Experiment 3 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Effective Concentration (EC50)	1.40 nM	Low FOLR1 expression (FOLR1+)
Method Description	The inhibitory activity of huFc-MMAE against cancer cell growth was evaluated in various human cancer cell lines in vitro.
In Vitro Model	Skin squamous cell carcinoma	A431 cells		CVCL_0037

Ref 1	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 2	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.