Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0TVMXR
ADC Name	C-IgG-Val-Cit-MMAE
Synonyms	C-IgG MMAE Click to Show/Hide
Drug Status	Investigative
Indication	In total 2 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative Epidermoid cancer [ICD11:XH4CR9] Investigative
Drug-to-Antibody Ratio	1.1
Structure
	3D MOL	2D MOL
Antibody Name	Cetuximab		Antibody Info
Antigen Name	Epidermal growth factor receptor (EGFR)		Antigen Info
Payload Name	Monomethyl auristatin E		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	Gly3-Val-Cit-PABC		Linker Info
Conjugate Type	Linker-payload was conjugated through sortase A (SrtA) recognition motif (LPETG) at the C-terminal end of the light chain.

General Information of The Activity Data Related to This ADC

Revealed Based on the Cell Line Data

Click To Hide/Show 3 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	0.44±0.03	nM	MDA-MB-468 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	> 100	nM	MCF-7 cells	Invasive breast carcinoma
Half Maximal Effective Concentration (EC50)	1.4	nM	A431 cells	Skin squamous cell carcinoma

Full List of Activity Data of This Antibody-drug Conjugate

Revealed Based on the Cell Line Data

Click To Hide/Show 3 Activity Data Related to This Level

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

References

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.