Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0NPYPV
ADC Name	T-CpHK-Mal-ADC
Synonyms	T-CpHK Mal ADC Click to Show/Hide
Drug Status	Investigative
Indication	In total 2 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative Gastric cancer [ICD11:2B72] Investigative
Drug-to-Antibody Ratio	3.7
Structure
	3D MOL	2D MOL
Antibody Name	Trastuzumab-CpHK		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	Monomethyl auristatin E		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	Mc-Val-Cit-PABC		Linker Info
Conjugate Type	Random conjugation through reduced inter-chain cysteines.
Combination Type	Vedotin

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)	0.2	nM	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	0.4	nM	NCI-N87 cells	Gastric tubular adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	45	nM	ZR-75-1 cells	Invasive breast 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)	0.20 nM	High HER2 expression (HER2+++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.40 nM	High HER2 expression (HER2+++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Gastric tubular adenocarcinoma	NCI-N87 cells		CVCL_1603
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	45.00 nM	Moderate HER2 expression (HER2++)
Method Description	ADCs were subjected to cytotoxicity assays to confirm potency toward cell lines with high and low HER2 expression.
In Vitro Model	Invasive breast carcinoma	ZR-75-1 cells		CVCL_0588

References

Ref 1	Cyclopentadiene as a Multifunctional Reagent for Normal- and Inverse-Electron Demand Diels-Alder Bioconjugation. Bioconjug Chem. 2022 Sep 21;33(9):1609-1619.