Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0CXIUK
ADC Name	T-CpHK-Tet-ADC
Synonyms	T-CpHK Tet 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	Tetrazine-PEG5-Val-Ala-PABC		Linker Info
Conjugate Type	CpHK was incorporated at the antibody heavy chain, replacing the amino acid residue K274 to yield reactive antibodies bearing cyclopentadiene groups, tetrazinecyclopentadiene conjugating, DielsAlder (DA) reaction.
Combination Type	Tetrazine-PEG5-Val-Ala-PABC-MMAE

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)	0.3	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)	68	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)	0.30 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)	68.00 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.