Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0APKYO
ADC Name	Alpha-HER2-Duo 405
Synonyms	AlphaHER2-Duo 405 Click to Show/Hide
Organization	Merck & Co., Inc.
Drug Status	Investigative
Indication	In total 1 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative
Drug-to-Antibody Ratio	2
	3D MOL	2D MOL
Antibody Name	Anti-HER2 mAb		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	Duocarmycin 405		Payload Info
Therapeutic Target	Human Deoxyribonucleic acid (hDNA)		Target Info
Linker Name	Undisclosed
Conjugate Type	The drug linker was conjugated to the unnatural amino acid (UAA) para-azido phenylalanine (p-AF)

General Information of The Activity Data Related to This ADC

Revealed Based on the Cell Line Data

Click To Hide/Show 2 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	0.08	nM	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	> 100	nM	MDA-MB-468 cells	Breast adenocarcinoma

Full List of Activity Data of This Antibody-drug Conjugate

Revealed Based on the Cell Line Data

Click To Hide/Show 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	0.08 nM	Positive HER2 expression (HER2 +++/++)
Method Description	The cells wereincubated with serial dilutions of Duocarmycin-405 conjugated to anti-HER2 or a non-targetingantibody, Duocarmycin free drug and naked ant-HER2 controls for 6 days.
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)	> 100 nM	Negative HER2 expression (HER2 -)
Method Description	The cells wereincubated with serial dilutions of Duocarmycin-405 conjugated to anti-HER2 or a non-targetingantibody, Duocarmycin free drug and naked ant-HER2 controls for 6 days.
In Vitro Model	Breast adenocarcinoma	MDA-MB-468 cells		CVCL_0419

References

Ref 1	Phosphate based linkers for intracellular delivery of drug conjugates; 2015-10-08.