Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0KGOWD
ADC Name	HER2-azide-alkyne MMAE conjugate
Synonyms	HER2 azide-alkyne MMAE conjugate Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative
Drug-to-Antibody Ratio	4
	3D MOL	2D MOL
Antibody Name	Trastuzumab		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	Azide-alkyne based linker 10a		Linker Info

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)	88	pM	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	13.9	ng/mL	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	> 10	ug/mL	T-47D 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)	88.00 pM	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
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)	13.90 ng/mL	Positive HER2 expression (HER2 +++/++)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 3 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 10.00 ug/mL	Low HER2 expression (HER2+)
Method Description	Cells were incubated with increasing concentrations in tested compounds for 96 h and cell viability was determined by MTS assay.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553

References

Ref 1	One-Pot Conversion of Free Sialoglycans to Functionalized Glycan Oxazolines and Efficient Synthesis of Homogeneous Antibody-Drug Conjugates through Site-Specific Chemoenzymatic Glycan Remodeling. Bioconjug Chem. 2021 Aug 18;32(8):1888-1897. doi: 10.1021/acs.bioconjchem.1c00314. Epub 2021 Aug 5.