Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0LYYQA
ADC Name	Anti-HER-AO-Cys-MC-VC-PABC-PEG8-Dol10
Synonyms	Anti-HER-AO-Cys-VC-PEG8-Dol10 Click to Show/Hide
Organization	Genzyme Corp.
Drug Status	Investigative
Indication	In total 2 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative Ovarian cancer [ICD11:2C73] Investigative
Drug-to-Antibody Ratio	1.5
	3D MOL	2D MOL
Antibody Name	Anti-HER2 mAb WT		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	Undisclosed
Linker Name	Anti-HER-AO-Cys-MC-VC-PABC-PEG8-Dol10 linker
Conjugate Type	Random conjugation through reduced inter-chain cysteines.

General Information of The Activity Data Related to This ADC

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 63.33	%	CVCL_0532	Ovarian serous cystadenocarcinoma

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)	0.97	nM	CVCL_0033	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	> 100	nM	CVCL_0062	Breast adenocarcinoma

Full List of Activity Data of This Antibody-drug Conjugate

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 63.33% (Day 66)	Positive HER2 expression (HER2+++/++)
Method Description	Nude mice were implanted with SK-OV-3 tumor cells which were allowed to establish tumors of ~150 mm³ prior to initiation of treatment. ADCs at 10 mg/kg doses were injected through tail vein on days 38, 45, 52 and 59. There were ~10 mice per group. The tumor volume of mice in different group was measured and their survival was recorded.
In Vivo Model	SK-OV-3 CDX model
In Vitro Model	Ovarian serous cystadenocarcinoma	SK-OV-3 cells		CVCL_0532

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)	0.97 nM	High HER2 expression (HER2+++)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO₂. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
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)	> 100.00 nM	Negative HER2 expression (HER2-)
Method Description	Cells were plated at a density of 5,000 cells per well in black walled 96-well plate and allowed to adhere overnight in a humidified at mosphere of 5% CO₂. CellTiter-Glo reagent was added to the wells at room temperature and the luminescent signal was measuredafter 10 min using a SpectraMax M5 plate reader.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

References

Ref 1	Site-specific antibody-drug conjugation through glycoengineering.