Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0KUNBK
ADC Name	Trastuzumab-MMAE conjugate DAR12
Synonyms	Trastuzumab MMAE conjugate 47; trastuzumab MMAE conjugate DA12 Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative
Drug-to-Antibody Ratio	12
	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	Man-beta-1,4-GlcNAc-DBCO-PEG5-VC-PAB		Linker Info
Conjugate Type	Endo-S2 (D184M)performs a simultaneous deglycosylation and glycosylation of an antibody (Asn 279) with the drug-loaded disaccharide oxazoline substrates to give homogeneous ADCs.

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 Effective Concentration (EC50)	> 10	uM	T-47D cells	Invasive breast carcinoma
Half Maximal Effective Concentration (EC50)	0.04 7.13	nM ng/mL	BT-474 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 2 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	> 10.00 uM	Negative HER2 expression (HER2-)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	T-47D cells		CVCL_0553
Experiment 2 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Effective Concentration (EC50)	0.04 nM, 7.13 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
In Vitro Model	Invasive breast carcinoma	BT-474 cells		CVCL_0179

References

Ref 1	General and Robust Chemoenzymatic Method for Glycan-Mediated Site-Specific Labeling and Conjugation of Antibodies: Facile Synthesis of Homogeneous Antibody-Drug Conjugates. ACS Chem Biol. 2021 Nov 19;16(11):2502-2514.