Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0DNFUC
ADC Name	Trastuzumab-MMAE conjugate DAR2
Synonyms	Trastuzumab MMAE conjugate 36; trastuzumab-Man-bata-1;4GlcNAc-DBCO-PEG5-VC-PAB-MMAE Click to Show/Hide
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	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 3 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)	0.07 10.67	nM ng/mL	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Effective Concentration (EC50)	0.41 6.20	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 3 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 SK-BR-3 and 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)	0.07 nM, 10.67 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and BT474 that have high levels of HER2 expression, and T47D that has low level expression of HER2 antigen.
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 Effective Concentration (EC50)	0.41 nM, 6.20 ng/mL	High HER2 expression (HER2+++)
Method Description	The cytotoxicity of the synthetic ADCs were tested in breast cancer cell lines SK-BR-3 and 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	Synthesis and Evaluation of Three Azide-Modified Disaccharide Oxazolines as Enzyme Substrates for Single-Step Fc Glycan-Mediated Antibody-Drug Conjugation. Bioconjug Chem. 2022 Jun 15;33(6):1179-1191.