Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0BTRCK
ADC Name	Trastuzumab I253Q-MMAE
Synonyms	Trastuzumab-I253Q-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 I253Q		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	Dansylcadaverine-BCN based linker		Linker Info
Conjugate Type	Random conjugation through nucleophilic lysines.

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)	0.16	nM	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	> 100	nM	HeLa cells	Endocervical 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)	0.16 nM	Positive HER2 expression (HER2+++/++)
Method Description	Cytotoxicity of MMAE-conjugated trastuzumab I253Q variant. Serial dilutions of trastuzumab variants (0.01 nM to 20 nM) were incubated for 3 days on SK-BR-3 (HER2) cells.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033
Experiment 2 Reporting the Activity Date of This ADC					[2]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	> 100 nM	Negative HER2 expression (HER2 -)
Method Description	Cytotoxicity of MMAE-conjugated trastuzumab I253Q variant. Serial dilutions of trastuzumab variants (0.01 nM to 20 nM) were incubated for 3 days on SK-BR-3 (HER2) cells.
In Vitro Model	Endocervical adenocarcinoma	HeLa cells		CVCL_0030

References

Ref 1	Tag-free, specific conjugation of glycosylated IgG1 antibodies using microbial transglutaminase. RSC Adv. 2022 Nov 22;12(52):33510-33515. doi: 10.1039/d2ra05630e. eCollection 2022 Nov 22.
Ref 2	Hiding Payload Inside the IgG Fc Cavity Significantly Enhances the Therapeutic Index of Antibody-Drug Conjugates. J Med Chem. 2023 Jan 12;66(1):1011-1026. doi: 10.1021/acs.jmedchem.2c01812. Epub 2022 Dec 30.