Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0FLEUN
ADC Name	Anti-HER2 DVD-Fab-h38c2-K99C_MMAF
Synonyms	Anti-HER2 DVD-Fab-H38c2-K99C MMAF Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative
Drug-to-Antibody Ratio	0.9
Structure
	3D MOL	2D MOL
Antibody Name	Anti-HER2 DVD-Fab-h38c2-K99C		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	Monomethyl auristatin F		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	Dibromomaleimide-PEG4		Linker Info
Conjugate Type	Dibromomaleimide selectively reacts with the engineered cysteine residue of h38C2_K99C DVD-Fab, Michael addition reaction.
Combination Type	Dibromomaleimide-PEG4-MMAF

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)	0.33	nM	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Effective Concentration (EC50)	> 10	uM	MDA-MB-231 cells	Breast 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)	0.33 nM	High HER2 expression (HER2+++)
Method Description	Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO₂ for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells. Click to Show/Hide
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 Effective Concentration (EC50)	> 10.00 uM	Negative HER2 expression (HER2-)
Method Description	Breast cancer SK-BR-3 (HER2+) and MDA-MB-231 (HER2-) cells were seeded in 96-well tissue culture plates. The prepared ADCs and their corresponding unconjugated DVD-IgG1 were added to the cells at 10-fold serial dilution (0.001100 nM), followed by incubation at 37°C, 5% CO₂ for 72 h. Cell viability was then measured using CellTiter 96 aqueous one solution (Promega) and plotted as a percentage of untreated cells. Click to Show/Hide
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

References

Ref 1	Sculpting a Uniquely Reactive Cysteine Residue for Site-Specific Antibody Conjugation. Bioconjug Chem. 2022 Jun 15;33(6):1192-1200.