Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0EVIRB
ADC Name	Tras-Gly5-May
Synonyms	Tras Gly5 EDA May Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative
Drug-to-Antibody Ratio	3.4
Structure
	3D MOL	2D MOL
Antibody Name	Trastuzumab		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	Mertansine DM1		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	Gly5		Linker Info

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)	18	ng/mL	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	> 110	ng/mL	SK-BR-3 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)	18.00 ng/mL	High HER2 expression (HER2+++; 694,000 HER2 molecules/cell)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO₂ atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
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)	> 110.00 ng/mL	Moderate HER2 expression (HER2++; 32,000 HER2 molecules/cell)
Method Description	Briefly, cells were plated on 96-well plates in 75 uL growth medium and grown at 37°C in a humidified incubator in a 7.5% CO₂ atmosphere. After one day incubation, 25 uL of 3.5-fold serial dilutions of each ADC in growth medium were added, typically resulting in final ADC concentrations from 20 ug/mL to 0.02 ng/mL.
In Vitro Model	Breast adenocarcinoma	SK-BR-3 cells		CVCL_0033

References

Ref 1	Highly Potent, Anthracycline-based Antibody-Drug Conjugates Generated by Enzymatic, Site-specific Conjugation. Mol Cancer Ther. 2017 May;16(5):879-892.