Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0VIDMZ
ADC Name	Tras-Gly5-EDA-Pnu
Synonyms	Tras-Gly5-PNU; Tras Gly5 PNU Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative
Drug-to-Antibody Ratio	3.7-3.9
Structure
	3D MOL	2D MOL
Antibody Name	Trastuzumab		Antibody Info
Antigen Name	Receptor tyrosine-protein kinase erbB-2 (ERBB2)		Antigen Info
Payload Name	PNU-159682		Payload Info
Therapeutic Target	DNA topoisomerase 2-alpha (TOP2A)		Target Info
Linker Name	Gly5-EDA		Linker Info

General Information of The Activity Data Related to This ADC

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Standard Type	Value	Units	Cell Line	Disease Model
Tumor Growth Inhibition value (TGI)	≈ 100	%	JIMT-1 cells	Breast ductal carcinoma

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)	2.7	ng/mL	SK-BR-3 cells	Breast adenocarcinoma
Half Maximal Inhibitory Concentration (IC50)	14.7	ng/mL	T-47D cells	Invasive breast carcinoma

Full List of Activity Data of This Antibody-drug Conjugate

Discovered Using Cell Line-derived Xenograft Model

Click To Hide/Show 1 Activity Data Related to This Level

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Tumor Growth Inhibition value (TGI)	≈ 100.00% (Day 26)	High HER2 expression (HER2+++; 170,000 HER2 molecules/cell)
Method Description	JIMT-1 cells were transplanted subcutaneously into CB17.SCID mice and tumors were allowed to grow to a volume of 100-150 mm³. Mice were then treated intravenously 3 times weekly with the 1 mg/kg ADC preparations.
In Vivo Model	Trastuzumab-resistant breast cancer CDX model
In Vitro Model	Breast ductal carcinoma	JIMT-1 cells		CVCL_2077

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)	2.70 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)	14.70 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	Invasive breast carcinoma	T-47D cells		CVCL_0553

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.