Antibody-drug Conjugate Information

General Information of This Antibody-drug Conjugate (ADC)

ADC ID	DRG0ESBWC
ADC Name	2G10 RED-425 maytansine 4
Synonyms	2G10-RED-425-maytansine-4 Click to Show/Hide
Drug Status	Investigative
Indication	In total 1 Indication(s) Breast cancer [ICD11:2C60-2C65] Investigative
Drug-to-Antibody Ratio	3.46
	3D MOL	2D MOL
Antibody Name	Anti-PLAUR mAb 2G10		Antibody Info
Antigen Name	Urokinase plasminogen activator surface receptor (PLAUR)		Antigen Info
Payload Name	Mertansine DM1		Payload Info
Therapeutic Target	Microtubule (MT)		Target Info
Linker Name	RED-425		Linker Info
Conjugate Type	SMARTag site specific conjugation platform (Heavy chain CH1/C-term)

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)	≈ 38.75	%	MDA-MB-231 cells	Breast adenocarcinoma

Revealed Based on the Cell Line Data

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

Standard Type	Value	Units	Cell Line	Disease Model
Half Maximal Inhibitory Concentration (IC50)	500	nM	MDA-MB-231 cells	Breast adenocarcinoma

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)	≈ 38.75% (Day 56)	Positive PLAUR expression (PLAUR +++/++)
Method Description	To compare the in vivo anti-tumor efficacy of the various ADC constructs, we used MDA-MB-231 xenografts in mice. Animals with tumors of approximately 100 mm³ were treated once a week for four weeks with a 10 mg/kg dose of a variety of DAR 4 ADCs or 2G10 antibody.
In Vivo Model	MDA-MB-231 CDX model
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

Revealed Based on the Cell Line Data

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

Experiment 1 Reporting the Activity Date of This ADC					[1]
Efficacy Data	Half Maximal Inhibitory Concentration (IC50)	500 nM	Positive PLAUR expression (PLAUR +++/++)
Method Description	MDA-MB-231 cells (0.5x10⁴ cells/well) were seeded in 96-well plates at the density and incubated for 120 h (5 days) with of ADCs or IgG. After 5 days of drug treatment at 37°C with 5% CO₂.
In Vitro Model	Breast adenocarcinoma	MDA-MB-231 cells		CVCL_0062

References

Ref 1	Antibody-Drug Conjugates Targeting the Urokinase Receptor (uPAR) as a Possible Treatment of Aggressive Breast Cancer. Antibodies (Basel). 2019 Nov 5;8(4):54. doi: 10.3390/antib8040054.