Linker Information

Linker Name

Linker Type

Hydrazino-iso-pictet-spengler linker

Antibody-Linker Relation

Uncleavable

General Information of This Linker

Each Antibody-drug Conjugate Related to This Linker

Full Information of The Activity Data of The ADC(s) Related to This Linker

2G10 RED-106 maytansine 4 [Investigative]

ADC Info

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)	≈ 30.42% (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

2G10 RED-106 maytansine 2 [Investigative]

ADC Info

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.