ARCC-4-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEARCC-4Cat. No.: HY-130492CAS No.: 1973403-00-7分式: CHFNOS分量: 1024.18作靶点: PROTAC; Androgen Receptor作通路: PROTAC; Others储存式: Please store the product under the recommended conditions inthe COA.BIOLOGICAL ACTIVITY物活性 ARCC-4 PROTAC 技术

2、的，纳尔级的雄激素受体 (AR) 降解剂，其 D50 值为 5 nM。ARCC-4种基于 enzalutamide 的 von Hippel-Lindau (VHL) 招募的 AR PROTAC。ARCC-4 能有效降解与抗雄激素研究相关的AR 突变 1。IC50 & Target VHL体外研究ARCC-4 induces apoptosis and inhibiting proliferation of AR-amplified prostate cancer cells 1.ARCC-4 enhances protein-protein interactions between AR a

3、nd VHL, thereby promoting the association ofthe trimeric complex 1.ARCC-4 (0.1-10,000 nM; 20 hours) potently degrades AR with a D50 of 5nM and Dmax of over 95% 1.ARCC-4 (100nM; 12 hours) shows near complete AR degradation (98%) in prostate cancer cells 1.ARCC-4 selectively degrades AR via the protea

4、some but not PR-A or PR-B suppression 1.ARCC-4 shows efficacy against clinically relevant AR mutations 1.ARCC-4 maintains activity despite elevated androgen levels 1.Western Blot Analysis 1Cell Line: VCaP cellsConcentration: 0.1 nM, 1 nM, 10 nM, 50 nM, 100 nM, 0.5M, 1M, 10 MIncubation Time: 20hours1

5、/2 Master of Small Molecules 您边的抑制剂师www.MedChemEResult: Potently degrades ARREFERENCES1. Salami J, et al. Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellularmodels of prostate cancer drug resistance. Commun Biol. 2018 Aug 2;1:100.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 021