E3-ligase-Ligand-1 _Ligand for E3 Ligase - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEE3 ligase Ligand 1Cat. No.: HY-42424CAS No.: 1948273-03-7分式: CHClNOS分量: 481.05作靶點(diǎn): Ligand for E3 Ligase作通路: PROTAC儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 63 mg/mL (130.96 mM)* means

2、 soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.0788 mL 10.3939 mL 20.7879 mL5 mM 0.4158 mL 2.0788 mL 4.1576 mL10 mM 0.2079 mL 1.0394 mL 2.0788 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 E3 ligase Ligand 1于 PROTAC 技術(shù)中的E3連接酶配體，來(lái)專利WO/2017

3、/030814A1，化合物實(shí)例202。IC50 & Target Ligand for E3 Ligase 1體外研究E3 ligase Ligand 1 is a VHL E3 ligase-binding ligand 1. E3 ligase Ligand 1 is used to synthesize ARV-771,a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC. ARV-771, a small-molecule pan-BET degrader1/2 Master of Small Molecules 您邊的抑制劑師www

4、.MedChemEbased on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacyin cellular models of castration-resistant prostate cancer (CRPC) as compared with BET inhibition 2.REFERENCES1. WO/2017/030814A12. Kanak R, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proceedings of theNational Academy of Sciences of the United States of America (2016), 113(26), 7124-7129McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 021-589559