(S,R,S)-AHPC-Medihydrochloride(VHLligand2dihydrochloride)是一种基于(S,R,S)-AHPC的，可募集vonHippel-Lindau(VHL)蛋白的VHL配体。(S,R,S)-AHPC-Medihydrochloride可用于合成ARV-771。ARV-771是一种基于VHLE3连接酶的BETPROTAC降解剂。ARV-771可有效降解去势抵抗性前列腺癌(CRPC)细胞中的BET蛋白，DC50<1nM。
货号:ajcx29856
CAS:N/A
分子式:C23H34Cl2N4O3S
分子量：517.51
溶解度:DMSO: 100 mg/mL (193.23 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein[1]. (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50<1 nM[2].

[1]. Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.