CAS NO: | 1948273-03-7 |
规格: | 98% |
分子量: | 481.05 |
包装 | 价格(元) |
100mg | 电议 |
500mg | 电议 |
1g | 电议 |
2g | 电议 |
Background:
E3 ligase Ligand 1 is a Ligand for E3 Ligase extracted from patent WO/2017/030814A1 compound example 202, used in PROTAC technology.
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 degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of castration-resistant prostate cancer (CRPC) as compared with BET inhibition[2].
[1]. WO/2017/030814A1 [2]. Kanak R, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proceedings of the National Academy of Sciences of the United States of America (2016), 113(26), 7124-7129