Cas No.: | 1948273-03-7 |
Chemical Name: | N-[3-[[4-[[3-(trifluoromethyl)phenyl]amino]-2-pyrimidinyl]amino]phenyl]-cyclopropanecarboxamide |
SMILES: | NC(C(=O)N1CC(O)CC1C(=O)NC(C1C=CC(C2SC=NC=2C)=CC=1)C)C(C)(C)C.Cl |
Formula: | C21H18F3N5O |
M.Wt: | 413.4 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | VHL ligand 2 hydrochloride is a Ligand for E3 Ligase extracted from patent WO/2017/030814A1 compound example 202, used in PROTAC technology. |
Target: | Ligand for E3 Ligase[1] |
In Vitro: | 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]. |
References: | [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 |