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VHL ligand 2 hydrochloride

  Cat. No.:  DC26119   Featured
Chemical Structure
1948273-03-7
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Field of application
VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader.
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
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC26119 VHL ligand 2 hydrochloride VHL ligand 2 hydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC-Me hydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader.
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