VHL ligand 2 hydrochloride
Cat. No.: DC26119
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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 |
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| 2018-0101 |
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| 2018-0101 |
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