| Identification | Back Directory | [Name]
(2S,4R)-1-((S)-2-amino-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide hydrochloride | [CAS]
1948273-03-7 | [Synonyms]
CPD101079
E3 ligase Ligand 1
VHL ligand 2 hydrochloride
3-Methyl-L-valyl-(4R)-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-L-Prolinamide HCl
L-Prolinamide, 3-methyl-L-valyl-4-hydroxy-N-[(1S)-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, hydrochloride (1:1), (4R)-
(2S,4R)-1-((S)-2-amino-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide hydrochloride
(2S,4R)-1-((S)-2-amino-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide dihydrochloride | [Molecular Formula]
C23H33ClN4O3S | [MDL Number]
MFCD30729675 | [MOL File]
1948273-03-7.mol | [Molecular Weight]
481.05 |
| Chemical Properties | Back Directory | [storage temp. ]
Inert atmosphere,2-8°C | [form ]
Solid | [color ]
Off-white to yellow | [InChIKey]
GHFOLQCCYGBOTL-HDOVMFICNA-N | [SMILES]
C(N1C[C@H](O)C[C@H]1C(=O)N[C@H](C1C=CC(C2SC=NC=2C)=CC=1)C)(=O)[C@@H](N)C(C)(C)C.Cl |&1:3,6,10,25,r| |
| Hazard Information | Back Directory | [Uses]
(S,R,S)-AHPC-Me 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[1]. (S,R,S)-AHPC-Me hydrochloride 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]. | [IC 50]
VHL | [References]
[1] WO/2017/030814A1
[2] 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. DOI:10.1073/pnas.1521738113 |
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