SML2923
ARV-771
≥98% (HPLC)
别名:
JQ1-VHL
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关于此项目
经验公式（希尔记法）:
C49H60ClN9O7S2
化学文摘社编号:
分子量:
986.64
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
ARV-771, ≥98% (HPLC)
SMILES string
[s]1cnc(c1c2ccc(cc2)[C@@H](NC(=O)[C@H]3N(C[C@@H](C3)O)C(=O)[C@@H](NC(=O)COCCCOCCNC(=O)C[C@@H]4N=C(c6c([s]c(c6C)C)[n]7c4nnc7C)c5ccc(cc5)Cl)C(C)(C)C)C)C
InChI
1S/C49H60ClN9O7S2/c1-27-30(4)68-48-41(27)42(33-14-16-35(50)17-15-33)54-37(45-57-56-31(5)59(45)48)23-39(61)51-18-21-65-19-9-20-66-25-40(62)55-44(49(6,7)8)47(64)58-24-36(60)22-38(58)46(63)53-28(2)32-10-12-34(13-11-32)43-29(3)52-26-67-43/h10-17,26,28,36-38,4
InChI key
PQOGZKGXGLHDGS-QQRWPDCKSA-N
ligand
VH032
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
A cell-permeable BET proteins degrader that inhibits castrate-resistent prostate cancer growth both in vitro and in vivo by downregulating AR and c-Myc levels.
ARV-771 is a bromodomain and extraterminal (BET) proteins degrader with a HIF-1?-derived von Hippel–Landau (VHL) E3 ligase-binding hydroxyproline and a BET-binding triazolo-diazepine acetamide. ARV-771 induces BET proteins degradation in castrate-resistent prostate cancer (CRPC) cultures (BRD2/3/4 DC50 <5 nM; 22Rv1, VCaP & LnCaP95) and reduces downstream c-Myc transcription with 10-500-fold higher potency than JQ-1, OTX015, and dBET1. ARV-771, but not JQ-1 or OTX015, effectively downregulates CRPC androgen receptor (30-300 nM) and causes CRPC tumor growth retardation/regression in mice in vivo (30 mg/kg s.c.; 22Rv1 and VCaP).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
B Sun et al.
Leukemia, 32(2), 343-352 (2017-07-01)
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Jonathan M Cooper et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 25(11), 3404-3416 (2019-02-24)
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Lu Zhang et al.
Molecular cancer therapeutics, 18(7), 1302-1311 (2019-05-09)
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Neeraj Jain et al.
Science translational medicine, 11(497) (2019-06-21)
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Philipp Ottis et al.
ACS chemical biology, 14(10), 2215-2223 (2019-09-26)
Proteolysis targeting chimeras are bifunctional small molecules capable of recruiting a target protein of interest to an E3 ubiquitin ligase that facilitates target ubiquitination followed by proteasome-mediated degradation. The first molecules acting on this novel therapeutic paradigm have just entered
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