SML2923
ARV-771
≥98% (HPLC)
Synonym(s):
JQ1-VHL
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About This Item
Empirical Formula (Hill Notation):
C49H60ClN9O7S2
CAS Number:
Molecular Weight:
986.64
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
ligand
VH032
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
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
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).
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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)
BET bromodomain inhibitors have emerged as a promising therapy for numerous cancer types in preclinical studies, including neurofibromatosis type 1 (NF1)-associated malignant peripheral nerve sheath tumor (MPNST). However, potential mechanisms underlying resistance to these inhibitors in different cancers are not
Neeraj Jain et al.
Science translational medicine, 11(497) (2019-06-21)
The activated B cell (ABC-like) subtype of diffuse large B cell lymphoma (DLBCL) is characterized by chronic activation of signaling initiated by immunoglobulin μ (IgM). By analyzing the DNA copy number profiles of 1000 DLBCL tumors, we identified gains of
B Sun et al.
Leukemia, 32(2), 343-352 (2017-07-01)
Bromodomain extraterminal protein (BETP) inhibitors transcriptionally repress oncoproteins and nuclear factor-κB (NF-κB) target genes that undermines the growth and survival of mantle cell lymphoma (MCL) cells. However, BET bromodomain inhibitor (BETi) treatment causes accumulation of BETPs, associated with reversible binding
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML2923-5MG | 04061841702108 |
| SML2923-25MG | 04061841704102 |