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SML2923

Sigma-Aldrich

ARV-771

≥98% (HPLC)

Sinônimo(s):

JQ1-VHL

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About This Item

Fórmula empírica (Notação de Hill):
C49H60ClN9O7S2
Número CAS:
1949837-12-0
Peso molecular:
986.64
Número MDL:
MFCD30738017
Código UNSPSC:
12352200
NACRES:
NA.77

ligand

VH032

Nível de qualidade

100

Ensaio

≥98% (HPLC)

Formulário

powder

cor

white to beige

solubilidade

DMSO: 2 mg/mL, clear

temperatura de armazenamento

2-8°C

cadeia de caracteres SMILES

[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

chave InChI

PQOGZKGXGLHDGS-QQRWPDCKSA-N

Categorias relacionadas

Ações bioquímicas/fisiológicas

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).

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable

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Certificados de análise (COA)

Lot/Batch Number

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Lu Zhang et al.
Molecular cancer therapeutics, 18(7), 1302-1311 (2019-05-09)
Proteolysis-targeting chimeras (PROTAC) are bifunctional molecules that hijack endogenous E3 ubiquitin ligases to induce ubiquitination and subsequent degradation of protein of interest. Recently, it has been shown that PROTACs with robust in vitro and in vivo activities and, in some
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
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
Dyana T Saenz et al.
Leukemia, 33(6), 1373-1386 (2018-12-24)
Transformation of post-myeloproliferative neoplasms into secondary (s) AML exhibit poor clinical outcome. In addition to increased JAK-STAT and PI3K-AKT signaling, post-MPN sAML blast progenitor cells (BPCs) demonstrate increased nuclear β-catenin levels and TCF7L2 (TCF4) transcriptional activity. Knockdown of β-catenin or
Daniel J Coleman et al.
Scientific reports, 9(1), 3823-3823 (2019-03-09)
The BET bromodomain protein BRD4 is a chromatin reader that regulates transcription, including in cancer. In prostate cancer, specifically, the anti-tumor activity of BET bromodomain inhibition has been principally linked to suppression of androgen receptor (AR) function. MYC is a

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