Merck
All Photos(1)

SML2923

Sigma-Aldrich

ARV-771

≥98% (HPLC)

Synonym(s):
JQ1-VHL
Empirical Formula (Hill Notation):
C49H60ClN9O7S2
CAS Number:
Molecular Weight:
986.64
Número MDL:

Nivel de calidad

100

ensayo

≥98% (HPLC)

formulario

powder

color

white to beige

solubilidad

DMSO: 2 mg/mL, clear

temp. de almacenamiento

2-8°C

Acciones bioquímicas o fisiológicas

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 clase de almacenamiento

11 - Combustible Solids

WGK

WGK 3

Punto de inflamabilidad F

Not applicable

Punto de inflamabilidad C

Not applicable

Certificate of Analysis

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Certificate of Origin

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