SML2923
ARV-771
≥98% (HPLC)
Sinonimo/i:
JQ1-VHL
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About This Item
Formula empirica (notazione di Hill):
C49H60ClN9O7S2
Numero CAS:
Peso molecolare:
986.64
Numero MDL:
Codice UNSPSC:
12352200
NACRES:
NA.77
Prodotti consigliati
ligand
VH032
Livello qualitativo
Saggio
≥98% (HPLC)
Forma fisica
powder
Colore
white to beige
Solubilità
DMSO: 2 mg/mL, clear
Temperatura di conservazione
2-8°C
Categorie correlate
Azioni biochim/fisiol
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).
Codice della classe di stoccaggio
11 - Combustible Solids
Classe di pericolosità dell'acqua (WGK)
WGK 3
Punto d’infiammabilità (°F)
Not applicable
Punto d’infiammabilità (°C)
Not applicable
Certificati d'analisi (COA)
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