ARV-771 (C005B-309868)

Biochem/physiol Actions

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).

UPC:

51182068

Condition:

New

Weight:

1.00 Ounces

HazmatClass:

No

Quantity:

5

Unit of Measurement:

MG

MPN:

SML2923-5MG

CAS:

1949837-12-0

Controlled Substances and Cyanide:

Yes