Synonyms: JQ1-VHL
Molecular Formula: C49H60ClN9O7S2
Molecular Weight: 986.64
Linear Structural Formula: C49H60ClN9O7S2
MDL Number: MFCD30738017
Purity: >=98% (HPLC)
Storage: 2-8C
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 egression in mice in vivo (30 mg g s.c.; 22rv1 and vcap).<>