ARV-771 (C005B-309869)

Catalog No.: C005B-309869
Mfr. No.: SML2923-25MG
Mfr. Name: Sigma-Aldrich
Qty/UOM: 25
UOM: MG

Price: $1,100.21

List Price: $1,222.45

Biochem/physiol Actions ARV-771 is a bromodomain and extraterminal (BET) proteins degrader with a HIF-1?-derived von HippelÃ¢â‚¬â€œLandau (VHL) E3 ligase-binding hydroxyproline and a BET-binding triazolo-diazepine acetamide. ARV-771 induces BET

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Description
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Biochem/physiol Actions

ARV-771 is a bromodomain and extraterminal (BET) proteins degrader with a HIF-1?-derived von HippelÃ¢â‚¬â€œLandau (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
Availability:: 3-5 Days
Weight:: 1.00 Ounces
HazmatClass:: No
MPN:: SML2923-25MG
CAS:: 1949837-12-0

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