Tocris Bioscience™ ARV 771

Description

Potent BET bromodomain PROTAC™; also degrades BRD-tagged chimeric antigen receptors (CAR) in T cells

ARV 771 is a potent BET bromodomain PROTAC™ degrader (DC50 = < 1nM). Comprises a BRD4-binding moiety joined by a linker to a ligand for Von Hippel-Lindau (VHL) protein. Degrades BRD2/3/4 in castration-resistant prostate cancer (CRPC) cell lines. Reduces androgen receptor levels and induces apoptosis in CRPC cells in vitro. Down-regulates BRD4 and induces tumor regression in CRPC xenografts in mice. Also reduces leukemia burden in a mouse model. Induces degradation of BRD-tagged CAR (chimeric antigen receptor) in T cells. PROTAC™ is a registered trademark of Arvinas Operations, Inc., and is used under license.

Specifications

• Chemical Name or Material: (2 S,4 R)-1-(-2-(tert-Butyl)-15-(-4-(4-chlorophenyl)-2,3,9-trimethyl-6 H-thieno[3,2-f][1,2,4 ]triazolo[4,3-a][1,4 ]diazepin-6-yl)-4,14-dioxo-6,10-dioxa-3,13-diazapentadecanoyl)-4-hydroxy-N-(-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carbox
• CAS: 1949837-12-0
• Quantity: 5 mg
• Target: Active Degraders
• Molecular Formula: C₄₉H₆₀ClN₉O₇S₂
• Purity: 0.98