ARV 771

Catalog # Availability Size / Price Qty
ARV 771 | CAS No. 1949837-12-0 | Active Degraders
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Description: Potent BET bromodomain PROTAC®; also degrades BRD-tagged chimeric antigen receptors (CAR) in T cells

Chemical Name: (2S,4R)-1-((S)-2-(tert-Butyl)-15-((S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-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-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

Purity: ≥98%

Product Details

Biological Activity

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.

Technical Data

Soluble to 100 mM in DMSO
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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