OARV-771

Names

[ Name ]:
OARV-771

Biological Activity

[Description]:

OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC50s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> PROTAC >> PROTAC

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

[Target]

BRD4:6 nM (DC50)

BRD2:1 nM (DC50)

BRD3:4 nM (DC50)

VHL

[In Vitro]

OARV-771 shows antiproliferative effect with an EC50 value of 4 nM in MV4;11[1].

[References]

[1]. Klein VG, et al. Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity. J Med Chem. 2021;64(24):18082-18101.

Chemical & Physical Properties

[ Molecular Formula ]:
C₄₉H₅₉ClN₈O₈S₂

[ Molecular Weight ]:
987.62

OARV-771

Names

Biological Activity

Chemical & Physical Properties

Related Compounds