OARV-771

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].

Product Specifications

CAS Number

[2683008-37-7]

UNSPSC

12352005

Target

Epigenetic Reader Domain; PROTACs

Type

Reference compound

Related Pathways

Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/oarv-771.html

Purity

98.77

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CC1=C(C)SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@@H](CC(OCCOCCCOCC(N[C@@H](C(C)(C)C)C(N4[C@@H](C[C@H](C4)O)C(N[C@H](C5=CC=C(C6=C(C)N=CS6)C=C5)C)=O)=O)=O)=O)C7=NN=C(C)N27

Molecular Formula

C49H59ClN8O8S2

Molecular Weight

987.62

References & Citations

[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.