ARV-771

ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2 (1), BRD2 (2), BRD3 (1), BRD3 (2), BRD4 (1), and BRD4 (2), respectively[1].

Product Specifications

CAS Number

[1949837-12-0]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

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/ARV-771.html

Purity

99.87

Solubility

DMSO : ≥ 50 mg/mL

Smiles

CC(C(C(C1=CC=C(Cl)C=C1)=N[C@@H](CC(NCCOCCCOCC(N[C@@H](C(C)(C)C)C(N(C[C@H](O)C2)[C@@H]2C(N[C@H](C3=CC=C(C(SC=N4)=C4C)C=C3)C)=O)=O)=O)=O)C5=NN=C(C)N65)=C6S7)=C7C

Molecular Formula

C49H60ClN9O7S2

Molecular Weight

986.64

Precautions

H302, H315, H319, H335

References & Citations

[1]Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Jun 28;113 (26) :7124-9.