Birabresib

Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM.

Product Specifications

CAS Number

[202590-98-5]

Product Name Alternative

OTX-015; MK-8628

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Epigenetic Reader Domain

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/OTX-015.html

Concentration

10mM

Purity

99.96

Solubility

DMSO : ≥ 49 mg/mL

Smiles

O=C(NC1=CC=C(O)C=C1)C[C@H]2C3=NN=C(C)N3C4=C(C(C)=C(C)S4)C(C5=CC=C(Cl)C=C5)=N2

Molecular Formula

C25H22ClN5O2S

Molecular Weight

491.99

Precautions

H302, H315, H319, H335

References & Citations

[1]J. Kay Noel, et al. Abstract C244: Development of the BET bromodomain inhibitor OTX015. Mol Cancer Ther November 2013 12; C244.|[2]Marie-Magdelaine Coudé, et al. BET inhibitor OTX015 targets BRD2 and BRD4 and decreases c-MYC in acute leukemia cells. Oncotarget. 2015 Jul 10; 6 (19) : 17698–17712.|[3]Lu P, et al. The BET inhibitor OTX015 reactivates latent HIV-1 through P-TEFb. Sci Rep. 2016 Apr 12;6:24100|[4]Vázquez R, et al. The bromodomain inhibitor OTX015 (MK-8628) exerts anti-tumor activity in triple-negative breast cancer models as single agent and in combination with RAD001. Oncotarget. 2017 Jan 31;8 (5) :7598-7613.