Birabresib (OTX015; MK8628)

Description: Birabresib (formerly OTX-015; MK-8628) is a potent and orally bioavailable inhibitor of BET bromodomain (BRD2/3/4) with antineoplastic activity. It inhibits BRD2/3/4 with EC50s in the range of 10 to 19 nM in cell-free assays. OTX 015 is the first BRD2/3/4 inhibitor to enter clinical trials (phase 2) for the treatment of cancer, and is currently in clinical trials for treating leukemia and glioblastoma. OTX015 exhibits excellent antiproliferative activity in a large panel of cell lines derived from mature B-cell lymphoid tumors with median IC50 of 240 nmol/L, and high in vivo antitumor efficacy.

References: Oncotarget. 2015 Mar 20; 6(8):5501-16; Mol Cancer Ther. 2013, 12, C244; Mol Cancer Ther. 2013, 12, A21

Related CAS: 202590-98-5; 204587-26-8 (dihydrate)

MK-8628; MK 8628; Birabresib; OTX015; OTX-015; MK8628; OTX 015

Chemical Name: (S)-2-(4-(4-chlorophenyl)-2, 3, 9-trimethyl-6H-thieno[3, 2-f][1, 2, 4]triazolo[4, 3-a][1, 4]diazepin-6-yl)-N-(4-hydroxyphenyl)acetamide.

SMILES Code: O=C(NC1=CC=C(O)C=C1)C[CH]2C3=NN=C(C)N3C4=C(C(C)=C(C)S4)C(C5=CC=C(Cl)C=C5)=N2