Birabresib
CAS No. | 202590-98-5 | Cat. No. | BCP09079 |
Name | Birabresib | ||
Synonyms | OTX015; OTX-015; OTX 015; MK-8628; MK 8628; MK8628; | ||
Formula | C25H22ClN5O2S | M. Wt | 491.12 |
Description | Birabresib, also known as OTX015 and MK-8628, a potent BET bromodomian inhibitor, which targets the BET bromodomain proteins 2, 3, and 4 (BRD2/3/4). BRDs 2, 3, and 4 are considered potential cancer targets because of their pivotal role in regulating the transcription of growth-promoting genes and cell cycle regulators. OTX015 is the first BRD2/3/4 inhibitor to enter clinical trials. OTX015 showed antiproliferative activity in a large panel of cell lines derived from mature B-cell lymphoid tumors with median IC50 of 240 nmol/L, without significant differences among the different histotypes. | ||
Pathways | Epigenetics | ||
Targets | Epigenetic Reader Domain |
Structure
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