Birabresib

  • Chemical Properties
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
  • Biological Activity
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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