OTX-015 (BIRABRESIB)

Background Information:

OTX-015 (Birabresib) is an orally bioavailable synthetic small
molecule BET Bromodomain inhibitor, selectively binding to the BRD2/3/4
in a competitive manner, with EC50 values of 10-19 nM. In vitro and in
vivo experiments showed that OTX015 targeted NFKB/TLR/JAK/STAT signaling
pathways, MYC- and E2F1-regulated genes, cell-cycle regulation, and
chromatin structure. Displaying in vitro synergism with several
anticancer agents, especially with mTOR and BTK inhibitors (ref 1).

Reference:

1. M. Boi, et al, The BET Bromodomain Inhibitor OTX015 Affects
Pathogenetic Pathways in Preclinical B-cell Tumor Models and Synergizes
with Targeted Drugs. Clin Cancer Res. 2015 Jan 26.
2. The optical purity of OTX-015 being offered by some vendors is too
poor to be reported in their Certificate of Analysis. An optically pure
OTX-015 is NOT a given even starting from optically pure synthon as it
readily racemizes (to ~20% wrong isomer) during the Lengthy multistep
preparation. A Chiral HPLC would be revealing.

APIM050340: OTX-015 (Birabresib)

CAS No.: 202590-98-5.
Molecular Formula: C₂₅H₂₂ClN₅O₂S ? 0.7H₂O.
Molecular Weight: 504.6.
Purity: >99.5% (HPLC at 215 and 254 nm), >99% Optical Purity (Chiral HPLC).
QC: HPLC-MS, ¹HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.