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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.
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