OTX-015
OTX-015 is an inhibitor of bromodomains (BRD) proteins such as BRD2/3/4; it is currently in clinical trials as a potential treatment for leukemias and other cancers. OTX-015 displays anticancer chemotherapeutic activity, inhibiting cell growth and tumor growth in various animal models, including anaplastic large cell lymphoma. This compound also induces apoptosis in activated B-cell-like diffuse large B-cell lymphoma cells.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18951445
| Cas No. |
202590-98-5 |
|---|---|
| Purity |
≥98% |
| Formula |
C25H22ClN5O2S |
| Formula Wt. |
491.99 |
| IUPAC Name |
2-[(6S)-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 |
| Synonym |
Y-803 |
| Appearance |
White to off white powder |
Boi M, Gaudio E, Bonetti P, 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 Apr 1;21(7):1628-38.PMID: 25633213.
Noel JK, Iwata K, Ooike S, et al. Development of the BET bromodomains inhibitor OTX015. Mol Cancer Ther. 2013 Nov:12;C244.
Boi M, Todaro M, Vurchio V, et al. OTX015, a bromodomains and extraterminal inhibitor, represents a novel agent for ALK positive anaplastic large cell lymphoma. Mol Cancer Ther. 2013 Nov:12;A219.
