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OTX-015 (Birabresib) 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.
| Cas No. | 202590-98-5 |
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| 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 | OTX015; Y-803; Birabresib; MK-8626; MK8628 |
| Solubility | DMSO: ≥ 49 mg/mL |
| Appearance | White to off white powder |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
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.