EPZ-5676
EPZ-5676 is an inhibitor of DOT1L histone methyltransferase (HMT) that exhibits anticancer chemotherapeutic activity. In acute myelogenous leukemia (AML) cells with MLL gene translocations, EPZ-5676 displays cytotoxicity; in similar animal models, this compound induces tumor regression without toxicity.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18921369
| Cas No. |
1380288-87-8 |
|---|---|
| Purity |
≥98% |
| Formula |
C30H42N8O3 |
| Formula Wt. |
562.71 |
| IUPAC Name |
(2R,3R,4S,5R)-2-(6-aminopurin-9-yl)-5-[[[3-[2-(6-tert-butyl-1H-benzimidazol-2-yl)ethyl]cyclobutyl]-propan-2-ylamino]methyl]oxolane-3,4-diol |
| Appearance |
White to off white powder |
Basavapathruni A, Olhava EJ, Daigle SR, et al. Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor. Biopharm Drug Dispos. 2014 Jan 10. [Epub ahead of print]. PMID: 24415392.
Daigle SR, Olhava EJ, Therkelsen CA, et al. Potent inhibition of DOT1L as treatment of MLL-fusion leukemia. Blood. 2013 Aug 8;122(6):1017-25. PMID: 23801631.
