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.
| 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 |
| Store Temp | 4°C |
|---|---|
| Ship Temp | Ambient |
| Info Sheet | E6398 Info Sheet PDF |
|---|---|
| Brochures | Epigenetic Modifiers Booklet |
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.
