| 货号 | 16175-25mg |
| 描述 | DOT1L is a non-SET domain containing methyltransferase whose function is important for the transcriptional activation of certain genes, DNA damage repair, and cell cycle regulation. DOT1L is known to play an essential role in MLL-rearranged leukemias, and thus has emerged as a drug target for these leukemias.1,2 EPZ5676 is a highly potent aminonucleoside inhibitor of DOT1L histone methyltransferase activity (Ki = 80 pM) that demonstrates 37,000-fold selectivity over other methyltransferases.3,4 In various human leukemia cell lines, EPZ5676 has been shown to inhibit the methylation of lysine 79 on histone 3 (IC50s = 3-5 nM), decreasing MLL-fusion target gene expression (IC50s = 53-67 nM).3 It can selectively inhibit the proliferation of acute leukemia cell lines bearing MLL translocations (IC50s range from 3.5 nM - 1.3 µM).3 Continuous intravenous infusion of EPZ5676 at a dose of 35 mg/kg has been reported to cause complete and sustained tumor regression in a rat xenograft model of MLL-rearranged leukemia.3 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Nguyen, A.T.,He, J.,Taranova, O., et al. Essential role of DOT1L in maintaining normal adult hematopoiesis. Cell Research 21(9), 1370-1373 (2011). 2.Bernt, K.M. and Armstrong, S.A. A role for DOT1L in MLL-rearranged leukemias. Epigenomics 3(6), 667-670 (2011). 3.Daigle, S.R.,Olhava, E.J.,Therkelsen, C.A., et al. Potent inhibition of DOT1L as treatment of MLL-fusion leukemia. Blood 122(6), 1017-1025 (2013). 4.Basavapathruni, A.,Olhava, E.J.,Daigle, S.R., et al. Nonclinical pharmacokinetics and metabolism of EPZ-5676, a novel DOT1L histone methyltransferase inhibitor. Biopharmaceutics & Drug Disposition 35(4), 237-252 (2014). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 562.7 |
| 分子式 | C30H42N8O3 |
| CAS号 | 1380288-87-8 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |