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EPZ004777(formate)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EPZ004777(formate)图片
包装与价格:
包装价格(元)
500 µg电议
1mg电议
5mg电议
10mg电议

产品介绍
A potent inhibitor of DOT1L
Canonical SMILESCC(C)(C)C1=CC=C(NC(NCCCN(C(C)C)C[C@@H]2[C@@H](O)[C@@H](O)[C@H](N3C=CC4=C3N=CN=C4N)O2)=O)C=C1.O=CO
分子式C28H41N7O4·CH2O2
分子量585.7
溶解度DMF: 10 mg/ml,DMSO: 10 mg/ml,Ethanol: 10 mg/ml,Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
储存条件-20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

EPZ004777 is a potent inhibitor of DOT1L (IC50= 400 pM) that selectively kills mixed lineage leukemia (MLL) cellsin vitroand prolongs survival in an MLL xenograft mouse model.1,2,3,4It displays >1,000-fold selectivity for DOT1L relative to a panel of histone methyltransferases.1DOT1L inhibition by EPZ004777 has also been shown to accelerate the reprogramming of somatic cells into induced pluripotent stem cells.5

1.Daigle, S.R., Olhava, E.J., Therkelsen, C.A., et al.Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitorCancer Cell.20(1)53-65(2011) 2.Chen, L., Deshpande, A.J., Banka, D., et al.Abrogation of MLL-AF10 and CALM-AF10-mediated transformation through genetic inactivation or pharmacological inhibition of the H3K79 methyltransferase Dot1lLeukemia27(4)813-822(2013) 3.Deshpande, A.J., Chen, L., Fazio, M., et al.Leukemic transformation by the MLL-AF6 fusion oncogene requires the H3K79 methyltransferase Dot1lBlood121(13)2533-2541(2013) 4.Yu, W., Chory, E.J., Wernimont, A.K., et al.Catalytic site remodelling of the DOT1L methyltransferase by selective inhibitorsNat. Commun.31288(2012) 5.Ye, J., Ge, J., Zhang, X., et al.Pluripotent stem cells induced from mouse neural stem cells and small intestinal epithelial cells by small molecule compoundsCell Res.26(1)34-45(2016)