CAS NO: | 1446502-11-9 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Enasidenib is an oral, potent, reversible, selective inhibitor of theIDH2mutant enzymes, withIC50s of 100 and 400 nM against IDH2R140Qand IDH2R172K, respectively. | ||||||||||||||||
IC50& Target | IC50: 100 nM (IDH2R140Q), 400 nM (IDH2R172K)[1] | ||||||||||||||||
体外研究 (In Vitro) | Enasidenib (AG-221) reverses the effects of mutant IDH2 on DNA methylation in mutant stem/progenitor cells. Enasidenib induces differentiation and impairs self-renewal of IDH2-mutant leukemia cells, effects that are further enhanced by simultaneous inhibition of Flt3ITD. Enasidenib (AG-221) therapy induces differentiation of leukemic cells, with an increase in the CD11b+population and a decrease in the c-Kit+population in the peripheral blood at 2wks[2]. | ||||||||||||||||
体内研究 (In Vivo) | Treatment with Enasidenib (AG-221) significantly improves survival in an IDH2-mutant acute myeloid leukemia (AML) primary xenograft mouse model[1]. Enasidenib (AG-221), a mutant IDH2 inhibitor, remodels the epigenetic state of IDH2-mutant cells and induces alterations in self-renewal/differentiation in IDH2-mutant AML model in vivo. Enasidenib treatment (10mg/kg or 100mg/kg bid) leads to a reduction in 2-HG in vivo (96.7% below pre-treatment levels). Moreover, Enasidenib treatment restores megakaryocyte-erythroid progenitor (MEP) differentiation that is suppressed by mutant IDH2 expression (mean MEP% mean, 39% Veh vs 50% AG-221). Enasidenib therapy reverses the effects of mutant IDH2; a significant reduction is observed in DNA methylation, including 180 genes that have 20 or more hypomethylated differentially methylated cytosines (DMCs) following treatment. Enasidenib (100mg/kg bid) treatment of mice engrafted with Mx1-Cre IDH2R140QFlt3ITDAML cells markedly reduces 2-hydroxyglutarate (2-HG) levels consistent with on target inhibition. Enasidenib inhibits mutant IDH2-mediated 2-HG production[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 473.38 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C19H17F6N7O | ||||||||||||||||
CAS 号 | 1446502-11-9 | ||||||||||||||||
中文名称 | 恩西地平 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(105.62 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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