Enasidenib mesylate(AG-221)
分子式：C20H21F6N7O4S 分子量：569.48
简介：Enasidenib mesylate 是一种有效的，可口服的，可逆的，选择性的 IDH2 突变酶抑制剂。
物理性状及指标：
外观：……………………粉末
溶解性：…………………DMSO : ≥ 100 mg/mL(175.60 mM)
含量：……………………>98%
储存条件：-20℃，避光防潮密闭干燥
生物活性
产品描述
Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.
体外研究
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 2 wks.
体内研究
Treatment with enasidenib (AG-221) significantly improves survival in an IDH2-mutant acute myeloid leukemia (AML) primary xenograft mouse model. 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 (10 mg/kg or 100 mg/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 (100 mg/kg bid) treatment of mice engrafted with Mx1-Cre IDH2R140QFlt3ITD AML cells markedly reduces 2-hydroxyglutarate (2-HG) levels consistent with on target inhibition. Enasidenib inhibits mutant IDH2-mediated 2-HG production.
用途及描述：科研试剂，广泛应用于分子生物学，药理学等科研方面，严禁用于人体。
储液配置：按表中溶解性配置；如溶解困难，可以通过快速搅拌，超声或温和加热（在45-60°C下水浴）。液体稳定性报道的很少，建议现配现用，如需储存，建议：-20℃1-3月；-80℃ 3-6月。
浓度/体积/质量
1 mg
5 mg
10 mg
1 mM
1.7560 mL
8.7799 mL
17.5599 mL
5 mM
0.3512 mL
1.7560 mL
3.5120 mL
10 mM
0.1756 mL
0.8780 mL
1.7560 mL
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