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  • AG-221
    • AG221,AG 221
    货号: abs810199
    CAS号: 1446502-11-9
    分子式: C19H17F6N7O
    分子量: 473.14
    产品说明书
    分享:
    货号-规格 货期 价格 数量
    abs810199-5mg 1-2周 ¥933.00
    - +
    abs810199-10mg 1-2周 ¥1583.00
    - +
    abs810199-50mg 1-2周 ¥5707.00
    - +
    abs810199-100mg 1-2周 ¥8283.00
    - +
    大包装询价
    产品描述
    描述
    AG-221 is an orally available, selective, potent inhibitor of the mutated IDH2 protein.
    纯度
    >98%
    储存/保存方法
    store at -20℃ for one year(Powder);
    in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.
    基本信息
    别名
    AG221,AG 221
    外观
    Powder
    可溶性/溶解性
    DMSO 100 mg/mL (211.24 mM)

    Ethanol 100 mg/mL (211.24 mM)


    生物活性
    靶点
    Isocitrate Dehydrogenase (IDH)
    In vitro(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 2wks.
    In vivo(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 (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 IDH2R140QFlt3ITD AML cells markedly reduces 2-hydroxyglutarate (2-HG) levels consistent with on target inhibition. Enasidenib inhibits mutant IDH2-mediated 2-HG production.
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