Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Enasidenib mesylate (AG-221 mesylate) 是一种具有有效性和选择性的 IDH2 突变酶抑制剂,可促进白血病成髓细胞的分化,可用于治疗急性髓系白血病。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 538 | 现货 | ||
10 mg | ¥ 787 | 现货 | ||
25 mg | ¥ 1,290 | 现货 | ||
50 mg | ¥ 1,930 | 现货 | ||
100 mg | ¥ 2,880 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 673 | 现货 |
产品描述 | Enasidenib mesylate (AG-221 mesylate) is a potent and selective IDH2 mutase inhibitor that promotes differentiation of leukemia myeloid cells for the treatment of acute myeloid leukemia. |
体外活性 | Reversing the effects of mutant IDH2 on DNA methylation in mutant stem/progenitor cells, Enasidenib mesylate (AG-221) induces differentiation and impairs self-renewal of IDH2-mutant leukemia cells. Simultaneous inhibition of Flt3ITD further enhances these effects. In the context of Enasidenib mesylate (AG-221) therapy, leukemic cells undergo differentiation, resulting in an increased CD11b+ population and a decreased c-Kit+ population in the peripheral blood at 2 weeks[2]. |
体内活性 | In an IDH2-mutant acute myeloid leukemia (AML) primary xenograft mouse model, treatment with Enasidenib mesylate (AG-221) significantly improves survival[1]. Acting as a mutant IDH2 inhibitor, enasidenib remodels the epigenetic state of IDH2-mutant cells, inducing alterations in self-renewal/differentiation in an IDH2-mutant AML model in vivo. Enasidenib mesylate treatment at doses of 10 mg/kg or 100 mg/kg bid results in a substantial reduction in 2-HG levels in vivo, reaching 96.7% below pre-treatment levels.Furthermore, Enasidenib mesylate treatment restores megakaryocyte-erythroid progenitor (MEP) differentiation, which is suppressed by mutant IDH2 expression, as indicated by a mean MEP% increase from 39% in the vehicle group to 50% in the AG-221 group. The therapy also reverses the effects of mutant IDH2 on DNA methylation, with a significant reduction observed in DNA methylation, affecting 180 genes with 20 or more hypomethylated differentially methylated cytosines (DMCs) following treatment.Enasidenib mesylate therapy, particularly at a dose of 100 mg/kg bid, applied to mice engrafted with Mx1-Cre IDH2R140QFlt3ITD AML cells, markedly reduces 2-hydroxyglutarate (2-HG) levels, consistent with on-target inhibition. Enasidenib effectively inhibits the production of 2-HG mediated by mutant IDH2[2]. |
别名 | AG221 mesylate, AG 221 mesylate, 恩西地平甲磺酸盐, AG-221 mesylate |
分子量 | 569.48 |
分子式 | C20H21F6N7O4S |
CAS No. | 1650550-25-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 80 mg/mL(140.48 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.756 mL | 8.7799 mL | 17.5599 mL | 43.8997 mL |
5 mM | 0.3512 mL | 1.756 mL | 3.512 mL | 8.7799 mL | |
10 mM | 0.1756 mL | 0.878 mL | 1.756 mL | 4.39 mL | |
20 mM | 0.0878 mL | 0.439 mL | 0.878 mL | 2.195 mL | |
50 mM | 0.0351 mL | 0.1756 mL | 0.3512 mL | 0.878 mL | |
100 mM | 0.0176 mL | 0.0878 mL | 0.1756 mL | 0.439 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Enasidenib mesylate 1650550-25-6 Metabolism Dehydrogenase AG221 mesylate AG 221 mesylate AG221 Mesylate AG-221 Mesylate AG 221 Mesylate 恩西地平甲磺酸盐 Enasidenib Mesylate AG-221 mesylate Inhibitor inhibitor inhibit