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AG-221

AG-221

价格: 889

品牌:爱必信

供货周期: 一周

货号:abs810199

规格:>98%

CAS:1446502-11-9

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抑制剂描述:

产品名称:AG-221

产品别名:见爱必信官网

英文别名:AG-221

靶点:IDH

CAS:1446502-11-9

纯度:>98%

外观:见爱必信官网

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.

描述:AG-221 is an orally available, selective, potent inhibitor of the mutated IDH2 protein.

溶解性:DMSO 100 mg/mL (211.24 mM)
Ethanol 100 mg/mL (211.24 mM)

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.

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.

产品信息订购:

  产品货号   产品名称   规格 价格 大包装及货期
  abs810199   AG-221   5mg   889.00   立即咨询
  abs810199   AG-221   10mg   1508.00   立即咨询
  abs810199   AG-221   50mg   5435.00   立即咨询
  abs810199   AG-221   100mg   7889.00   立即咨询

产品更多信息请进入爱必信网站咨询




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