Enasidenib mesylate(AG-221)

¥380.00¥1,500.00

CAS 号: 1650550-25-6
货号: MB4358

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

运输条件:2~8℃运输

生物活性

产品描述

Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of theIDH2mutant 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 IDH2R140QFlt3ITDAML 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

【注意】

●我司产品为非无菌包装,若用于细胞培养,请提前做预处理,除去热原细菌,否则会导致染菌。

●部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,以上数据仅供参考交流研究之用。

我司所售出产品仅供于科研研究用途(非临床科研研究),每次销售产品行为都适用于我司网上所列明的通用销售条款

规格

5mg, 25mg

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