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Enasidenib

(Synonyms: 恩西地平; AG-221)

目录号: PL14811 纯度: ≥99%

Enasidenib是可口服，可逆，选择性的 IDH2 突变酶抑制剂，抑制IDH2^R140Q 和 IDH2^R172K 的 IC50 分别为100 和 400 nM。

CAS No. :1446502-11-9

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PL14811-1 mL x 10 mM (in DMSO)		¥588.00	请登录

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中文名称	Enasidenib
中文别名	Enasidenib 抑制剂;Enasidenib（AG-221）抑制剂;Enasidenib;恩西地平
英文名称	Enasidenib
英文别名	AG-221;Enasidenib;AG221;Enasidenib mesylate;IDHIFA;3T1SS4E7AG;2-Methyl-1-(4-(6-(trifluoromethyl)pyridin-2-yl)-6-(2-(trifluoromethyl)pyridin-4-ylamino)-1,3,5-triazin-2-ylamino)propan-2-ol;2-methyl-1-((4-(6-(trifluoromethyl)pyridin-2-yl)-6-((2-(trifluoromethyl)pyridin-4-yl)amino)-1,3,5-triazin-2-yl)amino)propan-2-ol;2-Propanol, 2-methyl-1-((4-(6-(trifluoromethyl)-2-pyridinyl)-6-((2-(trifluoromethyl)-4-pyridinyl)amino)-1,3,5-triazin-2-yl)amino)-;En
Cas No.	1446502-11-9
分子式	C₁₉H₁₇F₆N₇O
分子量	473.38
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	Enasidenib是可口服，可逆，选择性的 IDH2 突变酶抑制剂，抑制IDH2^R140Q 和 IDH2^R172K 的 IC50 分别为100 和 400 nM。

产品详情

Enasidenib是可口服，可逆，选择性的 IDH2 突变酶抑制剂，抑制IDH2^R140Q 和 IDH2^R172K 的 IC₅₀ 分别为100 和 400 nM。

生物活性

Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC 50 s of 100 and 400 nM against IDH2 and IDH2, respectively.

性状

Solid

IC50 & Target[1][2]

IC50: 100 nM (IDH2), 400 nM (IDH2)

体外研究(In Vitro)

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 Flt3. 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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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 b

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Exploring the Pathway: IDH Mutations and Metabolic Dysregulation in Cancer Cells: A Novel Therapeutic Target. MAY 29, 2015
[2]. Alan H. Shih, et al. AG-221, a Small Molecule 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. Blood 2014 124:437.

溶解度数据	In Vitro: DMSO : 50 mg/mL (105.62 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Enasidenib

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