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。

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.

Solid

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

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.

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

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[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.

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