
Immunoway/AG-221(Enasidenib)/10mg 50mg 100mg/MC0921
市场价:
¥6000.00
美元价:
3000.00
联系Q Q:
3392242852
电话号码:
4000-520-616
电子邮箱:
info@ebiomall.com
商品介绍
AG-221(Enasidenib)
- Catalog No.:MC0921
- Data Sheet
- MSDS
- Support
- Description
- References ( 0 )
- Protocol
- CasNo:
- 1446502-11-9
- MolecularFormula:
- C19H17F6N7O
- Purity:
- >98%
- Target:
- Isocitrate Dehydrogenase (IDH)
- IC50:
- No data
- 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 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[2].
- In Vivo:
- Treatment with Enasidenib (AG-221) significantly improves survival in an IDH2-mutant acute myeloid leukemia (AML) primary xenograft mouse model[1]. 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
- Fields:
- AG-221 is an orally available, selective, potent inhibitor of the mutated IDH2 protein.
- Specificity:
- Target: Isocitrate Dehydrogenase (IDH) . Fields: AG-221 is an orally available, selective, potent inhibitor of the mutated IDH2 protein.
- Source:
- Rabbit
- Dilution:
- WB 1:500-2000
- Concentration:
- >98%
- Storage Stability:
- 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
- Other Name:
- AG221,AG 221
- MolecularWeight(Da):
- 473.14
- References:
- [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 Inhibit
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