1650550-25-6
1650550-25-6 structure
- Name: Enasidenib mesylate
- Chemical Name: Enasidenib mesylate
- CAS Number: 1650550-25-6
- Molecular Formula: C20H21F6N7O4S
- Molecular Weight: 569.481
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Isocitrate Dehydrogenase (IDH)
- Create Date: 2018-05-25 15:09:55
- Modify Date: 2024-01-09 08:16:27
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Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.
| Name | Enasidenib mesylate |
|---|---|
| Synonyms |
Enasidenib mesylate
AG-221 mesylate UF6PC17XAV CC-90007 2-Methyl-1-[(4-[6-(trifluoromethyl)-2-pyridinyl]-6-{[2-(trifluoromethyl)-4-pyridinyl]amino}-1,3,5-triazin-2-yl)amino]-2-propanol methanesulfonate (1:1) 2-Propanol, 2-methyl-1-[[4-[6-(trifluoromethyl)-2-pyridinyl]-6-[[2-(trifluoromethyl)-4-pyridinyl]amino]-1,3,5-triazin-2-yl]amino]-, methanesulfonate (1:1) (salt) UNII:UF6PC17XAV Enasidenib (mesylate) |
| Description | Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes. |
|---|---|
| Related Catalog | |
| 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 2 wks[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 (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 IDH2R140QFlt3ITD AML cells markedly reduces 2-hydroxyglutarate (2-HG) levels consistent with on target inhibition. Enasidenib inhibits mutant IDH2-mediated 2-HG production[2]. |
| References |
| Molecular Formula | C20H21F6N7O4S |
|---|---|
| Molecular Weight | 569.481 |
| Exact Mass | 569.127991 |
| Storage condition | 2-8℃ |