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Enasidenib is a potent and selective IDH2 (Isocitrate dehydrogenase 2) inhibitor with potential anticancer activity, with IC50s of 100 and 400 nM against IDH2R140Q and IDH2R172K, respectively. The inhibition of mutant IDH2 and its neoactivity is therefore a potential therapeutic treatment for cancer.
Enasidenib (AG-221) reverses the effects of mutant IDH2 on DNA methylation in mutant stem/progenitor cells. 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.
| Molecular Weight | 473.37 |
| Formula | C19H17F6N7O |
| CAS Number | 1446502-11-9 |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Maria Paola Martelli, et al. Enasidenib and ivosidenib in AML
[2] No authors listed. Enasidenib
[3] No authors listed. Enasidenib
[4] Eytan M Stein, et al. Enasidenib in mutant IDH2 relapsed or refractory acute myeloid leukemia
| Related Isocitrate Dehydrogenase (IDH) Products |
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| AGI-6780
AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM. |
| BAY-1436032
BAY1436032 is a novel pan-mutant IDH1 inhibitor, it specifically inhibits R-2HG production and colony growth, and induces myeloid differentiation of AML cells. |
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| Ivosidenib
Ivosidenib is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. |
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