| Name | Enasidenib |
| Description | Enasidenib (AG-221) is an orally available inhibitor of specific mutant forms of the mitochondrial enzyme isocitrate dehydrogenase type 2 (IDH2), with potential antineoplastic activity. |
| Kinase Assay | Untranslated region-mediated luciferase reporter expression: HEK293 cells are transfected with a GEMS reporter vector that contains the luciferase open-reading frame flanked by and under post-transcriptional control of the BMI-1 5′ and 3′ UTRs. The resulting stable cells (F8) are treated with PTC-209 or vehicle control overnight, and then luciferase reporter activity is determined using Bright-Glo assays. The assays are run in triplicate for each point, and the percentage of inhibition was calculated against vehicle control. |
| In vitro | The compound has been demonstrated to reduce 2-HG levels by >90% and reverse histone and deoxyribonucleic acid (DNA) hypermethylation in vitro, and to induce differentiation in leukemia cell models[2]. |
| In vivo | Enasidenib is able to potently reduce 2HG found in the bone marrow, plasma and urine of engrafted mice. Treatment also induced a dose dependent, statistically significant, survival benefit. A proliferative burst of the human specific CD45+ blast cells is followed by cellular differentiation as measured by the expression of CD11b, CD14 and CD15 and cell morphology after Enasidenib treatment[2]. Enasidenib treatment also restores megakaryocyte-erythroid progenitor (MEP) differentiation that is suppressed by mutant IDH2 expression and reverses the effects of mutant IDH2 on DNA methylation in mutant stem/progenitor cells. Clinicalal trials combining IDH2 inhibitors with other targeted AML therapies are warranted in order to increase therapeutic efficacy[1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 100 mg/mL (211.25 mM), Sonication is recommended.
DMSO : 245 mg/mL (517.55 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (10.56 mM), Sonication is recommended.
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| Keywords | IsocitrateDehydrogenase(IDH) | IsocitrateDehydrogenase | Isocitrate Dehydrogenase (IDH) | Isocitrate Dehydrogenase | Inhibitor | inhibit | IDH2 | IDH | Enasidenib | AG221 | AG 221 |
| Inhibitors Related | Disulfiram | Mycophenolate Mofetil | Rotenone | Ribavirin | 18β-Glycyrrhetinic acid | Benzyl alcohol | 2-Methylaminoethanol | Methotrexate disodium | Dimethyl malonate | Isomalt | D-Mannitol | Ethyl potassium malonate |
| Related Compound Libraries | Bioactive Compound Library | Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | NO PAINS Compound Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
