Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 39.00 | |
10 mg | In stock | $ 64.00 | |
25 mg | In stock | $ 94.00 | |
50 mg | In stock | $ 113.00 | |
100 mg | In stock | $ 147.00 | |
200 mg | In stock | $ 218.00 | |
500 mg | In stock | $ 369.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 43.00 |
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. |
Targets&IC50 | IDH2 (R172K):400 nM, IDH2 (R140Q):100nM |
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 | AG-221 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 AG-221 treatment[2]. AG-221 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]. |
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. |
Synonyms | AG-221 |
Molecular Weight | 473.38 |
Formula | C19H17F6N7O |
CAS No. | 1446502-11-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 100 mg/mL (211.25 mM)
DMSO: 50 mg/mL (105.62 mM)
You can also refer to dose conversion for different animals. More
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Enasidenib 1446502-11-9 Metabolism Dehydrogenase Isocitrate Dehydrogenase (IDH) AG 221 inhibit AG221 Inhibitor AG-221 inhibitor