Enasidenib (AG-221)

Catalog No.S8205

Enasidenib (AG-221) Chemical Structure

Molecular Weight(MW): 473.38

AG-221(Enasidenib) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme with IC50 of 12 nM.

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Biological Activity

Description AG-221(Enasidenib) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme with IC50 of 12 nM.
Targets
IDH2 [1]
12 nM
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. Clinical trials combining IDH2 inhibitors with other targeted AML therapies are warranted in order to increase therapeutic efficacy[1].

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (211.24 mM)
Ethanol 100 mg/mL (211.24 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 473.38
Formula

C19H17F6N7O

CAS No. 1446502-11-9
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Dehydrogenase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID