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Enasidenib mesylate

Catalog No. T2346L CAS 1650550-25-6

Synonyms: AG221 mesylate, AG 221 mesylate, AG-221 mesylate

Enasidenib mesylate (AG-221 mesylate) is a potent and selective IDH2 mutase inhibitor that promotes differentiation of leukemia myeloid cells for the treatment of acute myeloid leukemia.

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Enasidenib mesylate, CAS 1650550-25-6

Pack Size	Availability	Price/USD
5 mg	In stock	$ 40.00
10 mg	In stock	$ 64.00
25 mg	In stock	$ 89.00
50 mg	In stock	$ 113.00
100 mg	In stock	$ 147.00
500 mg	In stock	$ 368.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.86%

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Description	Enasidenib mesylate (AG-221 mesylate) is a potent and selective IDH2 mutase inhibitor that promotes differentiation of leukemia myeloid cells for the treatment of acute myeloid leukemia.
In vitro	Reversing the effects of mutant IDH2 on DNA methylation in mutant stem/progenitor cells, Enasidenib mesylate (AG-221) induces differentiation and impairs self-renewal of IDH2-mutant leukemia cells. Simultaneous inhibition of Flt3ITD further enhances these effects. In the context of Enasidenib mesylate (AG-221) therapy, leukemic cells undergo differentiation, resulting in an increased CD11b+ population and a decreased c-Kit+ population in the peripheral blood at 2 weeks[2].
In vivo	In an IDH2-mutant acute myeloid leukemia (AML) primary xenograft mouse model, treatment with Enasidenib mesylate (AG-221) significantly improves survival[1]. Acting as a mutant IDH2 inhibitor, enasidenib remodels the epigenetic state of IDH2-mutant cells, inducing alterations in self-renewal/differentiation in an IDH2-mutant AML model in vivo. Enasidenib mesylate treatment at doses of 10 mg/kg or 100 mg/kg bid results in a substantial reduction in 2-HG levels in vivo, reaching 96.7% below pre-treatment levels.Furthermore, Enasidenib mesylate treatment restores megakaryocyte-erythroid progenitor (MEP) differentiation, which is suppressed by mutant IDH2 expression, as indicated by a mean MEP% increase from 39% in the vehicle group to 50% in the AG-221 group. The therapy also reverses the effects of mutant IDH2 on DNA methylation, with a significant reduction observed in DNA methylation, affecting 180 genes with 20 or more hypomethylated differentially methylated cytosines (DMCs) following treatment.Enasidenib mesylate therapy, particularly at a dose of 100 mg/kg bid, applied to mice engrafted with Mx1-Cre IDH2R140QFlt3ITD AML cells, markedly reduces 2-hydroxyglutarate (2-HG) levels, consistent with on-target inhibition. Enasidenib effectively inhibits the production of 2-HG mediated by mutant IDH2[2].

Synonyms	AG221 mesylate, AG 221 mesylate, AG-221 mesylate
Molecular Weight	569.48
Formula	C20H21F6N7O4S
CAS No.	1650550-25-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL(140.48 mM), Sonication is recommended.

References and Literature

1. Alan H. Shih, et al. AG-221, a Small Molecule 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. Blood 2014 124:437. 2. Exploring the Pathway: IDH Mutations and Metabolic Dysregulation in Cancer Cells: A Novel Therapeutic Target. MAY 29, 2015 3. Tong Z, Atsriku C, Yerramilli U, Wang X, Li Y, Reyes J, Fan B, Yang H, Hoffmann M, Surapaneni S. Absorption, distribution, metabolism and excretion of an isocitrate dehydrogenase-2 inhibitor enasidenib in rats and humans. Xenobiotica. 2018 Jan 22:1-11. doi: 10.1080/00498254.2018.1425511. [Epub ahead of print] PubMed PMID: 29320949. 4. Perl AE. The role of targeted therapy in the management of patients with AML. Blood Adv. 2017 Nov 14;1(24):2281-2294. doi: 10.1182/bloodadvances.2017009829. eCollection 2017 Nov 14. Review. PubMed PMID: 29296877; PubMed Central PMCID: PMC5737125.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Approved Drug Library FDA-Approved & Pharmacopeia Drug Library Approved Drug Library

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Keywords

Enasidenib mesylate 1650550-25-6 Metabolism Dehydrogenase AG221 mesylate AG 221 mesylate AG221 Mesylate AG-221 Mesylate AG 221 Mesylate Enasidenib Mesylate AG-221 mesylate inhibitor inhibit

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