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Enasidenib

Catalog No. T2346 CAS 1446502-11-9

Synonyms: AG-221

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.

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Enasidenib, CAS 1446502-11-9

Pack Size	Availability	Price/USD
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

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Purity: 100%

Purity: 99.8%

Purity: 99.45%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

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

Storage

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

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 100 mg/mL (211.25 mM)

DMSO: 50 mg/mL (105.62 mM)

References and Literature

1. Alan H. Shih, et al. Blood. 2014, 124:437. 2. Kate Ellwood-Yen, et al. AACR. 2014, 74(19 Sup.):3116.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Targeted Therapy Drug Library Bioactive Compound Library Clinical Compound Library Metabolism Compound Library

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Keywords

Enasidenib 1446502-11-9 Metabolism Dehydrogenase Isocitrate Dehydrogenase (IDH) AG 221 inhibit AG221 Inhibitor AG-221 inhibitor

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