1. Metabolic Enzyme/Protease
  2. Isocitrate Dehydrogenase (IDH)

Enasidenib (Synonyms: AG-221)

Cat. No.: HY-18690 Purity: 99.91%
Data Sheet SDS Handling Instructions

Enasidenib is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.

For research use only. We do not sell to patients.
Enasidenib Chemical Structure

Enasidenib Chemical Structure

CAS No. : 1446502-11-9

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Description

Enasidenib is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.

IC50 & Target

IDH2[1]

In Vitro

Enasidenib (AG-221) reverses the effects of mutant IDH2 on DNA methylation in mutant stem/progenitor cells. Enasidenib induces differentiation and impairs self-renewal of IDH2-mutant leukemia cells, effects that are further enhanced by simultaneous inhibition of Flt3ITD. Enasidenib (AG-221) therapy induces differentiation of leukemic cells, with an increase in the CD11b+ population and a decrease in the c-Kit+ population in the peripheral blood at 2wks[2].

In Vivo

Treatment with Enasidenib (AG-221) significantly improves survival in an IDH2-mutant acute myeloid leukemia (AML) primary xenograft mouse model[1]. Enasidenib (AG-221), a 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. Enasidenib treatment (10mg/kg or 100mg/kg bid) leads to a reduction in 2-HG in vivo (96.7% below pre-treatment levels). Moreover, Enasidenib treatment restores megakaryocyte-erythroid progenitor (MEP) differentiation that is suppressed by mutant IDH2 expression (mean MEP% mean, 39% Veh vs 50% AG-221). Enasidenib therapy reverses the effects of mutant IDH2; a significant reduction is observed in DNA methylation, including 180 genes that have 20 or more hypomethylated differentially methylated cytosines (DMCs) following treatment. Enasidenib (100mg/kg bid) treatment of mice engrafted with Mx1-Cre IDH2R140QFlt3ITD AML cells markedly reduces 2-hydroxyglutarate (2-HG) levels consistent with on target inhibition. Enasidenib inhibits mutant IDH2-mediated 2-HG production[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01915498 Celgene|Agios Pharmaceuticals, Inc. Hematologic Neoplasms August 27, 2013 Phase 1|Phase 2
NCT02273739 Celgene|Celgene Corporation Solid Tumor|Glioma|Angioimmunoblastic T-cell Lymphoma|Intrahepatic Cholangiocarcinoma|Chondrosarcoma October 24, 2014 Phase 1|Phase 2
NCT02443168 Celgene Corporation|Celgene Healthy Volunteers May 2015 Phase 1
NCT02387866 Celgene Corporation|Celgene Healthy March 2015 Phase 1
NCT02677922 Celgene Leukemia, Myeloid, Acute June 3, 2016 Phase 1|Phase 2
NCT02577406 Celgene Leukemia, Myeloid|Isocitrate Dehydrogenase December 30, 2015 Phase 3
NCT02632708 Agios Pharmaceuticals, Inc.|Celgene Corporation Newly Diagnosed Acute Myeloid Leukemia (AML)|Untreated AML|AML Arising From Myelodysplastic Syndrome (MDS)|AML Arising From Antecedent Hematologic Disorder (AHD)|AML Arising After Exposure to Genotoxic Injury December 2015 Phase 1
NCT03013998 Beat AML, LLC Previously Untreated Acute Myeloid Leukemia November 2016 Phase 1|Phase 2
NCT01915498 Celgene|Agios Pharmaceuticals, Inc. Hematologic Neoplasms August 27, 2013 Phase 1|Phase 2
NCT02273739 Celgene|Celgene Corporation Solid Tumor|Glioma|Angioimmunoblastic T-cell Lymphoma|Intrahepatic Cholangiocarcinoma|Chondrosarcoma October 24, 2014 Phase 1|Phase 2
NCT02443168 Celgene Corporation|Celgene Healthy Volunteers May 2015 Phase 1
NCT02387866 Celgene Corporation|Celgene Healthy March 2015 Phase 1
NCT02677922 Celgene Leukemia, Myeloid, Acute June 3, 2016 Phase 1|Phase 2
NCT02577406 Celgene Leukemia, Myeloid|Isocitrate Dehydrogenase December 30, 2015 Phase 3
NCT02632708 Agios Pharmaceuticals, Inc.|Celgene Corporation Newly Diagnosed Acute Myeloid Leukemia (AML)|Untreated AML|AML Arising From Myelodysplastic Syndrome (MDS)|AML Arising From Antecedent Hematologic Disorder (AHD)|AML Arising After Exposure to Genotoxic Injury December 2015 Phase 1
NCT03013998 Beat AML, LLC Previously Untreated Acute Myeloid Leukemia November 2016 Phase 1|Phase 2
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References
Molecular Weight

473.38

Formula

C₁₉H₁₇F₆N₇O

CAS No.

1446502-11-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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