Enasidenib (AG-221)

Catalog No.S8205 Batch:S820503

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Technical Data

Formula

C19H17F6N7O
Molecular Weight 473.38 CAS No. 1446502-11-9
Solubility (25°C)* In vitro DMSO 91 mg/mL (192.23 mM)
Ethanol 91 mg/mL (192.23 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme.
Targets
IDH2 [1]
(Cell-free assay)
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 (from reference)

Cell Assay:

[3]
  • Cell lines

    OE19 cells

  • Concentrations

    5 μM

  • Incubation Time

    24 h

  • Method

    Cells were treated with different concentrations of Enasidenib.
Animal Study:

[1]
  • Animal Models

    Murine models of IDH2-mutant leukemia

  • Dosages

    10 mg/kg or 100 mg/kg bid

  • Administration

    --

Selleck's Enasidenib (AG-221) has been cited by 16 publications

Dysregulated Lipid Synthesis by Oncogenic IDH1 Mutation Is a Targetable Synthetic Lethal Vulnerability [ Cancer Discov, 2023, 13(2):496-515] PubMed: 36355448
ABCC1 and glutathione metabolism limit the efficacy of BCL-2 inhibitors in acute myeloid leukemia [ Nat Commun, 2023, 14(1):5709] PubMed: 37726279
ABCC1 and glutathione metabolism limit the efficacy of BCL-2 inhibitors in acute myeloid leukemia [ Nat Commun, 2023, 14(1):5709] PubMed: 37726279
Succinate mediates inflammation-induced adrenocortical dysfunction [ Elife, 2023, 12e83064] PubMed: 37449973
Phospholipid metabolic adaptation promotes survival of IDH2 mutant acute myeloid leukemia cells [ Cancer Sci, 2023, 10.1111/cas.15994] PubMed: 37882467
Proteogenomics refines the molecular classification of chronic lymphocytic leukemia [ Nat Commun, 2022, 13(1):6226] PubMed: 36266272
Proteogenomics refines the molecular classification of chronic lymphocytic leukemia [ Nat Commun, 2022, 13(1):6226] PubMed: 36266272
Regulatory chromatin rewiring promotes metabolic switching during adaptation to oncogenic receptor tyrosine kinase inhibition [ Oncogene, 2022, 41(43):4808-4822] PubMed: 36153371
Lysine acetylation restricts mutant IDH2 activity to optimize transformation in AML cells [ Mol Cell, 2021, S1097-2765(21)00507-4] PubMed: 34289383
Mutant Idh2 cooperates with a NUP98-HOXD13 fusion to induce early immature thymocyte precursor ALL [ Cancer Res, 2021, canres.1027.2021] PubMed: 34321240

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.