Enasidenib

SKU: orb1305629

Description

Enasidenib (AG-221) is a small molecule inhibitor that selectively targets mutant IDH2 enzymes. It is used in research to study its effects in models of acute myeloid leukemia (AML), both in vitro and in vivo, for its potential to induce cellular differentiation.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1446502-11-9
• MW: 473.38
• Purity: >98%
• Formula: C₁₉H₁₇F₆N₇O
• SMILES: CC(C)(O)CNc1nc(Nc2ccnc(c2)C(F)(F)F)nc(n1)-c1cccc(n1)C(F)(F)F
• Target: Dehydrogenase (GAPDH, GPDH, IMPDH, PHGDH, LDH, DHODH, ALDH, GDH, IDH, UGDH, DPD, DHPDH, KGDH, PDH, and MDH)
• Solubility: Soluble in DMSO (up to 25 mg/ml)

Bioactivity

• Target IC50:
  IDH2 (R172K):400 nM|IDH2 (R140Q):100nM
• In Vivo:
  Enasidenib 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 Enasidenib treatment. Enasidenib 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.
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AG-221

Compound Identifiers

PubChem CID

89683805