Abemaciclib
Abemaciclib Basic information
- Product Name:
- Abemaciclib
- Synonyms:
-
- 2-methyl-1-((4-(6-(trifluoromethyl)pyridin-2-yl)-6-((2-(trifluoromethyl)pyridin-4-yl)amino)-1,3,5-triazin-2-yl)amino)propan-2-ol methanesulfonate
- 2-methyl-1-[[4-[6-(trifluoromethyl)-2-pyridinyl]-6-[[2-(trifluoromethyl)-4-
- Enasidenib Mesylate （API）
- AG-221 mesylate
- AG-221 salt
- Enasidenib mesylate，Abemaciclib
- Enasidenib Mesylate (AG-221 Mesylate)
- denib mesylate
- CAS:
- 1650550-25-6
- MF:
- C20H21F6N7O4S
- MW:
- 569.48
- Mol File:
- 1650550-25-6.mol
Abemaciclib Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO : ≥ 100 mg/mL (175.60 mM)
- form
- Solid
- color
- White to off-white
- InChIKey
- ORZHZQZYWXEDDL-UHFFFAOYSA-N
- SMILES
- S(O)(=O)(=O)C.N(C1=CC=NC(C(F)(F)F)=C1)C1N=C(NCC(O)(C)C)N=C(C2=CC=CC(C(F)(F)F)=N2)N=1
Abemaciclib Usage And Synthesis
Uses
Enasidenib mesylate is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes.
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 (10 mg/kg or 100 mg/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 (100 mg/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].
IC 50
IDH2
References
[1] Exploring the Pathway: IDH Mutations and Metabolic Dysregulation in Cancer Cells: A Novel Therapeutic Target. MAY 29, 2015
[2] 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.
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