Molecular Weight(MW): 473.38
Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme with IC50 of 12 nM.
Purity & Quality Control
Choose Selective Dehydrogenase Inhibitors
|Description||Enasidenib (AG-221) is a first-in-class, oral, potent, reversible, selective inhibitor of the IDH2 mutant enzyme with IC50 of 12 nM.|
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.
|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. 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.|
|In vitro||DMSO||94 mg/mL (198.57 mM)|
|Ethanol||94 mg/mL (198.57 mM)|
* 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.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03383575||Recruiting||Myelodysplastic Syndrome||M.D. Anderson Cancer Center|Celgene||January 7 2018||Phase 2|
|NCT02577406||Recruiting||Leukemia Myeloid|Isocitrate Dehydrogenase||Celgene||December 30 2015||Phase 3|
|NCT02677922||Recruiting||Leukemia Myeloid Acute||Celgene||June 3 2016||Phase 1|Phase 2|
|NCT03683433||Not yet recruiting||Acute Bilineal Leukemia|Acute Biphenotypic Leukemia|Chronic Myelomonocytic Leukemia|IDH2 Gene Mutation|Myelodysplastic Syndrome|Recurrent Acute Myeloid Leukemia|Refractory Acute Myeloid Leukemia||M.D. Anderson Cancer Center|National Cancer Institute (NCI)||February 28 2019||Phase 2|
|NCT01915498||Active not recruiting||Hematologic Neoplasms||Celgene|Agios Pharmaceuticals Inc.||August 27 2013||Phase 1|Phase 2|
|NCT02273739||Completed||Solid Tumor|Glioma|Angioimmunoblastic T-cell Lymphoma|Intrahepatic Cholangiocarcinoma|Chondrosarcoma||Celgene|Celgene Corporation||October 24 2014||Phase 1|Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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