CP-17
CP-17 is a potent and selective IDH2/R140Q inhibitor with an IC50 of 40.75 nM. CP-17 exhibits excellent selectivity of >55-fold against the wild-type IDH2. CP-17 exhibits robust D-2-HG suppression activity in TF-1 (IDH2/R140Q) cells and reverses the cellular differentiation block induced by the R140Q mutation. CP-17 can be used for acute myeloid leukemia (AML) research.
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- CAS No.: 1111233-06-7
- Formule: C25H25ClN4O2
- Masse moléculaire:448.94
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
IDH2-R140Q 40.75 nM (IC50) |
Chemical Information
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CAS No. 1111233-06-7
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Masse moléculaire 448.94
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Formule C25H25ClN4O2
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SMILES
O=C(NC1=CC(Cl)=CC=C1C)NC2=CC(NC(C3=CC=CC=C3)=O)=CC=C2N4CCCC4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Genotoxicity/Mutagenicity Study
The bacterial reverse mutation assay detects point mutations that restore amino-acid prototrophy in auxotrophic Salmonella typhimurium or Escherichia coli tester strains; after exposure to a test article, mutagenic activity is read out as an increased number of revertant colonies on minimal agar compared with the vehicle control. The assay uses tester strains with different mutation targets so that base-substitution and frameshift mutagens can be detected, and testing is performed with and without exogenous mammalian metabolic activation because some chemicals require biotransformation to become mutagenic.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)