Chemical Structure : IDH2 R140Q inhibitor CP-17
CAS No.:
1111233-06-7
IDH2 R140Q inhibitor CP-17
Catalog No.: PC-20532Not For Human Use, Lab Use Only.
IDH2 R140Q inhibitor CP-17 is a potent, selective inhibitor of IDH2 R140Q mutation with IC50 of 40.75 nM, 50-fold selectivity over wild-type IDH1/2.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
IDH2 R140Q inhibitor CP-17 is a potent, selective inhibitor of IDH2 R140Q mutation with IC50 of 40.75 nM, 50-fold selectivity over wild-type IDH1/2.
CP-17 binds to an allosteric site located within the interface of IDH2/R140Q homodimer, stabilizing an open conformation of the active site.
CP-17 (3 uM) significantly inhibited the GM-CSF-independent growth of TF-1(IDH2/R140Q) cells but had no obvious effect on the proliferation of TF-1(WT) cells.
CP-17 showed a dose-dependent inhibition against intracellular D-2-HG production by TF-1(IDH2/R140Q) cells with IC50 of 141.4 nM.
CP-17 (1 and 3 uM) induced a dose-dependent decrease in histone methylation, thus restored the differentiation of TF-1(IDH2/R140Q) cells.
Physicochemical Properties
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M.Wt
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448.95
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Formula
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C25H25ClN4O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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O=C(NC1=CC=C(N2CCCC2)C(NC(NC3=CC(Cl)=CC=C3C)=O)=C1)C4=CC=CC=C4
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References
1. Jiao Chen, et al. Cell Commun Signal. 2020 Apr 3;18(1):55.
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