IDH2 R140Q inhibitor CP-17

Chemical Structure : IDH2 R140Q inhibitor CP-17

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货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	448.95
分子式	C25H25ClN4O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	O=C(NC1=CC=C(N2CCCC2)C(NC(NC3=CC(Cl)=CC=C3C)=O)=C1)C4=CC=CC=C4

参考文献

1. Jiao Chen, et al. Cell Commun Signal. 2020 Apr 3;18(1):55.