GSK864 新

参考资料仅供科学研究，不可用于个人用途。

货号：BCP38009CAS号：1816331-66-4纯度：98%

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CAS号	1816331-66-4	货号	BCP38009
中文名	GSK864
英文名	GSK864
中文别名
英文别名	GSK-864;GSK 864;
SMILES	CC1=CC(=CC(=C1OC)C)NC(=O)C2=NN(C3=C2CN(CC3(C)C(=O)N)C(=O)C4=CC=CN4)CC5=CC=C(C=C5)F
化学名称
分子式	C30H31FN6O4	分子量	558.61
纯度	98%	配送	惯例下常温包邮
产品描述	GSK864 is a potent and selective inhibitor of mutant IDH1. GSK864 inhibits IDH1 mutants R132C/R132H/R132G with IC50 values of 9/15/17 nM, respectively, and is moderately selective over wild-type IDH1 and IDH2 mutants/wild-type. Treatment of R132C IDH1 mutant HT-1080 cells for 24 hours with GSK864 results in a dose-dependent reduction of 2-hydroxyglutarate (2-HG), which is not observed with GSK990, a structurally similar compound which is inactive as an IDH1 inhibitor. GSK864 has been shown to be selective in vitro for IDH1 over other classes of proteins (7TMs, ion channels, kinases) and chemoproteomic studies with GSK321, an analog of GSK864, confirm selective binding of IDH1 by this chemical series. GSK864 has a pharmacokinetic profile suitable for in vivo studies.