GSK864 New

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP38009CAS No. ：1816331-66-4Purity：98%

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CAS No.	1816331-66-4	Cat. No.	BCP38009
Name	GSK864
Synonyms	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
Chemical Name
Formula	C30H31FN6O4	M. Wt	558.61
Purity	98%	Storage	Store at 4-8°C
Description	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.