GSK864 (C09-1134-712)

GSK864 is an isocitrate dehydrogenase 1 ( IDH1 ) mutant inhibitor; inhibits IDH1 mutants R132C, R132H, and R132G with IC 50 values of 8.8, 15.2 and 16.6 nM.In VitroGSK864 inhibits 2-HG production in R132C IDH1 mutant HT1080 fibrosarcoma cells with an EC 50 of 320 nM by LCMS/MS analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoFollowing intraperitoneal (IP) administration in CD-1 mice, significant concentrations of GSK864 are maintained in peripheral blood samples of mice for up to 24 hours. Analysis of BM cells for expression of markers of early differentiation reveals slightly increased numbers of huCD45 + CD38 + cells in R132C or R132H IDH1 mutant engrafted mice treated with GSK864 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:IC50: 8.8 nM (IDH1 mutants R132C), 15.2 nM (IDH1 mutants R132H), 16.6 nM (IDH1 mutants R132G). Specification: 0.99 Molecular Formula: C30H31FN6O4 Molecular Weight: 558.6 PubChem CID: 91864701 Isomeric SMILES: CC1=CC(=CC(=C1OC)C)NC(=O)C2=NN(C3=C2CN(C[C@]3(C)C(=O)N)C(=O)C4=CC=CN4)CC5=CC=C(C=C5)F