GNE-317|cas 1394076-92-6|DC Chemicals

GNE-317|cas 1394076-92-6|DC Chemicals

GNE-317 is a potent, brain-penetrant PI3K inhibitor.

Product Name: GNE-317 |Catalog Number:  DC8410 | cas: 1394076-92-6 | Other names: GNE-317,GNE 317,GNE317 | Chemical name：5-(6-(3-methoxyoxetan-3-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine | Molecule Formula: C19H22N6O3S | MW: 414.48

GNE-317 is not a substrate of P-gp or BCRP transporter in transfected Madin-Darby canine kidney (MDCK) cells. Binding of GNE-317 to plasma proteins exhibits a free fraction of 14.9 % in mouse plasma, and binding to brain tissues is higher, with a free fraction of 5.4%. GNE-317 shows cytostasis but no cell death to U87 cells.[1]GNE-317 (40 mg/kg, p.o.) markedly inhibits the PI3K pathway in mouse brain, causing 40% to 90% suppression of the pAkt and pS6 signals up to 6-hour postdose. GNE-317 (40 mg/kg, p.o.) is efficacious in the U87 and GS2 orthotopic models, achieving tumor growth inhibition of 90% and 50%, respectively. In the GBM10 tumor model, GNE-317 (30 mg/kg, p.o.; 40 mg/kg the first 2 weeks) extends the survival of mice from a median of 55.5 to 75 days.

For research and scientific purpose only, not for human use.