| References: |
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.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 the detailed information of GNE-317, the solubility of GNE-317 in water, the solubility of GNE-317 in DMSO, the solubility of GNE-317 in PBS buffer, the animal experiment (test) of GNE-317, the cell expriment (test) of GNE-317, the in vivo, in vitro and clinical trial test of GNE-317, the EC50, IC50,and affinity,of GNE-317, For the detailed information of GNE-317, the solubility of GNE-317 in water, the solubility of GNE-317 in DMSO, the solubility of GNE-317 in PBS buffer, the animal experiment (test) of GNE-317, the cell expriment (test) of GNE-317, the in vivo, in vitro and clinical trial test of GNE-317, the EC50, IC50,and affinity,of GNE-317, Please contact DC Chemicals. |
