GNE 317
GNE-317
CAS: 1394076-92-6
Molecular Formula: C19H22N6O3S
GNE 317 - Names and Identifiers
GNE 317 - Physico-chemical Properties
| Molecular Formula | C19H22N6O3S |
| Molar Mass | 414.48 |
| Solubility | DMSO: 20 mg/mL |
| Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| In vitro study | 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. |
| In vivo study | 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. |
GNE 317 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.413 ml | 12.063 ml | 24.127 ml |
| 5 mM | 0.483 ml | 2.413 ml | 4.825 ml |
| 10 mM | 0.241 ml | 1.206 ml | 2.413 ml |
| 5 mM | 0.048 ml | 0.241 ml | 0.483 ml |
Last Update：2024-01-02 23:10:35
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