GNE-317CAS号： 1394076-92-6分子式： C19H22N6O3S 分子量： 414.48描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献
| 产品描述 | |
| 描述 |
GNE-317 is a potent, brain-penetrant PI3K inhibitor.
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| 纯度 |
＞98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 可溶性/溶解性 |
体外:
DMSO 47mg/mLwarming(113.39mM) Water <1mg>Ethanol <1mg> |
| 生物活性 | |
| 靶点 |
PI3K
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| In vitro(体外研究) |
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.
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| In vivo(体内研究) |
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.
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| 参考文献 | |
| 参考文献 |
[1] Salphati L, et al. Clin Cancer Res. 2012, 18(22):6239-6248 |
分子结构图
