GNE-317
| CAS号 | 1394076-92-6 | 货号 | BCP23939 |
| 中文名 | GNE-317 | ||
| 英文名 | GNE-317 | ||
| 中文别名 | |||
| 英文别名 | GNE317; GNE 317; | ||
| 分子式 | C18H20N6O3S | 分子量 | 400.45 |
| 生物活性 | GNE-317 is a potent and selective PI3K inhibitor with potential anticncer activity. GNE-317 targets the PI3K pathway and can cross the Blood–Brain Barrier. GNE-317 was identified as having physicochemical properties predictive of low efflux by P-gp and BCRP. Studies in transfected MDCK cells showed that GNE-317 was not a substrate of either transporter. GNE-317 markedly inhibited the PI3K pathway in mouse brain, causing 40% to 90% suppression of the pAkt and pS6 signals up to 6-hour postdose. GNE-317 was efficacious in the U87, GS2, and GBM10 orthotopic models, achieving tumor growth inhibition of 90% and 50%, and survival benefit, respectively. GNE-317 could be effective in the treatment of GBM. | ||
| 信号通路 | PI3K/Akt/mTOR | ||
| 靶 点 | PI3K mTOR | ||
结构式
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