GNE-317
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CAS No. | 1394076-92-6 | Cat. No. | BCP23939 |
Name | GNE-317 | ||
Synonyms | GNE317; GNE 317; | ||
SMILES | NC1=NC=C(C2=NC(N3CCOCC3)=C4C(C(C)=C(C5(OC)COC5)S4)=N2)C=N1 | ||
Chemical Name | |||
Formula | C18H20N6O3S | M. Wt | 400.45 |
Purity | 98% | Storage | Store at 4-8°C |
Description | 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. |
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