GNE-317

  • Chemical Properties
CAS No. 1394076-92-6 Cat. No. BCP23939
Name GNE-317
Synonyms GNE317; GNE 317;
Formula C18H20N6O3S M. Wt 400.45
  • Biological Activity
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.
Pathways PI3K/Akt/mTOR 
Targets PI3K mTOR 

Structure

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