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|Solubility (25°C) *||In vitro||DMSO||47 mg/mL warmed (113.39 mM)|
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Description||GNE-317 is a potent, brain-penetrant PI3K inhibitor.|
|In vitro||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||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.|
|Animal Models||U87 and GS2 orthotopic tumor-bearing mice|
|Formulation||0.5% methylcellulose/0.2%Tween 80|
PLEASE KEEP THE PRODUCT UNDER -20°C FOR LONG-TERM STORAGE.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.
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