GNE-317 1208319-26-9

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Synonyms

：

Appearance

：

Chemical Formula

：

C19H22N6O3S

Solubility

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Molecular Weight

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414.48

Storage and Stability

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in stock

CAS No.

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1208319-26-9

Purity

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98%+

Introduction

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.

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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GNE-317 1208319-26-9

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GNE-317 1208319-26-9

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