GNE-317

Catalog No.S7798

GNE-317 Chemical Structure

Molecular Weight(MW): 414.48

GNE-317 is a potent, brain-penetrant PI3K inhibitor.

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Biological Activity

Description GNE-317 is a potent, brain-penetrant PI3K inhibitor.
Targets
PI3K [1]
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.[1]

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.[1]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: U87 and GS2 orthotopic tumor-bearing mice
  • Formulation: 0.5% methylcellulose/0.2%Tween 80
  • Dosages: 40 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 47 mg/mL warmed (113.39 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 414.48
Formula

C19H22N6O3S

CAS No. 1394076-92-6
Storage powder
Synonyms N/A

Bio Calculators

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID