[CAS NO. 1394076-92-6] GNE-317
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PRODUCTS SPECIFICATIONS [1394076-92-6]
Store
Catalog
SLK-S7798
Brand
Selleck
CAS
1394076-92-6
DESCRIPTION [1394076-92-6]
Overview
| MDL | MFCD28900677 |
|---|---|
| Molecular Weight | 414.48 |
| Molecular Formula | C19H22N6O3S |
| SMILES | NC1=NC=C(C2=NC(N3CCOCC3)=C4C(C(C)=C(C5(OC)COC5)S4)=N2)C=N1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4127 mL | 12.0633 mL | 24.1266 mL |
| 5 mM | 0.4825 mL | 2.4127 mL | 4.8253 mL |
| 10 mM | 0.2413 mL | 1.2063 mL | 2.4127 mL |
| 50 mM | 0.0483 mL | 0.2413 mL | 0.4825 mL |
Description
GNE-317 is a potent, brain-penetrant 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.
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.
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