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Technical Data
| Formula | C19H22N6O3S |
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| Molecular Weight | 414.48 | CAS No. | 1394076-92-6 | |
| Solubility (25°C)* | In vitro | DMSO | 21 mg/mL (50.66 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | GNE-317 is a potent, brain-penetrant PI3K inhibitor. | |
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| 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 (from reference)
| Animal Study:[1] |
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Selleck's GNE-317 has been cited by 4 publications
| APOE4/4 is linked to damaging lipid droplets in Alzheimer's disease microglia [ Nature, 2024, 628(8006):154-161.] | PubMed: 38480892 |
| APOE4/4 is linked to damaging lipid droplets in Alzheimer's disease microglia [ Nature, 2024, 628(8006):154-161] | PubMed: 38480892 |
| APOE4/4 is linked to damaging lipid droplets in Alzheimer's microglia [ bioRxiv, 2023, 2023.07.21.549930] | PubMed: 37546938 |
| APOE4/4 is linked to damaging lipid droplets in Alzheimer's microglia [ bioRxiv, 2023, 2023.07.21.549930] | PubMed: 37546938 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.