GNE-317CAS# 1394076-92-6 |
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Quality Control & MSDS
3D structure
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| Cas No. | 1394076-92-6 | SDF | Download SDF |
| PubChem ID | 70676303 | Appearance | Powder |
| Formula | C19H22N6O3S | M.Wt | 414.48 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 20 mg/mL (48.25 mM; Need ultrasonic and warming) | ||
| Chemical Name | 5-[6-(3-methoxyoxetan-3-yl)-7-methyl-4-morpholin-4-ylthieno[3,2-d]pyrimidin-2-yl]pyrimidin-2-amine | ||
| SMILES | CC1=C(SC2=C1N=C(N=C2N3CCOCC3)C4=CN=C(N=C4)N)C5(COC5)OC | ||
| Standard InChIKey | XOZLHJMDLKDZAL-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C19H22N6O3S/c1-11-13-14(29-15(11)19(26-2)9-28-10-19)17(25-3-5-27-6-4-25)24-16(23-13)12-7-21-18(20)22-8-12/h7-8H,3-6,9-10H2,1-2H3,(H2,20,21,22) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | GNE-317 is a PI3K/mTOR inhibitor, is able to cross the blood-brain barrier (BBB).In Vitro:GNE-317 is an oxetane derivative of GDC-0980 synthesized with the goal of reducing substrate affinity for efflux transporters. In vitro, GDC-0980 and GNE-317 demonstrate similar profiles in MTS cytotoxicity experiments using the GL261 cell line[1].In Vivo:Seven days after i.c. inoculation with GL261-GFP-Luc cells, mice are treated once daily with the maximum tolerated dose of GDC-0980 (7.5 mg/kg), GNE-317 (30 mg/kg), or vehicle. For GL261, tumor growth is tracked through bioluminescence imaging on a weekly basis. There are no significant changes in GL261 tumor growth among the 3 groups. In assessing survival benefits in GL261, neither GDC-0980 nor GNE-317 provides survival benefit over the vehicle-treated animals. The fact that these drugs are not effective in vivo is suggested by the in vitro cytotoxicity data showing that the drugs have limited efficacy in inducing cell death in the GL261 cell line. Neither drug is effective in the GL261 tumor in spite of greater delivery and enhanced therapeutic targeting efficacy of GNE-317[1]. References: | |||||
GNE-317 Dilution Calculator
GNE-317 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.4127 mL | 12.0633 mL | 24.1266 mL | 48.2532 mL | 60.3165 mL |
| 5 mM | 0.4825 mL | 2.4127 mL | 4.8253 mL | 9.6506 mL | 12.0633 mL |
| 10 mM | 0.2413 mL | 1.2063 mL | 2.4127 mL | 4.8253 mL | 6.0317 mL |
| 50 mM | 0.0483 mL | 0.2413 mL | 0.4825 mL | 0.9651 mL | 1.2063 mL |
| 100 mM | 0.0241 mL | 0.1206 mL | 0.2413 mL | 0.4825 mL | 0.6032 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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GNE-317 is a potent, brain-penetrant PI3K inhibitor.
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Distribution of the phosphatidylinositol 3-kinase inhibitors Pictilisib (GDC-0941) and GNE-317 in U87 and GS2 intracranial glioblastoma models-assessment by matrix-assisted laser desorption ionization imaging.[Pubmed:24754926]
Drug Metab Dispos. 2014 Jul;42(7):1110-6.
Glioblastoma multiforme (GBM) is the most common primary brain tumor in adults, and the limited available treatment options have not meaningfully impacted patient survival in the past decades. Such poor outcomes can be at least partly attributed to the inability of most drugs tested to cross the blood-brain barrier and reach all areas of the glioma. The objectives of these studies were to visualize and compare by matrix-assisted laser desorption ionization (MALDI) imaging mass spectrometry the brain and tumor distribution of the phosphatidylinositol 3-kinase (PI3K) inhibitors pictilisib (GDC-0941, 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-t hieno[3,2-d]pyrimidine) and GNE-317 [5-(6-(3-methoxyoxetan-3-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyr imidin-2-amine] in U87 and GS2 orthotopic models of GBM, models that exhibit differing blood-brain barrier characteristics. Following administration to tumor-bearing mice, pictilisib was readily detected within tumors of the contrast-enhancing U87 model whereas it was not located in tumors of the nonenhancing GS2 model. In both GBM models, pictilisib was not detected in the healthy brain. In contrast, GNE-317 was uniformly distributed throughout the brain in the U87 and GS2 models. MALDI imaging revealed also that the pictilisib signal varied regionally by up to 6-fold within the U87 tumors whereas GNE-317 intratumor levels were more homogeneous. Liquid chromatography coupled with tandem mass spectrometry (LC-MS/MS) analyses of the nontumored half of the brain showed pictilisib had brain-to-plasma ratios lower than 0.03 whereas they were greater than 1 for GNE-317, in agreement with their brain penetration properties. These results in orthotopic models representing either the contrast-enhancing or invasive areas of GBM clearly demonstrate the need for whole-brain distribution to potentially achieve long-term efficacy in GBM.
