5-(6-(3-Methoxyoxetan-3-yl)-4-Morpholinothieno[3,2-d]pyriMidin-2-yl)pyriMidin-2-aMine
- CAS No.
- 1394076-92-6
- Chemical Name:
- 5-(6-(3-Methoxyoxetan-3-yl)-4-Morpholinothieno[3,2-d]pyriMidin-2-yl)pyriMidin-2-aMine
- Synonyms
- GNE-317;CS-1716;GNE-317;GNE 317;GNE317;5-(6-(3-Methoxyoxetan-3-yl)-4-Morpholinothieno[3,2-d]pyriMidin-2-yl)pyriMidin-2-aMine;5-(6-(3-methoxyoxetan-3-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine;5-(6-(3-Methoxyoxetan-3-yl)-4-Morpholinothieno[3,2-d]pyriMidin-2-yl)pyriMidin-2-aMine USP/EP/BP;5-[6-(3-METHOXYOXETAN-3-YL)-7-METHYL-4-MORPHOLIN-4-YLTHIENO[3,2-D]PYRIMIDIN-2-YL]PYRIMIDIN-2-AMINE;inhibit,GNE-317,Inhibitor,Phosphoinositide 3-kinase,Mammalian target of Rapamycin,mTOR,GNE 317,PI3K;2-Pyrimidinamine, 5-[6-(3-methoxy-3-oxetanyl)-7-methyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-2-yl]-
- CBNumber:
- CB92715574
- Molecular Formula:
- C19H22N6O3S
- Molecular Weight:
- 414.48
- MDL Number:
- MFCD28900677
- MOL File:
- 1394076-92-6.mol
5-(6-(3-Methoxyoxetan-3-yl)-4-Morpholinothieno[3,2-d]pyriMidin-2-yl)pyriMidin-2-aMine price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ApexBio Technology | B4991 | GNE-317 | 1394076-92-6 | 5mg | $138 | 2021-12-16 | Buy |
Axon Medchem | Axon2994 | GNE317 98% | 1394076-92-6 | 2x5mg | $143 | 2021-12-16 | Buy |
ChemScene | CS-3961 | GNE-317 99.31% | 1394076-92-6 | 10mg | $150 | 2021-12-16 | Buy |
ApexBio Technology | B4991 | GNE-317 | 1394076-92-6 | 10mg | $236 | 2021-12-16 | Buy |
ChemScene | CS-3961 | GNE-317 99.31% | 1394076-92-6 | 50mg | $450 | 2021-12-16 | Buy |
5-(6-(3-Methoxyoxetan-3-yl)-4-Morpholinothieno[3,2-d]pyriMidin-2-yl)pyriMidin-2-aMine Chemical Properties,Uses,Production
Biological Activity
gne-317 is a potent inhibitor of pi3k [1].phosphatidylinositol-4,5-bisphosphate 3-kinase (pi3k) are a series of enzymes and play an important role in cell growth, proliferation, differentiation, survival, motility and intracellular trafficking.in the gl261 cell line, gne-317 showed cytotoxic activity [2].in mouse brain, gne-317(50 mg/kg) significantly inhibited pakt, p4ebp1 and ps6 by 80%, 84%, and 92% respectively, which were downstream markers of the pi3k/mtor pathway. in u87, gs2 and gbm10 tumor-bearing mice, gne-317 inhibited tumor growth by 90%, 50% and a survival benefit, respectively [1]. in c57b6/j mice inoculated with gl261-gfp-luc cells, the concentrations of gne-317 in the normal brain, tumor core and rim were not significantly different. in tumor-bearing mice, gne-317 significantly reduced the levels of p-aktser473, p-s6ser235/236 and p-4ebp1thr37/46 within the tumor [2]. in u87 and gs2 glioblastoma multiforme (gbm) models, gne-317 was uniformly distributed in the brain. the brain-to-plasma ratios for gne-317 were greater than 1, in agreement with the brain penetration properties of gne-317 [3].
in vitro
GNE-317 is not a substrate of P-gp or BCRP transporter in transfected Madin-Darby canine kidney (MDCK) cells. Binding of it 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%.It shows cytostasis but no cell death to U87 cells.
in vivo
GNE-317 (40 mg/kg, po) 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, po) ) is ef?cacious 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, po; 40 mg/kg the ?rst 2 weeks) extends the survival of mice from a median of 55.5 to 75 days.
target
PI3K
| mTOR
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Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32686 | 60 |
Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28180 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 28455 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
Jilin Chinese Academy of Sciences-yanshen Technology | +undefined18143011203 | info@chemextension.com | China | 42057 | 58 |
Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 57511 | 58 |
Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131981 | 58 |
Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2923 | 55 |