5-(6-(3-Methoxyoxetan-3-yl)-4-Morpholinothieno[3,2-d]pyriMidin-2-yl)pyriMidin-2-aMine
- Product Name
- 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
- Formula Weight
- 414.48
- MOL File
- 1394076-92-6.mol
5-(6-(3-Methoxyoxetan-3-yl)-4-Morpholinothieno[3,2-d]pyriMidin-2-yl)pyriMidin-2-aMine Property
- storage temp.
- Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
- solubility
- Soluble in DMSO
- form
- A solid
N-Bromosuccinimide Price
- Product number
- B4991
- Product name
- GNE-317
- Packaging
- 5mg
- Price
- $138
- Updated
- 2021/12/16
- Product number
- Axon2994
- Product name
- GNE317
- Purity
- 98%
- Packaging
- 2x5mg
- Price
- $143
- Updated
- 2021/12/16
- Product number
- CS-3961
- Product name
- GNE-317
- Purity
- 99.31%
- Packaging
- 10mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- B4991
- Product name
- GNE-317
- Packaging
- 10mg
- Price
- $236
- Updated
- 2021/12/16
- Product number
- CS-3961
- Product name
- GNE-317
- Purity
- 99.31%
- Packaging
- 50mg
- Price
- $450
- Updated
- 2021/12/16
5-(6-(3-Methoxyoxetan-3-yl)-4-Morpholinothieno[3,2-d]pyriMidin-2-yl)pyriMidin-2-aMine Chemical Properties,Usage,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
|