GNE-317
| 中文名称 | GNE-317 |
|---|---|
| 中文同义词 | PI3K/MTOR抑制剂(GNE-317);5-[6-(3-甲氧基-3-氧杂环丁基)-7-甲基-4-(4-吗啉基)噻吩并[3,2-D]嘧啶-2-基]-2-嘧啶胺;5-(6-(3-甲氧基氧杂环丁烷-3-基)-7-甲基-4-吗啉基噻吩并[3,2-D]嘧啶-2-基)嘧啶-2-胺;化合物GNE317;化合物GNE317,10 MM DMSO 溶液;GNE-317 (GNE317) |
| 英文名称 | 5-(6-(3-Methoxyoxetan-3-yl)-4-Morpholinothieno[3,2-d]pyriMidin-2-yl)pyriMidin-2-aMine |
| 英文同义词 | 5-(6-(3-Methoxyoxetan-3-yl)-4-Morpholinothieno[3,2-d]pyriMidin-2-yl)pyriMidin-2-aMine;GNE-317;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)-7-METHYL-4-MORPHOLIN-4-YLTHIENO[3,2-D]PYRIMIDIN-2-YL]PYRIMIDIN-2-AMINE;GNE-317;GNE 317;GNE317;CS-1716;2-Pyrimidinamine, 5-[6-(3-methoxy-3-oxetanyl)-7-methyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-2-yl]-;5-(6-(3-Methoxyoxetan-3-yl)-4-Morpholinothieno[3,2-d]pyriMidin-2-yl)pyriMidin-2-aMine USP/EP/BP |
| CAS号 | 1394076-92-6 |
| 分子式 | C19H22N6O3S |
| 分子量 | 414.48 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂;抑制剂 |
| Mol文件 | 1394076-92-6.mol |
| 结构式 |  |
GNE-317 性质
| 储存条件 | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
|---|---|
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 固体 |
| 颜色 | 浅黄至卡其色 |
| 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) |
| InChIKey | XOZLHJMDLKDZAL-UHFFFAOYSA-N |
| SMILES | NC1=NC=C(C2=NC3=C(C(N4CCOCC4)=N2)SC(C5(COC5)OC)=C3C)C=N1 |
GNE-317 是一种有效的，大脑渗透性 PI3K 抑制剂。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.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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PI3K
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mTOR
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安全信息
| WGK Germany | WGK 3 |
|---|---|
| 存储类别 | 11 - 可燃固体 |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025/12/22 | HY-12763 | GNE-317 GNE-317 | 1394076-92-6 | 5mg | 476元 |
| 2025/12/22 | HY-12763 | GNE-317 GNE-317 | 1394076-92-6 | 10mM * 1mLin DMSO | 523元 |