1394076-92-6
中文名称
GNE-317
英文名称
5-(6-(3-Methoxyoxetan-3-yl)-4-Morpholinothieno[3,2-d]pyriMidin-2-yl)pyriMidin-2-aMine
CAS
1394076-92-6
分子式
C18H20N6O3S
分子量
400.455
MOL 文件
1394076-92-6.mol
更新日期
2024/05/06 07:32:25
1394076-92-6 结构式
基本信息
中文别名
化合物GNE317PI3K/MTOR抑制剂(GNE-317)
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
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
英文别名
GNE-317CS-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
2-Pyrimidinamine, 5-[6-(3-methoxy-3-oxetanyl)-7-methyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidin-2-yl]-
所属类别
生物化工：PI3K 抑制剂常见问题列表
生物活性
GNE-317 是一种有效的，大脑渗透性 PI3K 抑制剂。体外研究
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.体内研究
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.靶点
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PI3K
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mTOR
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