| 中文名称: | GNE-493 | ||||
|---|---|---|---|---|---|
| 英文名称: | GNE-493 | ||||
| 别名: | 2-(2-氨基-5-嘧啶基)-ALPHA,ALPHA-二甲基-4-(4-吗啉基)噻吩并[3,2-D]嘧啶-6-甲醇;双重泛PI3K/MTOR抑制剂(GNE-493);化合物GNE-493;2-(2-(2-氨基嘧啶-5-基)-4-吗啉噻吩[3,2-D]嘧啶-6-基)丙-2-醇 GNE-493;2-(2-Amino-5-pyrimidinyl)-alpha,alpha-dimethyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidine-6-methanol;CS-1783;GNE493;GNE493;2-[2-(2-aminopyrimidin-5-yl)-4-morpholin-4-ylthieno[3,2-d]pyrimidin-6-yl]propan-2-ol;2-(2-Amino-5-pyrimidinyl)-alpha,alpha-dimethyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidine-6-methanolGNE-493;2-(2-(2-aminopyrimidin-5-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)propan-2-ol;Thieno[3,2-d]pyrimidine-6-methanol,2-(2-amino-5-pyrimidinyl)-α,α-dimethyl-4-(4-morpholinyl)- | ||||
| CAS No: | 1033735-94-2 | 分子式: | C17H20N6O2S | 分子量: | 372.44 |
| CAS No: | 1033735-94-2 | ||||
| 分子式: | C17H20N6O2S | ||||
| 分子量: | 372.44 | ||||
密度：
1.408±0.06 g/cm3(Predicted)
包装规格：
5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介：
一种泛 PI3-kinase 和 mTOR 的口服双效抑制剂，对PI3Kα、PI3Kβ、PI3Kδ、PI3Kγ和mTOR的IC50值分别为3.4 nM、12 nM、16 nM、16 nM和32 nM。
溶解性：
DMSO :45 mg/mL(120.82 mM;超声加热助溶)
储备液保存：
-80°C, 2 years
-20°C, 1 year
-20°C, 1 year
靶点：
PI3Kα:3.4nM (IC50);PI3Kβ:12 nM (IC50);PI3Kδ:16 nM (IC50);PI3Kγ:16 nM (IC50);mTOR;30 nM (IC50)
体外研究：
GNE-493 is a low molecular weight, potent dual inhibitor of pan-PI3 kinases and mTOR. GNE-493 displays approximately equipotent inhibition of Class I PI3K isoforms, is submitted for screening in a 142 kinase panel provided by Invitrogen’s SelectScreen service. Of these kinases, only three are subject to greater than 50% inhibition by GNE-493, and none are inhibited greater than 80% when tested at 1 μM. Subsequently measured IC50s demonstrated that GNE-493 is more than 100-fold selective for PI3Kα over these three unrelated kinases (Aurora A IC50>10 μM, MLK1 IC50=591 nM and SYK IC50=371 nM).
体内研究：
To confirm and compare in vivo efficacy, GNE-493 is examined in the human MCF7.1 breast cancer xenograft model that harbors a PI3Kα activating mutation. Mice bearing xenografts are dosed orally once daily with 10 mg/kg of GNE-493 for 21 continuous days. Similar to observations made in the PC3 prostate cancer xenograft model, 10 mg/kg of GNE-493 results in 73% tumor growth inhibition at day 21 when compared to vehicle control animals. When achieving comparable levels of drug exposure, GNE-493 shows a similar suppression of the PI3K pathway and consequently, a similar efficacy profile against MCF7.1 breast tumors.
保存条件：
-20°C
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
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安全说明：
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参考文献 & 客户发表文献
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稀释公式
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