中文名 | Compound 401 |
英文名 | Compound 401 |
别名 | 化合物COMPOUND 401 2-吗啉基-4H-嘧啶并[2,1-A]异喹啉-4-酮 2-(吗啉-4-基)嘧啶并[2,1-A]异喹啉-4-酮 2-MORPHOLINO-4H-PYRIMIDO[2,1-A]ISOQUINOLIN-4-ONE 2-吗啉基-4H-嘧啶并[2,1-A]异喹啉-4-酮 |
英文别名 | CS-315 COMPOUND401 Compound 401 COMPOUND-401 2-Morpholino-4H-pyrimido[2,1-a]isoquinolin-4-one 2-(Morpholin-4-yl)pyrimido[2,1-a]isoquinolin-4-one 2-(4-Morpholinyl)-4H-pyrimido[2,1-a]isoquinolin-4-one 4H-PyriMido[2,1-a]isoquinolin-4-one, 2-(4-Morpholinyl)- |
CAS | 168425-64-7 |
化学式 | C16H15N3O2 |
分子量 | 281.31 |
密度 | 1.36±0.1 g/cm3 (20 ºC 760 Torr) |
熔点 | 184-186℃ (ethanol ) |
沸点 | 456.9±55.0 °C(Predicted) |
酸度系数 | 1.01±0.20(Predicted) |
存储条件 | Store at RT |
外观 | 粉末或结晶 |
颜色 | White to Light yellow |
体外研究 | Compound 401 is a potent inhibitor of DNA-PK (IC 50 =0.28 μM). Compound 401 is reported to be a poor inhibitor of PI3K, ATM, and ATR in vitro, but it is active against mTOR. Compound 401 shows activity against mTOR (IC 50 =5.3 μM) but not p110α/p85α PI3K (IC 50 >100 μM). Treatment of cells with Compound 401 blocks the phosphorylation of sites modified by mTOR-Raptor and mTOR-Rictor complexes (ribosomal protein S6 kinase 1 Thr 389 and Akt Ser 473 , respectively). By contrast, there is no direct inhibition of Akt Thr 308 phosphorylation, which is dependent on PI3K. Similar effects are also observed in cells that lack DNA-PK. Compound 401 inhibits immunoprecipitated epitope-tagged mTOR or endogenous mTOR in Raptor immunoprecipitates. In both cases, inhibition of 67% or 78% is obtained at 5 μM or 10 μM Compound 401, respectively. By contrast, dose response curves show that the p110α/p85α or p110β/p85α PI3K complexes are poorly inhibited by Compound 401 at these concentrations. The proliferation of TSC1 -/- fibroblasts is inhibited in the presence of Compound 401, but TSC1 +/+ cells are resistant. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.555 ml | 17.774 ml | 35.548 ml |
5 mM | 0.711 ml | 3.555 ml | 7.11 ml |
10 mM | 0.355 ml | 1.777 ml | 3.555 ml |
5 mM | 0.071 ml | 0.355 ml | 0.711 ml |
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