GDC-0941/GDC0941

溶解度:DMSO

储存条件:at -20℃ 2 years

生物活性

1.The IC50 values of GDC0941 for the inhibition of phosphorylation of Ser473 on AKT in IGROV-1 cells following 2- or 8-hour exposure were 18 ± 1 and 38 ± 13 nmol/L, respectively.

2.GDC-0941 Causes Sustained Inhibition ofthe Phosphatidylinositide 3-Kinase Pathway in U87MG Glioblastoma Xenografts

3.GDC-0941 was much less potent on mTOR and DNA-PK. Importantly, the activity of GDC-0941 against the panel of human tumor cell lines was generally similar to that of PI-103, suggesting that high potency against mTOR and/or DNA-PK was not essential for the inhibition of cell proliferation. In addition,GDC-0941 potently inhibited growth of activated human endothelial cells, suggesting potential for antiangiogenic activity, as we previously reported for PI-103.

参考文献

1.Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941