380843-75-4

溶解度:10 mmol/L in DMSO

储存条件:-20C 2 years

生物活性

Inhibitors of SRC, ABL and TEC family kinases. It can cause a decrease in cell motility and invasion of breast cancer cell lines with an IC50 of ∼250 nmol/L, which was also the IC50 for inhibition of cellular Src kinase activity in intact tumor cells. SKI-606 inhibits the phosphorylation of focal adhesion kinase (FAK), proline-rich tyrosine kinase 2 (Pyk2), and Crk-associated substrate (p130Cas), with an IC50 similar to inhibition of cellular Src kinase. A promising therapeutic for breast cancer.

参考文献

1.Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors. Marcus Bantscheff, Dirk Eberhard, et al. Nature Biotechnology; 1087-0156; 2007; 25(9); 1035-1044

2.SKI-606 (bosutinib), a novel Src kinase inhibitor, suppresses migration and invasion of human breast cancer cells. Adina Vultur1, Ralf uettner, et al. Mol Cancer Ther 2008;7(5):1185-94

3.Effective and selective inhibition of chronic myeloid leukemia primitive hematopoietic progenitors by the dual Src/Abl kinase inhibitor SKI-606. Konig H, Holyoake TL, Bhatia R. Blood. 2008 Feb 15;111(4):2329-38. Epub 2007 Dec 4