In vitro
SU11274 can inhibit c-MET with IC50 of 12 nM. SU11274 differentially affects the kinase activity and subsequent signaling of various mutant forms of Met. SU11274 inhibit Met variants, M1268T and H1112Y, with IC50 of 2 uM, but shows little inhibition to Met variants, L1213V and Y1248H. For cell lines (1) NSCLC As a selective small molecule inhibitor of c-Met, SU11274 inhibited cell viability in c-Met-expressing NSCLC cells. SU11274 abrogated hepatocyte growth factor-induced phosphorylation of c-Met and its downstream signaling. (2) Ovarian carcinoma cells As c-Met is overexpressed in the majority of malignant ovarian epithelial cells, SU11274 can significantly decreased cell motility and invasion of ovarian carcinoma cells by decreasing activated c-Met.
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