TAS-115 (Pamufetinib) is a potent, dual VEGFR2/c-Met inhibitor with IC50 of 30 and 32 nM against rVEGFR2 and rMET, respectively.
TAS-115 also inhibits PDGFRα/β, Axl, c-Kit, Src, FLT-1 in a 192-kinase panel assay.
TAS-115 markedly inhibits the tyrosine phosphorylation of VEGFR2 at 10 nM in VEGF-stimulated HUVECs, also inhibits the tyrosine phosphorylation of MET in MKN45 cells.
TAS-115 inhibits cellular proliferation of HUVECs under VEGF-dependent growth condition with IC50 of 19 nM, with weak inhibition of growth (GI50>10 uM) in VEGFR signal- or MET signal-independent cells.
TAS-115 effectively suppresses the progression of MET-inactivated tumor by blocking angiogenesis in vivo.
