产品描述:
SU 14813 is a dual VEGFR and PDGFR family kinase inhibitor (IC50s = 0.002, 0.05, 0.004, and 0.015 µM for VEGFR1, VEGFR2, PDGFRβ, and KIT, respectively).{58125} It is selective for these kinases over FGFR1, EGFR, Src, and c-Met (IC50s = 3.5, >20, 2.5, and 9 µM, respectively). SU 14813 inhibits VEGFR2, PDGFRβ, KIT, and FLT3-internal tandem duplication (FLT3-ITD) phosphorylation in vitro (IC50s = 0.04, 0.02, 0.006, and 0.05 µM, respectively). It inhibits PDGF-dependent proliferation of NIH3T3 cells overexpressing PDGFRβ, as well as OC1-AML5 cells expressing wild-type FLT3 and MV4-11 cells carrying the activating FLT3-ITD mutation. SU 14813 inhibits VEGF-induced survival of human umbilical vein endothelial cells (HUVECs; IC50 = 6.8 nM). It reduces tumor growth in human acute myeloid leukemia, renal, and colon cancer, as well as rat glioma, mouse xenograft models when used at doses ranging from 10 to 80 mg/kg twice per day.