Kinase Inhibitors

A potent, cell-permeable, reversible, and ATP-competitive inhibitor of the kinase activities of KDR, Flt-1 and c-Kit (IC 50 = 20 nM, 180 nM and 240 nM, respectively), and minimally inhibit c-Src and EGF-R activities (IC 50 = 7.0 &#181M and 7.

A cell-permeable quinolyloxyphenyl-urea compound that acts as a VEGFR-2-selective inhibitior in both cell-based (IC 50 = 0.9 nM in VEGF-induced receptor phosphorylation) and cell-free (IC 50 = 4.

A cell-permeable quinazoline that acts as a potent, ATP-binding site-targeting, VEGFR2-selective inhibitor (IC 50 = 32 nM), while exhibiting much reduced or little activity against 16 other kinases. An effective antiangiogenesis agent (98%

Wortmannin, a fungal metabolite, is a cell-permeable, irreversible inhibitor of phosphatidylinositol 3 kinase (PI3 Kinase) with an IC50 of 5nM. It blocks the catalytic activity of PI3-Kinase without affecting upstream signaling events such as