Description
PDGFR Inhibitor
A potent and selective inhibitor of VEGFR-1 (IC50=130nM), VEGFR-2 (IC50=23nM) and VEGFR-3 (IC50=18nM). At higher concentrations it inhibits PDGFR (640nM), c-Kit (236nM) and CSF-1R (380nM). Inactive at other kinases such as EGFR, FGFR-1, CDK-1, Tie-2, c-Met, IGF-1R, c-Src and c-Abl1. X-ray crystal studies on AAL-993 complexed to the catalytic domain of diphosphorylated VEGFR- 2 indicates that it binds to an inactive conformation of the protein2. Cell permeable and active in vivo. Inhibits VEGF-induced angiogenesis (mouse model)1.
Scientific Background: A potent inhibitor of PDGF receptor tyrosine kinase (PDGFRalpha and beta), IC50=1 uM (1). Also inhibits FGF receptor tyrosine kinase (2), c-kit (3) and FLT3 (4) and reverses transformation induced by activated FLT3 (5). Induces apoptosis in a small-cell lung cancer cell line (H526) (3). Cell permeable