AAL-993

Inhibits VEGFR-1 (IC50 = 130 nM), VEGFR-2 (IC50 = 23 nM), and VEGFR-3 (IC50 = 18 nM) . PDGFR-ß, cKit, and CSF-1R are also inhibited at higher concentrations (IC50’s 640 nM, 236 nM and 380 nM respectively) . Screening studies have shown no inhibitory activity against a range of other kinases. X-Ray crystallography has shown that AAL-993 binds to the catalytic domain of VEGFR-2 when the protein is in an inactive conformation. Cell permeable, active in vivo and in whole animal studies.