纯度:98% by TLC [60% ethyl acetate in hexane; Rf = 0.36] NMR conforms
分子式:C20H16F3N3O
分子量:371.36
溶剂:DMSO (25 mg/ml) Ethanol (15 mg/ml)
性状:Pale yellow solid
存储:RT
Activity (short version):VEGFR inhibitor
Function / Pharmacology:Inhibits VEGFR-1 (IC50 = 130 nM), VEGFR-2 (IC50 = 23 nM), and VEGFR-3 (IC50 = 18 nM). PDGFR-?, 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.