|
VEGFR Tyrosine Kinase Inhibitor IV
N-(2-Chloro-4-((6,7-dimethoxy-4-quinolyl)oxy)phenyl)-N′-(5-methyl-3-isoxazolyl)urea, Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor IV, VEGFR2 Kinase Inhibitor XXI, VEGFR1 Kinase Inhibitor V, VEGFR3 Kinase Inhibitor V, PDGFR Tyrosine Kinase Inhibitor XII
A cell-permeable quinoline-urea compound that potently inhibits the kinase activity of VEGFR (IC50 = 30, 6.5, and 15 nM for VEGFR-1,-2,and -3, respectively), EphB2, PDGFR-α, PDGFR-β, c-Kit, and Tie-2 (IC50 = 24, 40, 49, 78, and 78 nM, respectively). It exhibits little or no activity towards a panel of 15 other tyrosine kinases, including FGFR, IR, and IGFR, in cell-free kinase assays, while showing more than 7-fold higher potency in inhibiting ligand-induced phosphorylation of VEGFR-1/2/3 vs. c-Kit, PDGFR-β, Flt3, FGFR1, and c-Met in cell-based assays. Shown to be orally available and suppress tumor angiogenesis and growth in rats in vivo.
产品信息
Form Pink solid
Molar mass 472.9
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥95% by HPLC
Solubility DMSO
Chemical formula C22H19ClN4O5 • H2O
CAS number 475108-18-0
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Standard Handling |