A cell-permeable quinolyloxyphenyl-urea compound that acts as a VEGFR-2-selective inhibitior in both cell-based (IC50 = 0.9 nM in VEGF-induced receptor phosphorylation) and cell-free (IC50 = 4.0 nM in kinase reactions) assays. It inhibits c-Kit, PDGFRα, and FGFR-2 only at much higher concentrations (IC50 = 40, 67, and 170 nM, respectively, in cell-based assays), while exhibiting no effect against eight other commonly studied receptor and non-receptor kinases even at concentrations as high as 10 µM. Effectively blocks VEGF-dependent, but not VEGF-independent, cell proliferation in vitro and tumor growth in mice and rats (5 to 20 mg/kg, daily p.o.) in vivo.
5 mg in Plastic ampoule
Packaged under inert gas
Toxicity: Regulatory Review (Z)
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Kubo, K., et al. 2005. J. Med. Chem.48, 1359.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
|Quality Level ||100|
|assay ||≥97% (HPLC)|
|mfr. no. ||Calbiochem®|
|storage condition ||OK to freeze|
| ||protect from light|
|storage conditions ||+2C to +8C|
|solubility ||DMSO: 50 mg/mL|
|shipped in ||ambient|
安全声明 (欧洲) 22-24/25-36/37/39