General description
A cell-permeable pyridopyrimidine compound that acts as a potent, ATP-competitive, and reversible inhibitor of FGF and VEGF receptors (IC50 = 21.5 nM for FGFR1). It inhibits PDGFR and c-Src only at much higher concentration (IC50 = 17.6 µM, 19.8 µM, respectively) and exhibits little effect against EGFR, InsR, MEK, and cPKC even at concentrations as high as 50 µM. Shown to inhibit the autophosphorylation of endogenous FGFR1 (IC50﹤5 nM) and overexpressed VEGFR2 (IC50﹤200 nM) in NIH3T3 cells in vitro, and FGF- and VEGF-induced angiogenesis in mice in vivo.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Koziczak, M., et al. 2004. Oncogene23, 3501.Trudel, S., et al. 2004. Blood103, 3521.Skaper, S.D., et al. 2000. J. Neurochem.75, 1520.Mohammadi, M., et al. 1998. EMBO J.17, 5896.
Packaging
Packaged under inert gas
5 mg in Plastic ampoule
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Warning
Toxicity: Irritant (B)
This product has met the following criteria to qualify for the following awards: