General description
A cell-permeable quinazoline that acts as a potent, ATP-binding site-targeting, VEGFR2-selective inhibitor (IC50 = 32 nM), while exhibiting much reduced potency against c-kit, Ret, FMS, PDGFRα, and Aurora A (IC50 = 0.62, 2.5, 2.9, 3.1, and 3.9 µM, respectively) and little or no activity against 11 other kinases (IC50 >10 µM). An effective antiangiogenesis agent (86%, 92%, and 98% inhibition, respectively, of HUVEC migration, invasion, and tube formation at 10 µM; 80% inhibition of zebrafish embryos intersegmental vessel growth at 2.5 µM) that significantly suppresses SW620- and HepG2-derived tumor growth in mice (by 72% and 63%, respectively, in 18 days; 100 mg/kg/day; i.p.) in vivo.
A cell-permeable quinazoline that acts as a potent, ATP-binding site-targeting, VEGFR2-selective inhibitor (IC50 = 32 nM), while exhibiting much reduced or little activity against 16 other kinases. An effective antiangiogenesis agent (98% inhibition of HUVEC tube formation at 10 µM; 80% inhibition of zebrafish embryos intersegmental vessel growth at 2.5 µM) that significantly suppresses SW620- and HepG2-derived tumor growth in mice (by 72% and 63%, respectively, in 18 days; 100 mg/kg/day; i.p.) in vivo.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Other Notes
Zhang, S., et al. 2011. Clin. Cancer Res.17, 4439.
Packaging
Packaged under inert gas
10 mg in Glass bottle
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Warning
Toxicity: Regulatory Review (Z)
This product has met the following criteria: