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)