The VEGFR2 Kinase Inhibitor VII, SKLB1002 controls the biological activity of VEGFR2 Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
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.
包装
Packaged under inert gas
警告
Toxicity: Regulatory Review (Z)
再構成
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
その他情報
Zhang, S., et al. 2011. Clin. Cancer Res.17, 4439.
法的情報
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany