A cell-permeable quinazoline that acts as a potent, ATP-binding site-targeting, VEGFR2-selective inhibitor (IC50=32nM), while exhibiting much reduced or little activity against 16 other kinases. An effective antiangiogenesis agent (98% inhibition of HUVEC tube formation at 10uM; 80% inhibition of zebrafish embryos intersegmental vessel growth at 2.5uM) that significantly suppresses SW620- and HepG2-derived tumor growth in mice (by 72% and 63%, respectively, in 18 days; 100mg/kg/day; i.p.) in vivo.
Formula:C13H12N4O2S2
Molecular Weight:320.4
Solubility:DMSO (2.5mg/ml)
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
