ZM323881 is a potent and selective inhibitor of VEGFR2 with an IC50 of less than 2 nM.

ZM323881, an anilinoquinazoline compound, functions as a potent inhibitor of VEGFR2 (KDR) tyrosine kinase, displaying exceptional selectivity by significantly limiting its activity compared to that of other receptor tyrosine kinases like PDGFRβ, FGFR1, EGFR, and erbB2 (IC 50 >50 μM). It effectively suppresses VEGF-A-driven endothelial cell proliferation (IC 50 =8 nM) and VEGFR2 tyrosine phosphorylation [1]. Notably, ZM323881 specifically targets VEGFR-2 inhibition without affecting VEGFR-1, EGFR, PDGFR, or HGF receptor activation. Additionally, in HAECs, it completely blocks VEGF-induced ERK phosphorylation at a concentration of 1 μM [2], showcasing its potential therapeutic utility in conditions characterized by abnormal angiogenesis.