ZM 323881 is a potent and selective VEGFR2 inhibitor with IC50 of <2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2. ZM323881 inhibits VEGF-A-induced endothelial cell proliferation (IC(50) = 8 nM) and VEGF-R2 tyrosine phosphorylation in vitro. ZM 323881 (10 nM) abolishes VEGF-A-mediated increases in vascular permeability in perfused mesenteric microvessels in male leopard. ZM 323881 (10 nM) blocks the increase in intensity of the VEGF-R2 band in the lung of male leopard frogs.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
ZM323881, a novel inhibitor of vascular endothelial growth factor-receptor-2 tyrosine kinase activity.
Whittles CE, et al. Microcirculation. 2002 Dec;9(6):513-22. PMID: 12483548.
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