ZM323881 is a potent and selective inhibitor of the kinase activity of the human vascular endothelial growth factor receptor 2 (VEGFR2/KDR). ZM323881 selectively inhibits VEGFR2 over VEGFR1 and other receptor tyrosine kinases with an IC50 = 2nM. ZM323881 inhibits VEGF-A-induced endothelial cell proliferation (IC(50) = 8 nM) and VEGF-R2 tyrosine phosphorylation in vitro. VEGF-A-mediated increases in vascular permeability in perfused mesenteric microvessels in vivo were reversibly abolished by both ZM323881 and the class III receptor tyrosine kinase inhibitor PTK787/ZK222584. ZM323881 alone did not cause any alteration. Premedication with ZM323881 or L-NAME decreased the dilatory effects of VEGF. ZM323881 (10 nM) completely blocks VEGF-induced VEGF promoter activity in SCC-9 cells. ZM323881 (10 nM) blocks VEGF stimulated Hif-1α protein accumulation in SCC-9 cells. ZM323881 (10 nM) blocks VEGF-induced Rac1 activation at 30 min in HUVECs. ZM323881 (10 nM) prevents Vav2 tyrosine phosphorylation in response to VEGF in HUVECs.
|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.
Vascular endothelial growth factor modulates the function of the retinal pigment epithelium in vivo.
Dahrouj M, et al. Invest Ophthalmol Vis Sci. 2014 Apr 9;55(4):2269-75. PMID: 24550368.
Investigation of the venodilatory effect of vascular endothelial growth factor (VEGF) in rat gingiva.
Gyurkovics M, et al. Fogorv Sz. 2013 Jun;106(2):53-9. PMID: 24344561.
Microvascular regulatory role and increased expression of vascular endothelial growth factor receptor type 2 in experimental gingivitis.
Gyurkovics M, et al. J Periodontal Res. 2013 Apr;48(2):194-202. PMID: 22957787.
VEGF-induced Rac1 activation in endothelial cells is regulated by the guanine nucleotide exchange factor Vav2.
Garrett TA, et al. Exp Cell Res. 2007 Sep 10;313(15):3285-97. PMID: 17686471.
IGF-1 induced vascular endothelial growth factor secretion in head and neck squamous cell carcinoma.
Slomiany MG, et al. Biochem Biophys Res Commun. 2006 Apr 14;342(3):851-8. PMID: 16499871.
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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Fruquintinib (HMPL-013) is a highly potent and selective VEGFR 1/2/3 inhibitor with IC50s of 33, 0.35, and 35 nM, respectively.
SUN11602 is a novel aniline compound with basic fibroblast growth factor-like activity.
Anlotinib Dihydrochloride is a novel multi-target tyrosine kinase inhibitor that is designed to primarily inhibit VEGFR2/3, FGFR1-4, PDGFRα/β, c-Kit, and Ret.
Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.
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