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ZM323881

Cat. No. M3740
ZM323881 Structure
Size Price Availability Quantity
10mg USD 120 In stock
50mg USD 480 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 375.4
Formula C22H18FN3O2
CAS Number 193001-14-8
Purity >99%
Solubility DMSO
Storage at -20°C
References

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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  Catalog
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Keywords: ZM323881 supplier, VEGFR/PDGFR, inhibitors

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