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ZM323881

Catalog No.
A3954
VEGFR-2/KDR inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
10mg
$163.00
Ship with 10-15 days
50mg
$650.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

ZM323881 inhibits VEGF-A-induced endothelial cell proliferation (IC50 = 8 nM) and VEGF-R2 tyrosine phosphorylation (IC50 < 2 nM).

Vascular endothelial growth factor (VEGF) increases vascular permeability and angiogenesis in many pathological conditions, such as cancer, arthritis, and diabetes. VEGF activates VEGF-Receptor 1 (VEGF-R1) and VEGF-Receptor 2 (VEGF-R2) that autophosphorylate to initiate a signaling cascade resulting in angiogenesis and increased microvascular permeability. ZM323881 is a potent and selective inhibitor of VEGF-R2 tyrosine kinase.

In vitro: ZM323881 was found to inhibit VEGF-A-induced endothelial cell proliferation (IC50 = 8 nM) and VEGF-R2 tyrosine phosphorylation in vitro (IC50 < 2 nM) [1].

In vivo: VEGF-Amediated 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, suggesting that VEGF-R2 phosphorylation is necessary for VEGF-A-mediated increases in microvascular permeability in vivo [1].

Clinical trials: There is no clinical data are available currenlty.

Reference:
[1] Whittles CE, Pocock TM, Wedge SR, Kendrew J, Hennequin LF, Harper SJ, Bates DO.   ZM323881, a novel inhibitor of vascular endothelial growth factor-receptor-2 tyrosine kinase activity. Microcirculation. 2002;9(6):513-22.

Chemical Properties

StorageStore at -20°C
M.Wt375.4
Cas No.193001-14-8
FormulaC22H18FN3O2
SynonymsZM 323881;ZM-323881
SolubilitySoluble in DMSO
Chemical Name4-fluoro-2-methyl-5-[(7-phenylmethoxyquinazolin-4-yl)amino]phenol
SDFDownload SDF
Canonical SMILESCC1=CC(=C(C=C1O)NC2=NC=NC3=C2C=CC(=C3)OCC4=CC=CC=C4)F
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description ZM323881 is a potent and selective inhibitor of human vascular endothelial growth factor receptor 2 (VEGFR-2/KDR) with IC50 value of 2 nM.
Targets VEGFR-2/KDR          
IC50 2 nM          

Quality Control

Quality Control & MSDS

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Chemical structure

ZM323881