ZM323881

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Cat No.

CEI-1595

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.

Product Overview

ZM323881 inhibits VEGF-A-induced endothelial cell proliferation (IC50 = 8 nM) and VEGF-R2 tyrosine phosphorylation (IC50Vascular 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. Clinical trials: There is no clinical data are available currenlty.

CAS_No

193001-14-8

Molecular Weight

375.4

Purity

0.98

Storage

Store at -20°C

Synonyms

ZM 323881; ZM-323881

Targets

VEGFR-2/KDR

IC50

2 nM

Molecular Formula

C22H18FN3O2

Chemical Name

4-fluoro-2-methyl-5-[(7-phenylmethoxyquinazolin-4-yl)amino]phenol

Solubility

DMSO

Shipping Conditions

Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request

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).

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.

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Our Products Cannot Be Used As Medicines Directly For Personal Use.

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