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ZM323881
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ZM323881图片
CAS NO:193001-14-8
规格:98%
分子量:375.4
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
VEGFR-2/KDR inhibitor,potent and selective
CAS:193001-14-8
分子式:C22H18FN3O2
分子量:375.4
纯度:98%
存储:Store at -20°C

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.