ZM 323881 HCl

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Biological Activity

Description	ZM 323881 is a potent and selective VEGFR2 inhibitor with IC50 of <2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2.
Targets	VEGFR2
IC50	< 2 nM [1]
In vitro	ZM323881 inhibits VEGF-A, EGF and bFEF induced HUVEC cell proliferation with IC50 of 8 nM, 1.9 μM and 1.6 μM, respectively. ZM323881 (10 nM) abolishes VEGF-A-mediated increases in vascular permeability in perfused mesenteric microvessels in male leopard. ZM323881 (10 nM) blocks the increase in intensity of the VEGF-R2 band in the lung of male leopard frogs. [1] ZM323881 (1 μM) blocks activation of extracellular regulated-kinase, p38, Akt, and endothelial nitric oxide synthetase (eNOS) by VEGF, but did not inhibit p38 activation by the VEGFR-1-specific ligand, placental growth factor (PIGF) in human aortic endothelial cells (HAECs). ZM323881 (1 μM) also perturbes VEGF-induced membrane extension, cell migration, and tube formation by HAECs. ZM323881 (1 μM) reverses VEGF-stimulated phosphorylation of CrkII and its Src homology 2 (SH2)-binding protein p130Cas, which are known to play a pivotal role in regulating endothelial cell migration. [2] 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. [3] 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. [4] ZM323881 (< 1 μM) inhibits VEGF stimulated neural stem cell proliferation in a dose-dependent manner. ZM323881 (< 1 μM) inhibits neural stem cell proliferation in a dose-dependent manner even when no exogenous VEGF is added. [5]
In vivo
Features

Protocol(Only for Reference)

Kinase Assay: ^[1]

Binding assay	ZM323881 is incubated (20 minutes, room temperature) with enzyme in an HEPES (pH 7.5) buffered solution containing 10 mM MnCl2 and 2 μM ATP, in 96-well plates coated with a poly(Glu, Ala, Tyr) 6:3:1 random copolymer substrate. IC50 data are interpolated by nonlinear regression (four-parameter logistic equation) using Microcal Origin software.

1

References

Chemical Information

Download ZM 323881 HCl SDF

Chemical Name	Phenol, 4-fluoro-2-methyl-5-[[7-(phenylmethoxy)-4-quinazolinyl]amino]-, hydrochloride (1:1)

Preparing Stock Solutions

Stock Solution (1ml DMSO)	1mM	10mM	20mM	30mM
Mass(mg)	0.41186	4.1186	8.2372	-