Name | ZM 323881 HCl |
Synonyms | ZM 323881 HCl ZM 323881 hydrochloride |
CAS | 193000-39-4 |
Molecular Formula | C22H19ClFN3O2 |
Molar Mass | 411.8565632 |
Storage Condition | -20℃ |
In vitro study | ZM323881 inhibited 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) acts on the perfused mesenteric microvasculature of the male photon, abrogating the VEGF-A-mediated increase in vascular permeability. ZM323881(10 nM) acts on the lung of the male frog, and inhibits the increase of the intensity of the VEGF-R2 band. ZM323881(1 μm) acts on human aortic endothelial cells (HAECs) to inhibit VEGF-induced activation of extracellular regulated kinase, p38,Akt, and endothelial nitric oxide synthase (eNOS), but does not inhibit VEGFR-1 of the specific ligand, placental growth factor (PIGF)-induced activation of p38. ZM323881 (1 μm) acts on human aortic endothelial cells (HAECs) and interferes with VEGF-induced membrane elongation, cell migration and tube formation. ZM323881(1 μm) reversed the phosphorylation of VEGF-stimulated CrkII and its Src homology region 2(SH2) binding protein p130Cas, which plays a key role in regulating endothelial cell migration. ZM323881(10 nM) completely inhibited VEGF-induced VEGF promoter activity in SCC-9 cells. ZM323881(10 nM) inhibited VEGF-stimulated Hif-1α protein accumulation in SCC-9 cells. ZM323881(10 nM) inhibited VEGF-induced Rac1 activation in human umbilical vein endothelial cells (HUVECs) for 30 minutes. ZM323881(10 nM) acts on human umbilical vein endothelial cells (HUVECs) to inhibit Vav2 tyrosine phosphorylation in response to VEGF. ZM323881(< 1 μm) inhibited VEGF-stimulated neural stem cell proliferation in a dose-dependent manner. ZM323881(< 1 μm) inhibited neural stem cell proliferation in a dose-dependent manner, even in the absence of exogenous VEGF addition. |
Biological activity | ZM 323881 HCl is an effective, selective VEGFR2 inhibitor with an IC50 of <2 nM and almost no activity for VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2. |
in vitro study | ZM323881 inhibit the proliferation of HUVEC cells induced by VEGF-A, EGF and bFEF with IC50 of 8 nM, 1.9 μM and 1.6 μM respectively. ZM323881(10 nM) acts on perfused mesenteric microvessels of male leopards, abolishing VEGF-A-mediated increase in vascular permeability. ZM323881(10 nM) acts on the lungs of male leopard frogs, inhibiting the increase of VEGF-R2 band intensity. ZM323881(1 μM) acts on human aortic endothelial cells (HAECs) and inhibits the activation of extracellular regulatory kinases, p38,Akt, and endothelial nitric oxide synthase (eNOS) caused by VEGF, but does not inhibit the activation of p38 caused by VEGFR-1-specific ligand, placental growth factor (PIGF). ZM323881 (1 μM) acts on human aortic endothelial cells (HAECs), interfering with VEGF-induced membrane extension, cell migration and tube formation. ZM323881(1 μM) reverses VEGF-stimulated phosphorylation of CrkII and its Src homologous region 2(SH2)-binding protein p130Cas, which plays a key role in regulating endothelial cell migration. ZM323881(10 nM) acts on SCC-9 cells and completely inhibits VEGF-induced VEGF promoter activity. ZM323881(10 nM) acts on SCC-9 cells to inhibit VEGF-stimulated Hif-1α protein accumulation. ZM323881(10 nM) acts on human umbilical vein endothelial cells (HUVECs) for 30 minutes to inhibit VEGF-induced Rac1 activation. ZM323881(10 nM) acts on human umbilical vein endothelial cells (HUVECs) to inhibit Vav2 tyrosine phosphorylation in response to VEGF. ZM323881(< 1 μM) inhibited VEGF-stimulated proliferation of neural stem cells in a dose-dependent manner. ZM323881(< 1 μM) inhibits neural stem cell proliferation, which is dose-dependent, even in the absence of exogenous VEGF addition. |
target | VEGFR2 2 nM (IC 50 ) |