product name ZM 323881 HCl
Description: ZM 323881 is a potent and selective VEGFR2 tyrosine kinase inhibitorwith IC50 of <2 nM, it almost has no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2. ZM323881. ZM323881 inhibits VEGF-A-induced endothelial cell proliferation (IC50 = 8 nM) and VEGF-R2 tyrosine phosphorylation in vitro. ZM323881 (10 nM) blocks VEGF-induced Rac1 activation at 30 min in HUVECs.
References: Microcirculation. 2002 Dec;9(6):513-22; Biochem Biophys Res Commun. 2006 Apr 14;342(3):851-8.
411.86
Formula
C22H18FN3O2.HCl
CAS No.
193000-39-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 10 mg/mL (24.3 mM)
Water: <1 mg/mL
Ethanol:<1 mg/mL
Solubility (In vivo)
1% CMC Na: 20 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 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. 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. 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. 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. 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. Kinase Assay: Cell Assay: |
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| In Vivo | |
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| Formulation & Dosage | |
| References | Microcirculation. 2002 Dec;9(6):513-22; Biochem Biophys Res Commun. 2006 Apr 14;342(3):851-8. |
