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10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
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Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
ZM 323881 is a potent and selectiveVEGFR2inhibitor withIC50of <2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2.
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. 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.
In vivo
Cell Data
cell lines:SK-MES-1
Concentrations:
Incubation Time:
Powder Purity:≥99%
| Isomeric SMILES | CC1=CC(=C(C=C1O)NC2=NC=NC3=C2C=CC(=C3)OCC4=CC=CC=C4)F.Cl |
|---|---|
| Alternate CAS | 193001-14-8 |
| Molecular Weight | 411.86 |
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View spec sheet →| Solubility | Solubility (25°C) In vitro DMSO: 65 mg/mL (199.28 mM); Water: Insoluble; Ethanol: Insoluble; |
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