ZM 323881 hydrochloride

Cat. No. 2475

ZM 323881 hydrochloride C22H18FN3O2.HCl [193000-39-4]

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Chemical Name: 5-((7-Benzyloxyquinazolin-4-yl)amino)-4-fluoro-2-methylphenol hydrochloride

Biological Activity

Potent and selective inhibitor of human vascular endothelial growth factor receptor 2 (VEGFR-2/KDR) activity. Selectively inhibits VEGFR-2 (IC50 = 2 nM) over VEGFR-1 and a range of other receptor tyrosine kinases such as PDGFRβ, FGFR1, EGFR and erbB2 (IC50 > 50 μM). Inhibits VEGF-A-induced endothelial cell proliferation in vitro (IC50 = 8 nM).

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

Technical Data

M.Wt:
411.86
Formula:
C22H18FN3O2.HCl
Solubility:
Soluble to 50 mM in DMSO
Purity:
>99 %
Storage:
Desiccate at +4°C
CAS No:
193000-39-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Endo et al (2003) Selective inhibition of vascular endothelial growth factor receptor-2 (VEGFR-2) identifies a central role for VEGFR-2 in human aortic endothelial cell responses to VEGF. J.Recept.Signal Transduct.Res. 23 239. PMID: 14626450.

Whittles et al (2002) ZM323881, a novel inhibitor of vascular endothelial growth factor-receptor-2 tyrosine kinase activity. Microcirculation 9 513. PMID: 12483548.

If you know of a relevant reference for ZM 323881 hydrochloride please let us know.

Citations are publications that use Tocris products. Selected citations for ZM 323881 hydrochloride include:

Maertens et al (2014) Bone marrow-derived mesenchymal stem cells drive lymphangiogenesis. Arterioscler Thromb Vasc Biol 9 e106976. PMID: 25222747.

Kawakami et al (2011) Investigation of a novel molecular descriptor for the lead optimization of 4-aminoquinazolines as vascular endothelial growth factor receptor-2 inhibitors: application for quantitative structure-activity relationship analysis in lead optimization. PLoS One 21 1371. PMID: 21306896.

Zhong et al (2011) Combinatory action of VEGFR2 and MAP kinase pathways maintains endothelial-cell integrity. Cell Res 21 1080. PMID: 21423276.

Chandrasekharan et al (2010) Synergistic induction of mitogen-activated protein kinase phosphatase-1 by thrombin and epidermal growth factor requires vascular endothelial growth factor receptor-2. Biomed Rep 30 1983. PMID: 20671228.

Holmes et al (2010) VEGF stimulates RCAN1.4 expression in endothelial cells via a pathway requiring Ca2+/calcineurin and protein kinase C-delta. PLoS One 5 e11435. PMID: 20625401.

Do you know of a great paper that uses ZM 323881 hydrochloride from Tocris? If so please let us know.show all ▼show less ▲

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