ZM 323881 hydrochloride

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Description: Potent, selective inhibitor of VEGFR-2
Chemical Name: 5-((7-Benzyloxyquinazolin-4-yl)amino)-4-fluoro-2-methylphenol hydrochloride
Purity: ≥99% (HPLC)
Citations (11)
Literature (1)
Pathways (1)

Biological Activity for ZM 323881 hydrochloride

ZM 323881 hydrochloride is a 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.

Compound Libraries for ZM 323881 hydrochloride

ZM 323881 hydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for ZM 323881 hydrochloride

M. Wt 411.86
Formula C22H18FN3O2.HCl
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 193000-39-4
PubChem ID 22624897
Smiles Cl.CC1=C(O)C=C(NC2=C3C=CC(OCC4=CC=CC=C4)=CC3=NC=N2)C(F)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for ZM 323881 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 20.59 50

Preparing Stock Solutions for ZM 323881 hydrochloride

The following data is based on the product molecular weight 411.86. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.86 mL 24.28 mL 48.56 mL
2.5 mM 0.97 mL 4.86 mL 9.71 mL
5 mM 0.49 mL 2.43 mL 4.86 mL
25 mM 0.1 mL 0.49 mL 0.97 mL

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Product Datasheets for ZM 323881 hydrochloride

Certificate of Analysis / Product Datasheet
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References for ZM 323881 hydrochloride

References are publications that support the biological activity of the product.

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

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

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View Related Products by Product Action

View all VEGFR Inhibitors

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11 Citations for ZM 323881 hydrochloride

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

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

Busceti et al (2018) Dickkopf-3 Causes Neuroprotection by Inducing Vascular Endothelial Growth Factor. Front Cell Neurosci 12 292 PMID: 30258353

Durré et al (2018) uPARAP/Endo180 receptor is a gatekeeper of VEGFR-2/VEGFR-3 heterodimerisation during pathological lymphangiogenesis. Nat Commun 9 5178 PMID: 30518756

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

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for ZM 323881 hydrochloride

VEGF Signaling Pathway

VEGF Signaling Pathway

VEGF signaling pathway is involved in embryonic vascular development (vasculogenesis) and in the formation of new blood vessel (angiogenesis). It also induces cell migration, proliferation and survival.