ZM 323881 hydrochloride

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Cat.No. 2475 - ZM 323881 hydrochloride | C22H18FN3O2.HCl | CAS No. 193000-39-4
Description: Potent, selective inhibitor of VEGFR-2
Chemical Name: 5-((7-Benzyloxyquinazolin-4-yl)amino)-4-fluoro-2-methylphenol hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (5)
Literature
Pathways

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.

Compound Libraries

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

Technical Data

M. Wt 411.86
Formula C22H18FN3O2.HCl
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 193000-39-4
PubChem ID 22624897
InChI Key AVRHWGLIYGJSOD-UHFFFAOYSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 411.86. Batch specific molecular weights may vary from batch to batch due to solvent 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
1 mM 2.43 mL 12.14 mL 24.28 mL
5 mM 0.49 mL 2.43 mL 4.86 mL
10 mM 0.24 mL 1.21 mL 2.43 mL
50 mM 0.05 mL 0.24 mL 0.49 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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

Keywords: ZM 323881 hydrochloride, supplier, Potent, selective, inhibitors, inhibits, VEGFR-2, Vascular, Endothelial, Growth, Factor, Receptors, KDR, Flt, Receptor, Tyrosine, Kinases, RTKs, ZM323881, hydrochloride, AstraZeneca, VEGFR, VEGFR, Tocris Bioscience

5 Citations for ZM 323881 hydrochloride

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

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

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

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

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

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


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

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Reviews

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, 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

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.

Protocols

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