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Submit ReviewZM 323881 hydrochloride
Description: Potent, selective inhibitor of VEGFR-2
Chemical Name: 5-((7-Benzyloxyquinazolin-4-yl)amino)-4-fluoro-2-methylphenol hydrochloride
Purity: ≥99% (HPLC)
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 |
| 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.
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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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
If you know of a relevant reference for ZM 323881 hydrochloride, please let us know.
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11 Citations for ZM 323881 hydrochloride
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
Zhong et al (2011) Combinatory action of VEGFR2 and MAP kinase pathways maintains endothelial-cell integrity. Cell Res 21 1080 PMID: 21423276
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
Lakshmikanthan et al (2011) Rap1 promotes VEGFR2 activation and angiogenesis by a mechanism involving integrin αvβ?. Blood 118 2015 PMID: 21636859
Huang et al (2010) Pharmacological and genetic accumulation of hypoxia-inducible factor-1alpha enhances excitatory synaptic transmission in hippocampal neurons through the production of vascular endothelial growth factor. J Neurosci 30 6080 PMID: 20427666
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
Page et al (2019) Positive Feedback Defines the Timing, Magnitude, and Robustness of Angiogenesis. Cell Rep 27 3139 PMID: 31189101
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
Hulse et al (2016) The control of alternative splicing by SRSF1 in myelinated afferents contributes to the development of neuropathic pain. Neurobiol Dis 96 186 PMID: 27616424
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
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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
