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ZM 323881 hydrochloride
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).
Sold with the permission of AstraZeneca UK Ltd.
|Storage||Desiccate at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 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|
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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11 Citations for ZM 323881 hydrochloride
Citations are publications that use Tocris products. Selected citations for ZM 323881 hydrochloride include:
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
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
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
Page et al (2019) Positive Feedback Defines the Timing, Magnitude, and Robustness of Angiogenesis. Cell Rep 27 3139 PMID: 31189101
Lakshmikanthan et al (2011) Rap1 promotes VEGFR2 activation and angiogenesis by a mechanism involving integrin αvβ?. Blood 118 2015 PMID: 21636859
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
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
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
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