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ZM 323881 hydrochloride

Catalog #: 2475
11 Citations Datasheet
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ZM 323881 hydrochloride | CAS No. 193000-39-4 | VEGF Receptor Inhibitors
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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%

Product Details
Citations (11)
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Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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).

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

Additional Information

Licensing Caveats:
Sold with the permission of AstraZeneca UK Ltd.

Background References

  1. Bone marrow-derived mesenchymal stem cells drive lymphangiogenesis.
    Maertens L, Erpicum C, Detry B, Blacher S, Lenoir B, Carnet O, Pequeux C, Cataldo D, Lecomte J, Paupert J, Noel A
    PLoS ONE, 2014;9(9):e106976.
  2. uPARAP/Endo180 receptor is a gatekeeper of VEGFR-2/VEGFR-3 heterodimerisation during pathological lymphangiogenesis
    T Durré, F Morfoisse, C Erpicum, M Ebroin, S Blacher, M García-Cab, C Deroanne, T Louis, C Balsat, M Van de Vel, S Kaijalaine, F Kridelka, L Engelholm, I Struman, K Alitalo, N Behrendt, J Paupert, A Noel
    Nat Commun, 2018;9(1):5178.
  3. The control of alternative splicing by SRSF1 in myelinated afferents contributes to the development of neuropathic pain

    Neurobiol Dis, 2016;96(0):186-200.
  4. ZM323881, a novel inhibitor of vascular endothelial growth factor-receptor-2 tyrosine kinase activity.
    Whittles et al.
    Microcirculation, 2002;9:513
  5. 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.
    Endo et al.
    J.Recept.Signal Transduct.Res., 2003;23:239

Product Datasheets

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Citations for ZM 323881 hydrochloride

The citations listed below are publications that use Tocris products. Selected citations for ZM 323881 hydrochloride include:

11 Citations: Showing 1 - 10

  1. Positive Feedback Defines the Timing, Magnitude, and Robustness of Angiogenesis.
    Authors: Page Et al.
    Cell Rep  2019;27:3139
  2. uPARAP/Endo180 receptor is a gatekeeper of VEGFR-2/VEGFR-3 heterodimerisation during pathological lymphangiogenesis.
    Authors: Durré Et al.
    Nat Commun  2018;9:5178
  3. Dickkopf-3 Causes Neuroprotection by Inducing Vascular Endothelial Growth Factor.
    Authors: Busceti Et al.
    Front Cell Neurosci  2018;12:292
  4. The control of alternative splicing by SRSF1 in myelinated afferents contributes to the development of neuropathic pain.
    Authors: Hulse Et al.
    Neurobiol Dis  2016;96:186
  5. Bone marrow-derived mesenchymal stem cells drive lymphangiogenesis.
    Authors: Maertens Et al.
    Arterioscler Thromb Vasc Biol  2014;9:e106976
  6. 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.
    Authors: Kawakami Et al.
    PLoS One  2011;21:1371
  7. Combinatory action of VEGFR2 and MAP kinase pathways maintains endothelial-cell integrity.
    Authors: Zhong Et al.
    Cell Res  2011;21:1080
  8. Rap1 promotes VEGFR2 activation and angiogenesis by a mechanism involving integrin αvβ?.
    Authors: Lakshmikanthan Et al.
    Blood  2011;118:2015
  9. VEGF stimulates RCAN1.4 expression in endothelial cells via a pathway requiring Ca2+/calcineurin and protein kinase C-delta.
    Authors: Holmes Et al.
    PLoS One  2010;5:e11435
  10. Pharmacological and genetic accumulation of hypoxia-inducible factor-1alpha enhances excitatory synaptic transmission in hippocampal neurons through the production of vascular endothelial growth factor.
    Authors: Huang Et al.
    J Neurosci  2010;30:6080

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