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12616
Vandetanib 
Activators & Inhibitors
Chemical Modulators

Vandetanib  #12616

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Vandetanib : Image 1
Western blot analysis of extracts from HUVE cells serum-starved overnight, untreated (-) or pre-treated with Vandetanib (5 µM, 2 hr; +) and treated with Human Vascular Endothelial Growth Factor-165 (hVEGF165) #8065 (50 ng/ml, 5 min; +) as indicated, using Phospho-VEGF Receptor 2 (Tyr1175) (19A10) Rabbit mAb #2478 (upper) or VEGF Receptor 2 (55B11) Rabbit mAb #2479 (lower).
Vandetanib : Image 2
Chemical structure of vandetanib.

Product Usage Information

Vandetanib is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 5 mg in 1.05 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 1-10 µM for 0.5-2 hr prior to treating with a stimulator. It can also be used alone, with varying treatment times lasting up to 24 hr. Soluble in DMSO at 30 mg/ml; soluble in ethanol at 10 mg/ml with warming; very poorly soluble in water with maximum ~10-20 µM.

Storage

Store lyophilized or in solution at -20ºC, desiccated. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Product Description

Molecular Weight 475.35 g/mol
Purity >99%
Molecular Formula C22H24BrFN4O2
CAS 443913-73-3
Solubility Soluble in DMSO at 30mg/ml and EtOH at 10mg/ml.

Background

Vandetanib, also known as ZD6474, is a selective inhibitor of VEGFR and EGFR tyrosine kinases (1-5). Researchers have shown that vandetanib inhibits VEGFR-2, VEGFR-3, and EGFR in recombinant enzyme assays with IC50 values of 40 nM, 108 nM, and 500 nM, respectively, and had selectivity over a variety of other tyrosine and serine/threonine kinases (2). Vandetanib inhibits VEGF and EGF stimulated proliferation of HUVE cells with an IC50 of 60 nM and 170 nM, respectively (2), and effectively blocks VEGF and EGF induced autophosphorylation (3-5). Inhibition of RET by vandetanib has also been observed (6).
  1. Morabito, A. et al. (2009) Oncologist 14, 378-90.
  2. Wedge, S.R. et al. (2002) Cancer Res 62, 4645-55.
  3. Jane, E.P. et al. (2009) J Pharmacol Exp Ther 331, 327-37.
  4. McCarty, M.F. et al. (2004) Mol Cancer Ther 3, 1041-8.
  5. Ciardiello, F. et al. (2003) Clin Cancer Res 9, 1546-56.
  6. Carlomagno, F. et al. (2002) Cancer Res 62, 7284-90.

Limited Uses

Except as otherwise expressly agreed in a writing signed by a legally authorized representative of CST, the following terms apply to Products provided by CST, its affiliates or its distributors. Any Customer's terms and conditions that are in addition to, or different from, those contained herein, unless separately accepted in writing by a legally authorized representative of CST, are rejected and are of no force or effect.

Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

For Research Use Only. Not For Use In Diagnostic Procedures.
Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
To Purchase # 12616
Cat. # Size Qty. Price
12616S
5 mg $ 133