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ZD6474 (Vandetanib) | KDR/VEGFR2 inhibitor

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Price:
$89.00
Catalog #:
C9364-10
Quantity:


Product Description

Vandetanib (ZD6474) is an orallly-bioavailable, ATP-competitive, quinazoline-based inhibitor of VEGFR2 that has been shown to inhibit both VEGF-induced signalling in endothelial cells and tumor-induced angiogenesis. [1] Vandetanib inhibits VEGFR2, VEGFR3, EGFR, and RET at IC50s of 40 nM, 110 nM, 500 nM, and 130 nM, respectively. It has been found to inhibit cell proflieration of VEGFR-stimulated cells (IC50 60 nM) and EGFR-stimulated HUVEC proliferation (IC50 170 nM). [2]

Vandetanib shows robust inhibition of VEGF-stimulated VEGFR2 phosphorylation, Erk-1/2 phosphorylation, as well as endothelial cell proliferation at doses less than 100 nM. [3]

More recently, Vandetanib has been shown to antagonize ABCC1- and ABCG2-mediated MDR by inhibition of transport function. ABCG2, expressed in a wide variety of cancer stem cells, is inhibited by vandetanib, potentially reversing MDR at low concentrations. [4]


Technical information:

Chemical Formula:   C22H24BrFN4O2
CAS #:   443913-73-3
Molecular Weight:   475.35
Purity:   >98%
Appearance:   White
Chemical Name:   N-(4-bromo-2-fluorophenyl)-6-methoxy-7-((1-methylpiperidin-4-yl)methoxy)quinazolin-4-amine
Solubility:   Up to 40 mM in DMSO
Synonyms:   ZD6474, ZD-6474, Vandetanib, Zactima

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


Reference:

1. Ryan et al., Clin. Cancer 2005, 92, S6-S13.
2. Flanigan et al., Current status of vandetanib (ZD6474) in the treatment of non-small cell lung cancer. Biologics: Targets and Therapy, 2010, 4, 237-243. Pubmed ID: 20859451
3. McCarty et al., ZD6474, a vascular endothelial growth factor receptor tyrosine kinase inhibitor with additional activity against epidermal growth factor receptor tyrosine kinase, inhibits orthotopic growth and angiogenesis of gastric cancer. Mol. Cancer Ther. 2004, 3(9), 1041-1048. Pubmed ID: 15367698
4. Zheng et al., Vandetanib (Zactima, ZD6474) antagonizes ABCC1- and ABCG2-mediated multidrug resistance by inhibition of their transport function. PLoSONE, 2009, 4(4), e5172. Pubmed ID: 20859451

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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