Vandetanib-d6 is intended for use as an internal standard for the quantification of Vandetanib by GC- or LC-MS. Vandetanib is a broad spectrum, orally available kinase inhibitor that targets primarily tyrosine kinases, including vascular endothelial growth factor receptor (VEGFR) and epidermal growth factor receptor (EGFR), with IC50 values in the nanomolar range.1,2 It also potently blocks non-receptor tyrosine kinases, including ABL, RET, and SRC, as well as several serine/threonine kinases.3,4 Primarily because of its effects on receptor tyrosine kinases like VEGFR and EGFR, vandetanib inhibits angiogenesis, cell growth, and metastasis and is effective against certain forms of cancer.4,5
|1. Kiselyov, A.S., Piatnitski, E., Milligan, D., et al. 1H-1,2,4-Triazol-3-yl-anilines: Novel potent inhibitors of vascular endothelial growth factor receptors 1 and 2. Chem.Biol.Drug Des. 69(5), 331-337 (2007).|2. Hennequin, L.F., Stokes, E.S.E., Thomas, A.P., et al. Novel 4-anilinoquinazolines with C-7 basic side chains: Design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors. Journal of Medicinal Chemistry 45(6), 1300-1312 (2002).|3. Davis, M.I., Hunt, J.P., Herrgard, S., et al. Comprehensive analysis of kinase inhibitor selectivity. Nat.Biotechnol. 29(11), 1046-1051 (2011).|4. Morabito, A., Piccirillo, M.C., Falasconi, F., et al. Vandetanib (ZD6474), a dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and epidermal growth factor receptor (EGFR) tyrosine kinases: Current status and future directions. Oncologist 14(4), 378-390 (2009).|5. Ton, G.N., Banaszynski, M.E., and Kolesar, J.M. Vandetanib: A novel targeted therapy for the treatment of metastatic or locally advanced medullary thyroid cancer. Am. J. Health Syst. Pharm. 70(10), 849-855 (2013).