Chemical Name : AG-1478 hydrochloride/
CAS : 153436-53-4
Solubility:Soluble in DMSO at 30mg/ml
Storage:-20C 2 years
The IC50 values for vandetanib in HT-29 and LoVo cells are 10-80 µM and 3.5-16 µM, respectively, when the exposure times are from 3 days to 18 hours.Vandetanib is a potent, orally-active inhibitor of kinase insert domain-containing receptor [KDR/vascular endothelial growth factor receptor (VEGFR) 2] tyrosine kinase activity (IC50 = 40 nM). This compound also inhibits fms-like tyrosine kinase 4 (VEGFR3, IC50 = 110 nM) and epidermal growth factor receptor (EGFR/HER1, IC50 = 500 nM) but shows selectivity relating to a range of other tyrosine and serine-threonine kinases. The activity of vandetanib against KDR tyrosine kinase may explain its potent inhibition of vascular endothelial growth factor A-stimulated human umbilical vein endothelial cell proliferation in vitro (IC50 = 60 nM).
1Vandetanib inhibits VEGFR-dependent tumor angiogenesis and EGFR- and RET-dependent tumor cell proliferation and survival. Herbst, R.S., et al. "Vandetanib (ZD6474): an orally available receptor tyrosine kinase inhibitor that selectively targets pathways critical for tumor growth and angiogenesis." Expert Opin. Investig. Drugs 16: 239-249 (2007).
2Azzariti, A., et al. "Prolonged exposure of colon cancer cells to the epidermal growth factor receptor inhibitor gefitinib (Iressa) and to the antiangiogenic agent ZD6474: Cytotoxic and biomolecular effects." World J. Gastroenterol. 12: 5140-5147 (2006).
3Wedge S.R., et al. "ZD6474 Inhibits Vascular Endothelial Growth Factor Signaling, Angiogenesis, and Tumor Growth following Oral Administration." Cancer Res. 62: 4645-4655 (2002).