Vandetanib, Free Base (Caprelsa, Zactima, ZD6474, CAS 443913-73-3), >99%

LC Laboratories' Product Number V-9402 - Vandetanib, Free Base (Caprelsa, Zactima, ZD6474), >99% - for research use only. Vandetanib inhibits VEGFR-dependent tumor angiogenesis and EGFR- and RET-dependent tumor cell proliferation and survival. 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). Vandetanib dose-dependently inhibited EGFR tyrosine kinase activity with IC50 of 0.25 µM. Vandetanib also inhibited colony formation of seven cancer cell lines in soft agar with IC50's ranging between 0.5 and 1 µM. Vandetanib is the active ingredient in the drug sold under the trade name Caprelsa® and has been approved in at least one country for treatment of patients with follicular, medullary, anaplastic, and locally advanced and metastatic papillary thyroid cancer.

• Supplier: LC Laboratories
• Product #: V-9402
• Sku #: V-9402_1g