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V-9402 Vandetanib, Free Base, >99%

[Caprelsa] [Zactima] [ZD6474] [ZD-6474] [ZD 6474]

M.W. 475.35

C22H24BrFN4O2

[443913-73-3]

M.I. 14:  10249

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 30 mg/mL; soluble in ethanol at 10 mg/mL with warming; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-20 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Appearance:  White solid.  Disposal:  A

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• Vandetanib 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).

• 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.  Azzariti, 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).

• 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).  Wedge S.R., et al.  "ZD6474 Inhibits Vascular Endothelial Growth Factor Signaling, Angiogenesis, and Tumor Growth following Oral Administration."  Cancer Res. 62:  4645-4655 (2002).

• 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.  Ciardiello F., et al.  "Antitumor Effects of ZD6474, a Small Molecule Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor, with Additional Activity against Epidermal Growth Factor Receptor Tyrosine Kinase."  Clin. Cancer Res. 9:  1546-1556 (2003).

• 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.  NOTE:  The vandetanib sold by LC Laboratories is NOT Caprelsa®, and is NOT for human use.

• Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.