Antitumor activity of oxali-titanocene Y in xenografted CAKI-1 tumors in mice

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Item Type:	Article
Title:	Antitumor activity of oxali-titanocene Y in xenografted CAKI-1 tumors in mice
Creators Name:	Fichtner, I., Behrens, D., Claffey, J., Gleeson, B., Hogan, M., Wallis, D., Weber, H. and Tacke, M.
Abstract:	The para-methoxybenzyl-substituted titanocene oxalate (Oxali-Titanocene Y) was tested in vitro in an anti-angiogenesis assay against human umbilical vein endothelial cells, HUVEC, delivering an IC50 value of 14 mu M and in a cytotoxicity assay against the human renal cancer cells, CAKI-1, which demonstrated an IC50 value greater than 100 mu M. Then Oxali-Titanocene Y was given at 30 mg/kg/d, which is the maximum tolerable dose, on five consecutive days per week for three weeks to one cohort of eight CAKI-1 tumor-bearing female NMRI:nu/nu mice, while a second cohort was treated with solvent only. The titanocene-treated mouse cohort showed a statistically significant tumor growth reduction with respect to the solvent-treated control group with an optimal T/C value of 38% at the end of the experiment. Immunohistological analysis revealed that the expression of the proliferation marker Ki-67 was reduced by 30%. Furthermore, an anti-angiogenic activity was identified by CD31 staining; the number of micro vessels in a defined tumor area was significantly decreased due to Oxali-Titanocene Y treatment.
Keywords:	Anti-Cancer Drug, Titanocene, Renal-Cell Cancer, CAKI-1, Cytotoxicity, Xenograft, HUVEC, Anti-Angiogenesis, Animals, Mice
Source:	Letters in Drug Design & Discovery
ISSN:	1570-1808
Publisher:	Bentham
Volume:	5
Number:	8
Page Range:	489-493
Date:	December 2008
Official Publication:	https://doi.org/10.2174/157018008786898545

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