In vitro cytotoxic activity of tri-n-butyltin(IV)lupinylsulfide hydrogen fumarate (IST-FS 35) and preliminary antitumor activity in vivo

Angela Alama, Maurizio Viale, Michele Cilli, Cristina Bruzzo, Federica Novelli, Bruno Tasso, Fabio Sparatore

Research output: Contribution to journalArticlepeer-review

Abstract

The cytotoxicity in vitro and antitumor activity in vivo of the organotin compound tri-n-butyltin(IV)lupinylsulfide hydrogen fumarate (IST-FS 35) have been investigated. The IC50 values obtained in a panel of tumor cell lines were compared to those of the parental compound IST-FS 29 in the same cells. IST-FS 35 resulted significantly more active than IST-FS 29 with IC50 values in the range 0.16-1.8 μM. Toxicity studies in vivo, after intravenous administration of escalating concentrations of IST-FS 35, provided the identification of the maximal tolerated dose (3.5 mg/kg) which was employed as therapeutic dose in the antitumor activity experiments. Preliminary results, in transplanted murine tumor models, revealed that both the P388 myelomonocytic leukaemia and the B16-F10 melanoma, implanted subcutaneously in BDF1 mice, were inhibited about 96% in their tumor volume at day 11, following a single intravenous injection of the compound. Additional studies are mandatory to unravel the mechanism of action for the development of IST-FS 35 as potential antitumor drug.

Original languageEnglish
Pages (from-to)124-130
Number of pages7
JournalInvestigational New Drugs
Volume27
Issue number2
DOIs
Publication statusPublished - Apr 2009

Keywords

  • Antitumor activity
  • Cytotoxicity
  • In vivo
  • Murine tumors
  • Organotin

ASJC Scopus subject areas

  • Oncology
  • Pharmacology (medical)
  • Pharmacology

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