Preparation of [45Ti] Ti-salan-dipic

Gregory W. Severin, Andreas Tue Ingemann Jensen, Jesper Fonslet, Fedor Zhuravlev

    Research output: Contribution to journalConference abstract in journalResearchpeer-review

    Abstract

    We report the carrier-free radiochemical synthesis of a neutral, bio-active, titanium-45 complex, [45Ti]Ti-salan-dipic. In 2012, the Huhn group at Universität Konstanz reported the non-radioactive compound, Ti-salan-dipic, and demonstrated therapeutic efficacy in a xenograft cervical cancer mouse model as well as enhanced in-vitro cytotoxicity over several other titanium-based chemotherapeutics [1]. The mechanism of action for this class of therapeutics is under investigation and the determination of which will be aided by radiotracing and PET with 45Ti.
    45Ti was prepared by proton irradiation of natSc foil followed by extraction onto a polystyrene-based diol-resin (RAPP polymers) after dissolution of the foil in 37% HCl. Synthesis proceeded on the column after quenching the residual acidity with pyridine. The ligands, salan and dipic, were added sequentially in pyridine, with the release of the final compound upon ligand exchange to dipic. [45Ti]Ti-salan-dipic was characterized by radio-TLC on silica in 1:1 ethylacetate:chloroform in comparison to the cold compound.
    This is a hydrolytically stable, cytotoxic, 45Ti compound. The solid-phase synthesis is robust, and provides opportunity for producing other 45Ti tracers. PET and radiotracer studies with [45Ti]Ti-salan-dipic and other Ti-based cytotoxic compounds will aid in mechanism determination, drug design, and eventually more effective treatment of cancer.
    Original languageEnglish
    JournalNuclear Medicine and Biology
    Volume41
    Issue number7
    Pages (from-to)632-632
    Number of pages1
    ISSN0969-8051
    DOIs
    Publication statusPublished - 2014
    Event2nd International Symposium on Technetium and other Radiometals in Chemistry and Medicine - Bolzano, Italy
    Duration: 10 Sep 201413 Sep 2014
    Conference number: 2
    http://www.terachem2014.com/

    Conference

    Conference2nd International Symposium on Technetium and other Radiometals in Chemistry and Medicine
    Number2
    Country/TerritoryItaly
    CityBolzano
    Period10/09/201413/09/2014
    Internet address

    Keywords

    • RADIOLOGY,

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