Extensive structure-activity relationships studies have previously shown that alkylphosphocholine (APC) analogs selectively deliver radioiodine and larger fluorophores to a variety of tumor types in rodent models and humans1-3. To further explore the payload capacity of APCs, we synthesized several new APC-chelates and assessed their ability to deliver Gd (MRI) and 64Cu (PET) selectively to tumors in vivo. Prolonged T1-weighted signal enhancement following Gd-DOTA-APC injection was observed in all tumor models. Clinical PET/MR imaging of U87 flank xenograft at 24h and 48h post-administration of Gd-DOTA-APC and 64Cu-DOTA-APC demonstrated co-localization of T1-weighted signal enhancement and PET activity in the tumor.
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