Synthesis, Physicochemical, Labeling and In Vivo Characterization of ⁴⁴Sc-Labeled DO3AM-NI as a Hypoxia-Sensitive PET Probe.

ABSTRACT: Hypoxia promotes angiogenesis, which is crucial for tumor growth, and induces malignant progression and increases the therapeutic resistance. Positron emission tomography (PET) enables the detection of the hypoxic regions in tumors using 2-nitroimidazole-based radiopharmaceuticals. We describe here a physicochemical study of the Sc(DO3AM-NI) complex, which indicates: (a) relatively slow formation of the Sc(DO3AM-NI) chelate in acidic solution; (b) lower thermodynamic stability than the reference Sc(DOTA); (c) however, it is substantially more inert and consequently can be regarded as an excellent Sc-binder system. In addition, we report a comparison of ⁴⁴Sc-labeled DO3AM-NI with its known ⁶⁸Ga-labeled analog as a hypoxia PET probe. The in vivo and ex vivo biodistribut

SUBMITTER: Szucs D 

PROVIDER: S-EPMC9228955 | biostudies-literature | 2022 May

REPOSITORIES: biostudies-literature