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Inorg Chem. 2019 Feb 18;58(4):2275-2285. doi: 10.1021/acs.inorgchem.8b01208. Epub 2018 Jul 10.

H2hox: Dual-Channel Oxine-Derived Acyclic Chelating Ligand for 68Ga Radiopharmaceuticals.

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Medicinal Inorganic Chemistry Group, Department of Chemistry , University of British Columbia , 2036 Main Mall , Vancouver , British Columbia V6T 1Z1 , Canada.
BC Cancer Agency , 675 West 10th Avenue , Vancouver , British Columbia V5Z 1L3 , Canada.


An acyclic hexadentate oxine-derived chelating ligand, H2hox, was investigated as an alternative to current chelators for 68Ga. The straightforward preparation of H2hox, involving only one or two steps, obviates the synthetic challenges associated with many reported 68Ga chelators; it forms a Ga3+ complex of great stability (log K = 34.4) with a remarkably high gallium scavenging ability (pGa3+ = -log[Ga3+free] = 28.3, ([Ga3+] = 1 μM; [L x-] = 10 μM; pH 7.4, and 25 °C)). Moreover, H2hox coordinates 68Ga quantitatively in 5 min at room temperature in ligand concentrations as low as 1 × 10-7 M, achieving an unprecedented high molar activity of 11 ± 1 mCi/nmol (407 ± 3.7 MBq/nmol) without purification, suggesting prospective kit-based convenience. [68Ga(hox)]+ showed no decomposition in a plasma challenge. Good in vivo stability and fast renal and hepatic clearance of the [68Ga(hox)]+ complex were demonstrated using dynamic positron emission tomography/computed tomography imaging. The intrinsic fluorescence of [Ga(hox)]+ allowed for direct fluorescence imaging of cellular uptake and distribution, demonstrating the dual-channel detectability and intracellular stability of the metal complex.

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