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Liu Z.,University of British Columbia | Hundal-Jabal N.,BC Cancer Research Agency | Wong M.,BC Cancer Research Agency | Yapp D.,BC Cancer Research Agency | And 3 more authors.
MedChemComm | Year: 2014

An 18F-heteroaryltrifluoroborate was designed as a novel radioprosthetic for PET imaging. The stability of the new prosthetic was confirmed using 19F-NMR spectroscopy: the solvolytic half-life was measured to be >16000 min. Conjugation to RGD gave a stable radiotracer precursor for kit-like labeling by 18F-19F isotope exchange in 15 min. The total radiosynthetic procedure including HPLC purification requires <45 min. A plasma stability assay showed negligible defluoridation following 150 min and stability is corroborated by in vivo imaging showing minimal bone uptake. With Curie levels of 18F- fluoride, yields of 20% and specific activities as high as 3 Ci μmol -1 (110 GBq μmol-1) are achieved (n = 3). © 2014 The Royal Society of Chemistry. Source

Liu Z.,University of British Columbia | Pourghiasian M.,BC Cancer Research Agency | Radtke M.A.,University of British Columbia | Lau J.,BC Cancer Research Agency | And 6 more authors.
Angewandte Chemie - International Edition | Year: 2014

A new zwitterionic organotrifluoroborate is appended to three radiosynthons that afford undergo facile bioconjugation to several clinically relevant peptides and one enzyme inhibitor. Molecularly complex bioconjugates are 18Flabeled in a single aqueous step in rapid time (< 15 min) without HPLC purification to afford tracers in good yields (> 200 mCi, 20-40%) at high specific activity (≥ 3 Ci/mmol) and at > 98% purity. PET imaging shows in vivo stability and tumor uptake. © 2014 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim. Source

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