Sc-HOPO: A potential construct for use in radioscandium-based radiopharmaceuticals Journal Article


Authors: Phipps, M. D.; Cingoranelli, S.; Bhupathiraju, N. V. S. D. K.; Younes, A.; Cao, M.; Sanders, V. A.; Neary, M. C.; Devany, M. H.; Cutler, C. S.; Lopez, G. E.; Saini, S.; Parker, C. C.; Fernandez, S. R.; Lewis, J. S.; Lapi, S. E.; Francesconi, L. C.; Deri, M. A.
Article Title: Sc-HOPO: A potential construct for use in radioscandium-based radiopharmaceuticals
Abstract: Three isotopes of scandium-43Sc, 44Sc, and 47Sc- have attracted increasing attention as potential candidates for use in imaging and therapy, respectively, as well as for possible theranostic use as an elementally matched pair. Here, we present the octadentate chelator 3,4,3-(LI-1,2-HOPO) (or HOPO), an effective chelator for hard cations, as a potential ligand for use in radioscandium constructs with simple radiolabeling under mild conditions. HOPO forms a 1:1 Sc-HOPO complex that was fully characterized, both experimentally and theoretically. [47Sc]Sc-HOPO exhibited good stability in chemical and biological challenges over 7 days. In healthy mice, [43,47Sc]Sc-HOPO cleared the body rapidly with no signs of demetalation. HOPO is a strong candidate for use in radioscandium-based radiopharmaceuticals.
Keywords: chemistry; chelation; agents; stability; dota; dtpa; pcm; basis-sets; scandium(iii) complexes; sc-44
Journal Title: Inorganic Chemistry
Volume: 62
Issue: 50
ISSN: 0020-1669
Publisher: ACS Publications  
Date Published: 2023-12-18
Start Page: 20567
End Page: 20581
Language: English
ACCESSION: WOS:000927035600001
DOI: 10.1021/acs.inorgchem.2c03931
PROVIDER: wos
PMCID: PMC10390652
PUBMED: 36724083
Notes: Article -- Source: Wos
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  1. Jason S Lewis
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  2. Michael David Phipps
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