Abstract
In this study, we developed a saccharin (SAC)-based radiopharmaceutical (68Ga-NOTA-SAC) and evaluated the possibility of its application as a PET tracer in the diagnosis of carbonic anhydrase IX (CA IX)-overexpressed tumors. We did a water-soluble tetrazolium assay and flow cytometry analysis to identify the cell viability decrease by SAC. The radiochemical purity and stability of 68Ga- NOTA-SAC in human and mouse serum was greater than 98%. The small animal PET image-based radioactivity distribution of all organs decreased over time.68Ga-NOTA-SAC presented the highest tumor-to-muscle ratio at 90 min post injection (p.i). The growth rates of tumor-to-muscle ratios of 68Ga-NOTA-SAC were 88% at 60 min and 220% at 90 min, compared to 30 min p.i. The potential of 68Ga-NOTA-SAC as a PET tracer is expected to contribute to the diagnostic research on CA IX-overexpressed tumors with the advantages of a relatively simple synthesis method.
Original language | English |
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Pages (from-to) | 129-139 |
Number of pages | 11 |
Journal | Journal of Labelled Compounds and Radiopharmaceuticals |
Volume | 64 |
Issue number | 3 |
DOIs | |
Publication status | Published - 2021 Mar |
Bibliographical note
Funding Information:This work was supported by Kyung‐In Synthetic Corporation (KISCO) and a Korea University Grant.
Publisher Copyright:
© 2020 The Authors. Journal of Labelled Compounds and Radiopharmaceuticals published by John Wiley & Sons Ltd
Keywords
- Carbonic anhydrase IX
- Ga-NOTA-SAC
- PET tracer
- Saccharin
- U87MG
ASJC Scopus subject areas
- Analytical Chemistry
- Biochemistry
- Radiology Nuclear Medicine and imaging
- Drug Discovery
- Spectroscopy
- Organic Chemistry