Development of a Ga-68-labelled PET tracer for carbonic anhydrase IX-overexpressed tumors using the artificial sweetener saccharin
- Authors
- Shin, Un Chul; Choi, Jeong Su; Beak, Yeon Jae; Lee, Min Woo; Kim, Hyung Soo; Choi, Dal Woong; Kim, Dong Gil; Kim, Suhng Wook
- Issue Date
- 3월-2021
- Publisher
- WILEY
- Keywords
- Ga-68& #8208; NOTA& #8208; SAC; Carbonic anhydrase IX; PET tracer; Saccharin; U87MG
- Citation
- JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, v.64, no.3, pp.129 - 139
- Indexed
- SCIE
SCOPUS
- Journal Title
- JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS
- Volume
- 64
- Number
- 3
- Start Page
- 129
- End Page
- 139
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/49502
- DOI
- 10.1002/jlcr.3893
- ISSN
- 0362-4803
- Abstract
- In this study, we developed a saccharin (SAC)-based radiopharmaceutical (Ga-68-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 Ga-68- 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.Ga-68-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 Ga-68-NOTA-SAC were 88% at 60 min and 220% at 90 min, compared to 30 min p.i. The potential of Ga-68-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.
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