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Development of a 68 Ga‐labelled PET tracer for carbonic anhydrase IX‐overexpressed tumors using the artificial sweetener saccharin
Author(s) -
Shin Un chul,
Choi Jeong Su,
Beak Yeon Jae,
Lee Min woo,
Kim Hyung Soo,
Choi Dal Woong,
Kim Dong Gil,
Kim Suhng Wook
Publication year - 2021
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3893
Subject(s) - chemistry , saccharin , carbonic anhydrase , flow cytometry , pet imaging , nuclear medicine , radiochemistry , microbiology and biotechnology , enzyme , biochemistry , positron emission tomography , pathology , medicine , biology
In this study, we developed a saccharin (SAC)‐based radiopharmaceutical ( 68 Ga‐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 68 Ga‐ 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. 68 Ga‐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 68 Ga‐NOTA‐SAC were 88% at 60 min and 220% at 90 min, compared to 30 min p.i. The potential of 68 Ga‐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.