Synthesis and Construction of I-124 Labeled Small Molecular Probe for Noninvasive PET Imaging of CAIX Expression
- 09-04-2025
- Positron Emission Tomography
- Research Article
Published in:
- Authors
- Xianteng Yang
- Chengxue He
- Feng Wang
- Li Wen
- Haifeng Huang
- Jing Wang
- Zhi Yang
- Hua Zhu
- Published in
- Molecular Imaging and Biology | Issue 3/2025
Abstract
Purpose
Carbonic anhydrase IX (CAIX) which is high expression in the most of hypoxic tumor than normal tissue, promoting the growth, invasion, and metastasis of the tumor. Therefore, the study aimed to evaluate the retention and diagnostic ability of [124I]I-XYIMSR- 01 in CAIX-overexpression tumor by using positron emission tomography (PET) imaging.
Procedures
[124/125I]I-XYIMSR- 01 was labeled by 124/125I, and its CAIX-targeting properties in different cell lines were assayed by cell uptaken study. Its diagnose and retention ability in vivo were verified in different CAIX-expression models using PET imaging and biodistribution study. Pathological tissues were obtained for immunohistochemical (IHC) and Hematoxylin–Eosin (HE) staining to explore the relationship between CAIX and hypoxic, and further analyze PET/CT results.
Results
[124I]I-XYIMSR- 01 was obtained with high specific activity, good radiochemical purity, and good stability. The uptake of of [124I]I-XYIMSR- 01 in HT- 29 cells, which have high CAIX expression, was significant higher than that in HCT116 cells with low CAIX expression (12.78 ± 0.47 vs 1.06 ± 0.10, p = 0.000, at 1 h). This indicated that the probe has good targeting capability and specificity for CAIX. In Micro-PET imaging, clear molecular images lasting for 48 h were achieved in HT29 model. Quantitative biodistribution results showed that the tumor and digestive tract background tissues had a good signal-to-noise ratio within 24 h after injection, indicating [124I]I-XYIMSR- 01 could enable delayed imaging in digestive tract tumors (tumor-to-small intestine: 8.79 ± 0.98). Tumors uptakes were also confirmed by IHC pathology.
Conclusion
The study have shown that [124I]I-XYIMSR- 01 is an ideal molecular probe for tumor hypoxia, enabling long-term dynamic monitoring and imaging of hypoxic tumors.
Graphical Abstract
Construction of 124I-labeled a novel CAIX-targeting probe [124I]I-XYIMSR-01 for noninvasive imaging in tumor with high CAI expression.
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- Title
- Synthesis and Construction of I-124 Labeled Small Molecular Probe for Noninvasive PET Imaging of CAIX Expression
- Authors
-
Xianteng Yang
Chengxue He
Feng Wang
Li Wen
Haifeng Huang
Jing Wang
Zhi Yang
Hua Zhu
- Publication date
- 09-04-2025
- Publisher
- Springer International Publishing
- Published in
-
Molecular Imaging and Biology / Issue 3/2025
Print ISSN: 1536-1632
Electronic ISSN: 1860-2002 - DOI
- https://doi.org/10.1007/s11307-025-02004-5
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