Abstract
Two carbonic anhydrase IX (CA IX) inhibitors were radiolabeled with (18)F, and evaluated for imaging CA IX expression. Despite good affinity for CA IX and excellent plasma stability, uptake of both tracers in CA IX-expressing HT-29 tumor xenografts in mice was low. (18)F-FEC accumulated predominately in the liver and nasal cavity, whereas a significant amount of (18)F-U-104 was retained in blood. Due to minimal uptake in HT-29 tumors compared to other organs/tissues, these two tracers are not suitable for use for CA IX-targeted imaging.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adenocarcinoma / diagnostic imaging
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Animals
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Antigens, Neoplasm / metabolism*
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Carbonic Anhydrase IX
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Carbonic Anhydrase Inhibitors / chemical synthesis*
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Carbonic Anhydrase Inhibitors / chemistry
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Carbonic Anhydrase Inhibitors / pharmacokinetics
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Carbonic Anhydrase Inhibitors / pharmacology
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Carbonic Anhydrases / metabolism*
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Drug Stability
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Fluorine Radioisotopes
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HT29 Cells
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Humans
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Mice
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Mice, Inbred NOD
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Mice, Knockout
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Mice, SCID
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Molecular Structure
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Positron-Emission Tomography / methods*
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Radiopharmaceuticals
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Receptors, Interleukin-2 / genetics
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Tissue Distribution
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Xenograft Model Antitumor Assays
Substances
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Antigens, Neoplasm
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Carbonic Anhydrase Inhibitors
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Fluorine Radioisotopes
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Radiopharmaceuticals
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Receptors, Interleukin-2
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CA9 protein, human
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Carbonic Anhydrase IX
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Carbonic Anhydrases