Compounds > 2-deoxy-2-((18)F)fluoro-beta-D-glucose

2-deoxy-2-((18)F)fluoro-beta-D-glucose and Disease-Models--Animal

2-deoxy-2-((18)F)fluoro-beta-D-glucose has been researched along with Disease-Models--Animal* in 2 studies

Other Studies

2 other study(ies) available for 2-deoxy-2-((18)F)fluoro-beta-D-glucose and Disease-Models--Animal

Article	Year
Imatinib analogs as potential agents for PET imaging of Bcr-Abl and c-KIT expression at a kinase level. Bioorganic & medicinal chemistry, 2014, Jan-01, Volume: 22, Issue:1 We synthesized two series of imatinib mesylate (STI-571) analogs to develop a Bcr-Abl and c-KIT receptor-specific labeling agent for positron emission tomography (PET) imaging to measure Bcr-Abl and c-KIT expression levels in a mouse model. The methods of molecular modeling, synthesis of STI-571 and its analogs, in vitro kinase assays, and radiolabeling are described. Molecular modeling revealed that these analogs bind the same Bcr-Abl and c-KIT binding sites as those bound by STI-571. The analogs potently inhibit the tyrosine kinase activity of Bcr-Abl and c-KIT, similarly to STI-571. [(18)F]-labeled STI-571 was prepared with high specific activity (75 GBq/μmol) by nucleophilic displacement and an average radiochemical yield of 12%. [(131)I]-labeled STI-571 was prepared with high purity (>95%) and an average radiochemical yield of 23%. The uptake rates of [(18)F]-STI-571 in K562 cells expressing Abl and in U87WT cells overexpressing c-KIT were significantly higher than those in the U87 cell and could be inhibited by STI-71 (confirming the specificity of uptake). PET scans of K562 and U87WT tumor-bearing mice with [(18)F]-STI-571 as a contrast agent showed visible tumor uptake and tumor-to-non-target contrast. Topics: Animals; Antineoplastic Agents; Benzamides; Disease Models, Animal; Fusion Proteins, bcr-abl; Humans; Imatinib Mesylate; Mice; Models, Molecular; Piperazines; Positron-Emission Tomography; Proto-Oncogene Proteins c-kit; Pyrimidines	2014
An efficient and expedient method for the synthesis of 11C-labeled α-aminoisobutyric acid: a tumor imaging agent potentially useful for cancer diagnosis. Bioorganic & medicinal chemistry letters, 2011, Apr-15, Volume: 21, Issue:8 We describe the synthesis of (11)C-labeled α-aminoisobutyric acid 2 from iodo[(11)C]methane and methyl N-(diphenylmethylen)-d,l-alaniate (5). The tetrabutylammonium fluoride (TBAF)-promoted α-[(11)C]methylation of sterically hindered analog 5 was a key step in our synthesis process. Total radiochemical conversion of 2 was high and a remote-controlled synthesis was carried out. A comparative tumor positron emission tomography (PET) imaging study using the same model mouse showed higher uptake of 2 than with (11)C-labeled methionine and [(18)F] fluorodeoxyglucose (FDG). Topics: Aminoisobutyric Acids; Animals; Carbon Radioisotopes; Disease Models, Animal; Mice; Neoplasms; Positron-Emission Tomography; Radiopharmaceuticals	2011

Article

Year

Imatinib analogs as potential agents for PET imaging of Bcr-Abl and c-KIT expression at a kinase level.

Bioorganic & medicinal chemistry, 2014, Jan-01, Volume: 22, Issue:1

We synthesized two series of imatinib mesylate (STI-571) analogs to develop a Bcr-Abl and c-KIT receptor-specific labeling agent for positron emission tomography (PET) imaging to measure Bcr-Abl and c-KIT expression levels in a mouse model. The methods of molecular modeling, synthesis of STI-571 and its analogs, in vitro kinase assays, and radiolabeling are described. Molecular modeling revealed that these analogs bind the same Bcr-Abl and c-KIT binding sites as those bound by STI-571. The analogs potently inhibit the tyrosine kinase activity of Bcr-Abl and c-KIT, similarly to STI-571. [(18)F]-labeled STI-571 was prepared with high specific activity (75 GBq/μmol) by nucleophilic displacement and an average radiochemical yield of 12%. [(131)I]-labeled STI-571 was prepared with high purity (>95%) and an average radiochemical yield of 23%. The uptake rates of [(18)F]-STI-571 in K562 cells expressing Abl and in U87WT cells overexpressing c-KIT were significantly higher than those in the U87 cell and could be inhibited by STI-71 (confirming the specificity of uptake). PET scans of K562 and U87WT tumor-bearing mice with [(18)F]-STI-571 as a contrast agent showed visible tumor uptake and tumor-to-non-target contrast.

Topics: Animals; Antineoplastic Agents; Benzamides; Disease Models, Animal; Fusion Proteins, bcr-abl; Humans; Imatinib Mesylate; Mice; Models, Molecular; Piperazines; Positron-Emission Tomography; Proto-Oncogene Proteins c-kit; Pyrimidines

2014

An efficient and expedient method for the synthesis of 11C-labeled α-aminoisobutyric acid: a tumor imaging agent potentially useful for cancer diagnosis.

Bioorganic & medicinal chemistry letters, 2011, Apr-15, Volume: 21, Issue:8

We describe the synthesis of (11)C-labeled α-aminoisobutyric acid 2 from iodo[(11)C]methane and methyl N-(diphenylmethylen)-d,l-alaniate (5). The tetrabutylammonium fluoride (TBAF)-promoted α-[(11)C]methylation of sterically hindered analog 5 was a key step in our synthesis process. Total radiochemical conversion of 2 was high and a remote-controlled synthesis was carried out. A comparative tumor positron emission tomography (PET) imaging study using the same model mouse showed higher uptake of 2 than with (11)C-labeled methionine and [(18)F] fluorodeoxyglucose (FDG).

Topics: Aminoisobutyric Acids; Animals; Carbon Radioisotopes; Disease Models, Animal; Mice; Neoplasms; Positron-Emission Tomography; Radiopharmaceuticals

2011