Source:http://linkedlifedata.com/resource/pubmed/id/19968287
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
2010-1-8
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pubmed:abstractText |
We report the radiosynthesis and evaluation of 3-[3,5-dimethyl-4-(4-[11C]methylpiperazinecarbonyl)-1H-pyrrol-2-ylmethylene]-2-oxo-2,3-dihydro-1H-indole-5-sulfonic acid (3-chlorophenyl)methylamide, termed [11C]SU11274 ([11C]14) for in vivo imaging of mesenchymal-epithelial transition (MET) receptor by positron emission tomography (PET). Following the synthesis of the precursor (13) that was achieved in 10 steps with a total yield of 9.7%, [11C]14 was obtained through radiomethylation in a range of 5-10% radiochemical yield and over 95% radiochemical purity. For in vivo PET studies, two human lung cancer xenograft models were established using MET-positive NCI-H1975 and MET-negative NCI-H520 cell lines. Quantitative [11C]14-PET studies showed that the tumor uptake of [11C]14 in the NCI-H1975 xenografts was significantly higher than that in the NCI-H520 xenografts, which is consistent with their corresponding immunohistochemical tissue staining patterns of MET receptors from the same animals. These studies demonstrated that [11C]14-PET is an appropriate imaging marker for quantification of MET receptor in vivo, which can facilitate efficacy evaluation in the clinical development of MET-targeted cancer therapeutics.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/((3Z)-N-(3-chlorophenyl)-3-((3,5-dim...,
http://linkedlifedata.com/resource/pubmed/chemical/Antineoplastic Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Indoles,
http://linkedlifedata.com/resource/pubmed/chemical/Piperazines,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor, Epidermal Growth Factor,
http://linkedlifedata.com/resource/pubmed/chemical/Receptor Protein-Tyrosine Kinases,
http://linkedlifedata.com/resource/pubmed/chemical/Sulfonamides
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
1520-4804
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
14
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pubmed:volume |
53
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
139-46
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pubmed:meshHeading |
pubmed-meshheading:19968287-Animals,
pubmed-meshheading:19968287-Antineoplastic Agents,
pubmed-meshheading:19968287-Cell Line, Tumor,
pubmed-meshheading:19968287-Drug Evaluation,
pubmed-meshheading:19968287-Humans,
pubmed-meshheading:19968287-Indoles,
pubmed-meshheading:19968287-Lung Neoplasms,
pubmed-meshheading:19968287-Mice,
pubmed-meshheading:19968287-Mice, Nude,
pubmed-meshheading:19968287-Molecular Imaging,
pubmed-meshheading:19968287-Piperazines,
pubmed-meshheading:19968287-Positron-Emission Tomography,
pubmed-meshheading:19968287-Receptor, Epidermal Growth Factor,
pubmed-meshheading:19968287-Receptor Protein-Tyrosine Kinases,
pubmed-meshheading:19968287-Sulfonamides,
pubmed-meshheading:19968287-Xenograft Model Antitumor Assays
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pubmed:year |
2010
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pubmed:articleTitle |
In vivo positron emission tomography (PET) imaging of mesenchymal-epithelial transition (MET) receptor.
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pubmed:affiliation |
Division of Radiopharmaceutical Science, Case Center for Imaging Research, Department of Radiology, Case Western Reserve University, Cleveland, Ohio 44106, USA.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't,
Research Support, N.I.H., Extramural
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