Development and Evaluation of 18F-IRS for Molecular Imaging Mutant EGF Receptors in NSCLC

Abstract To prepare and evaluate a new radiotracer 18F-IRS for molecular imaging mutant EGF Receptors in vitro and vivo. Uptake and efflux of 18F-IRS were performed with four NSCLC cell lines including HCC827, H1975, H358 and H520. In vivo tumor targeting and pharmacokinetics of the radiotracers wer...

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Autores principales: Yan Song, Zunyu Xiao, Kai Wang, Xiance Wang, Chongqing Zhang, Fang Fang, Xilin Sun, Baozhong Shen
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Lenguaje:EN
Publicado: Nature Portfolio 2017
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Acceso en línea:https://doaj.org/article/452db1280f254c18bf3d8e4ea86f72c1
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spelling oai:doaj.org-article:452db1280f254c18bf3d8e4ea86f72c12021-12-02T16:08:09ZDevelopment and Evaluation of 18F-IRS for Molecular Imaging Mutant EGF Receptors in NSCLC10.1038/s41598-017-01443-72045-2322https://doaj.org/article/452db1280f254c18bf3d8e4ea86f72c12017-06-01T00:00:00Zhttps://doi.org/10.1038/s41598-017-01443-7https://doaj.org/toc/2045-2322Abstract To prepare and evaluate a new radiotracer 18F-IRS for molecular imaging mutant EGF Receptors in vitro and vivo. Uptake and efflux of 18F-IRS were performed with four NSCLC cell lines including HCC827, H1975, H358 and H520. In vivo tumor targeting and pharmacokinetics of the radiotracers were also evaluated in HCC827, H1975, H358 and H520 tumor-bearing nude mice by PET/CT imaging. Ex vivo biodistribution assays were performed to quantify the accumulation of 18F-IRS in vivo. We also performed 18F-IRS PET/CT imaging of three patients with NSCLC. We labeled this small molecule with QD620 for flow cytometry and confocal imaging analyses. The uptakes of 18F-IRS by HCC827 and HCC827 tumors were significantly higher than those of H358, H1975 and H520, and they were reduced by the addition of 100 μM of gefitinib. Biodistribution experiments showed an accumulation of 18F-IRS in tumors of HCC827 xenografts. Flow cytometry and confocal imaging with QD620-IRS further demonstrated that binding specifically to HCC827 cells. 18F-IRS accumulation was preferential in the tumor, which was NSCLC with responsive EGFR exon 19 deleted. 18F-IRS showed high binding stability and specificity to 19 exon deleted EGFR mutation in vitro and vivo.Yan SongZunyu XiaoKai WangXiance WangChongqing ZhangFang FangXilin SunBaozhong ShenNature PortfolioarticleMedicineRScienceQENScientific Reports, Vol 7, Iss 1, Pp 1-12 (2017)
institution DOAJ
collection DOAJ
language EN
topic Medicine
R
Science
Q
spellingShingle Medicine
R
Science
Q
Yan Song
Zunyu Xiao
Kai Wang
Xiance Wang
Chongqing Zhang
Fang Fang
Xilin Sun
Baozhong Shen
Development and Evaluation of 18F-IRS for Molecular Imaging Mutant EGF Receptors in NSCLC
description Abstract To prepare and evaluate a new radiotracer 18F-IRS for molecular imaging mutant EGF Receptors in vitro and vivo. Uptake and efflux of 18F-IRS were performed with four NSCLC cell lines including HCC827, H1975, H358 and H520. In vivo tumor targeting and pharmacokinetics of the radiotracers were also evaluated in HCC827, H1975, H358 and H520 tumor-bearing nude mice by PET/CT imaging. Ex vivo biodistribution assays were performed to quantify the accumulation of 18F-IRS in vivo. We also performed 18F-IRS PET/CT imaging of three patients with NSCLC. We labeled this small molecule with QD620 for flow cytometry and confocal imaging analyses. The uptakes of 18F-IRS by HCC827 and HCC827 tumors were significantly higher than those of H358, H1975 and H520, and they were reduced by the addition of 100 μM of gefitinib. Biodistribution experiments showed an accumulation of 18F-IRS in tumors of HCC827 xenografts. Flow cytometry and confocal imaging with QD620-IRS further demonstrated that binding specifically to HCC827 cells. 18F-IRS accumulation was preferential in the tumor, which was NSCLC with responsive EGFR exon 19 deleted. 18F-IRS showed high binding stability and specificity to 19 exon deleted EGFR mutation in vitro and vivo.
format article
author Yan Song
Zunyu Xiao
Kai Wang
Xiance Wang
Chongqing Zhang
Fang Fang
Xilin Sun
Baozhong Shen
author_facet Yan Song
Zunyu Xiao
Kai Wang
Xiance Wang
Chongqing Zhang
Fang Fang
Xilin Sun
Baozhong Shen
author_sort Yan Song
title Development and Evaluation of 18F-IRS for Molecular Imaging Mutant EGF Receptors in NSCLC
title_short Development and Evaluation of 18F-IRS for Molecular Imaging Mutant EGF Receptors in NSCLC
title_full Development and Evaluation of 18F-IRS for Molecular Imaging Mutant EGF Receptors in NSCLC
title_fullStr Development and Evaluation of 18F-IRS for Molecular Imaging Mutant EGF Receptors in NSCLC
title_full_unstemmed Development and Evaluation of 18F-IRS for Molecular Imaging Mutant EGF Receptors in NSCLC
title_sort development and evaluation of 18f-irs for molecular imaging mutant egf receptors in nsclc
publisher Nature Portfolio
publishDate 2017
url https://doaj.org/article/452db1280f254c18bf3d8e4ea86f72c1
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AT zunyuxiao developmentandevaluationof18firsformolecularimagingmutantegfreceptorsinnsclc
AT kaiwang developmentandevaluationof18firsformolecularimagingmutantegfreceptorsinnsclc
AT xiancewang developmentandevaluationof18firsformolecularimagingmutantegfreceptorsinnsclc
AT chongqingzhang developmentandevaluationof18firsformolecularimagingmutantegfreceptorsinnsclc
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