Synthesis and preliminary evaluation of F-18-icotinib for EGFR-targeted PET imaging of lung cancer

doi:10.1016/j.bmc.2018.12.034

CORC > 上海应用物理研究所 > 中国科学院上海应用物理研究所 > 中科院上海应用物理研究所2011-2017年

	Synthesis and preliminary evaluation of F-18-icotinib for EGFR-targeted PET imaging of lung cancer
	Lu, XM ; Wang, C ; Li, X ; Gu, PL ; Jia, LN ; Zhang, L
刊名	BIOORGANIC & MEDICINAL CHEMISTRY
	2019
卷号	27 期号:3 页码:545—551
关键词	TYROSINE KINASE INHIBITOR DERIVATIVES BIOMARKERS MUTATIONS DRUG
ISSN号	0968-0896
DOI	10.1016/j.bmc.2018.12.034
文献子类	期刊论文
英文摘要	Epidermal growth factor receptor (EGFR) has emerged as an attracting target in the field of imaging and treatment for non-small cell lung cancer (NSCLC). Radiolabeled EGFR-tyrosine kinase inhibitors (EGFR-TKIs) specifically targeting EGFR are deemed as promising probes for the imaging of NSCLC. This study aimed to label icotinib (one kind of EGFR-TKI) with F-18 through click reaction to develop a new EGFR-targeting PET probe-F-18-icotinib. F-18-icotinib was obtained in 44.81% decay-corrected yield in 100 min synthesis time with 34 GBq/mu mol specific activity and > 99% radiochemical purity at the end of synthesis. The identity of the product was confirmed by co-injection with F-18-icotinib and F-19-icotinib. The Log P was 1.28 +/- 0.04 (n = 6). The tracer displayed excellent stability after incubation for 4 h in vitro. F-18-icotinib showed satisfying binding ability to A549 NSCLC cells, which could be inhibited by icotinib. PET imaging studies demonstrated a specific uptake of the radiotracer (0.90 +/- 0.24% ID/g) in A549 tumor-bearing mice, while lower uptake was observed in heart, lung and spleen at 1.5 h post injection. Inmunohistochemical staining confirmed that the A549 tumor was EGFR-positive. Therefore, we considered that F-18-icotinib was a highly promising compound for EGFR-based tumor PET imaging.
语种	英语
内容类型	期刊论文
源URL	[http://ir.sinap.ac.cn/handle/331007/31846]
专题	上海应用物理研究所_中科院上海应用物理研究所2011-2017年
作者单位	1.Chinese Acad Sci, Shanghai Inst Appl Phys SINAP, Shanghai 201800, Peoples R China; 2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China; 3.Shanghai Jiao Tong Univ, Sch Med, Ren Ji Hosp, Dept Nucl Med, Shanghai 200127, Peoples R China; 4.Shanghai Jiao Tong Univ, Inst Nucl Med, Sch Med, Shanghai 200127, Peoples R China; 5.Changhai Hosp, Dept Nucl Med, Shanghai 200433, Peoples R China
推荐引用方式 GB/T 7714	Lu, XM,Wang, C,Li, X,et al. Synthesis and preliminary evaluation of F-18-icotinib for EGFR-targeted PET imaging of lung cancer[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2019,27(3):545—551.
APA	Lu, XM,Wang, C,Li, X,Gu, PL,Jia, LN,&Zhang, L.(2019).Synthesis and preliminary evaluation of F-18-icotinib for EGFR-targeted PET imaging of lung cancer.BIOORGANIC & MEDICINAL CHEMISTRY,27(3),545—551.
MLA	Lu, XM,et al."Synthesis and preliminary evaluation of F-18-icotinib for EGFR-targeted PET imaging of lung cancer".BIOORGANIC & MEDICINAL CHEMISTRY 27.3(2019):545—551.