Development of a high quantum yield dye for tumour imaging

Dan Yang; Huasen Wang; Chengjie Sun; Hui Zhao; Kuan Hu; Weirong Qin; Rui Ma; Feng Yin; Xuan Qin; Qianling Zhang; Yongye Liang; Zigang Li

doi:10.1039/C7SC02698F

Development of a high quantum yield dye for tumour imaging†

Dan Yang,‡^a Huasen Wang,‡^b Chengjie Sun,‡^a Hui Zhao,^a Kuan Hu,

^a Weirong Qin,^a Rui Ma,^b Feng Yin,

^a Xuan Qin,^a Qianling Zhang,^c Yongye Liang*^b and Zigang Li*^a

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* Corresponding authors

^a School of Chemical Biology and Biotechnology, Shenzhen Graduate School of Peking University, Shenzhen, China
E-mail: lizg@pkusz.edu.cn

^b Department of Materials Science and Engineering, South University of Science and Technology of China, Shenzhen 518055, China
E-mail: liangyy@sustc.edu.cn

^c Shenzhen Key Laboratory of Functional Polymer, College of Chemistry and Environmental Engineering, Shenzhen University, Shenzhen, Guangdong 518060, China

Abstract

A fluorescent dye, FEB, with high fluorescence quantum yield for tumour imaging is reported. FEB dyes can be efficiently synthesized in three steps and then easily modified with either PEG or PEG-iRGD to yield FEB-2000 or FEB-2000-iRGD, respectively. Both modified dyes showed negligible toxicity and were thus able to be adopted for in vivo tumour imaging. PEG modification endowed the dye FEB-2000 with both long circulating times and good tumour targeting properties in a MDA-MB-231 xenograft model. Further conjugation with iRGD to generate FEB-2000-iRGD showed minimal targeting enhancement. These results provide a template for the efficient preparation of FEB dyes for use in tumour imaging, thus providing a foundation for future modifications.

Chemical Science

Development of a high quantum yield dye for tumour imaging†

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