4.6 Article

Molecular engineering of a commercially available NIR-II fluorescent cyanine dye for improved tumor targeting and imaging

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NEW JOURNAL OF CHEMISTRY
卷 47, 期 43, 页码 20088-20094

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ROYAL SOC CHEMISTRY
DOI: 10.1039/d3nj03868h

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The study reports an RGD-conjugated cyanine dye, IR806-RGD, for NIR-II fluorescence imaging of tumors. Compared to the commonly used cyanine dye IR806, IR806-RGD shows improved tumor targeting capability and higher fluorescence intensity.
Second near-infrared window (NIR-II) fluorescence imaging has shown great promise in cancer imaging. Among the numerous NIR-II fluorescence probes, cyanine dyes have shown potential in clinical translation and attracted more and more attention. However, most commercially available NIR-II fluorescent cyanine dyes are not suitable for cancer imaging due to their low tumor targeting capability. Herein, we report an arginylglycylaspartic acid (RGD)-conjugated cyanine dye (IR806-RGD) for NIR-II fluorescence imaging of tumors. IR806-RGD is synthesized via conjugation of RGD onto the commercially available cyanine dye IR806 with three steps. Compared with IR806, IR806-RGD has a longer emission wavelength, higher NIR-II fluorescence intensity and better tumor targeting capability. In vivo tumor imaging study demonstrates that IR806-RGD can be applied for both NIR-II fluorescence and photoacoustic (PA) imaging and has a better imaging efficacy than IR806. Our work provides an approach for modification of cyanine dyes to simultaneously improve their NIR-II fluorescence signal and tumor targeting capability.

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