A small-molecule dye for NIR-II imaging

  • Nat Mater. 2016 Feb;15(2):235-42. doi: 10.1038/nmat4476.
Alexander L Antaris  1  2 ,  Hao Chen  1  3 ,  Kai Cheng  3 ,  Yao Sun  1 ,  Guosong Hong  2 ,  Chunrong Qu  1 ,  Shuo Diao  2 ,  Zixin Deng  1 ,  Xianming Hu  1 ,  Bo Zhang  2 ,  Xiaodong Zhang  2 ,  Omar K Yaghi  2 ,  Zita R Alamparambil  2 ,  Xuechuan Hong  1 ,  Zhen Cheng  3 ,  Hongjie Dai  2
Affiliations
  • 1. State Key Laboratory of Virology, Key Laboratory of Combinatorial Biosynthesis and Drug Discovery (Wuhan University), Ministry of Education, Wuhan University School of Pharmaceutical Sciences, Wuhan 430071, China.
  • 2. Department of Chemistry, Stanford University, California 94305, USA.
  • 3. Molecular Imaging Program at Stanford (MIPS), Bio-X Program, and Department of Radiology, Canary Center at Stanford for Cancer Early Detection, Stanford University, California 94305-5344, USA.
PMID: 26595119 DOI: 10.1038/nmat4476
Abstract

Fluorescent imaging of biological systems in the second near-infrared window (NIR-II) can probe tissue at centimetre depths and achieve micrometre-scale resolution at depths of millimetres. Unfortunately, all current NIR-II fluorophores are excreted slowly and are largely retained within the reticuloendothelial system, making clinical translation nearly impossible. Here, we report a rapidly excreted NIR-II fluorophore (∼90% excreted through the kidneys within 24 h) based on a synthetic 970-Da organic molecule (CH1055). The fluorophore outperformed indocyanine green (ICG)-a clinically approved NIR-I dye-in resolving mouse lymphatic vasculature and sentinel lymphatic mapping near a tumour. High levels of uptake of PEGylated-CH1055 dye were observed in brain tumours in mice, suggesting that the dye was detected at a depth of ∼4 mm. The CH1055 dye also allowed targeted molecular imaging of tumours in vivo when conjugated with anti-EGFR Affibody. Moreover, a superior tumour-to-background signal ratio allowed precise image-guided tumour-removal surgery.

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