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A small-molecule dye for NIR-II imaging.

Alexander L Antaris1,2, Hao Chen1,3, Kai Cheng3

  • 1State 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.

Nature Materials
|November 24, 2015
PubMed
Summary
This summary is machine-generated.

Researchers developed a new, rapidly excreted fluorescent dye (CH1055) for second near-infrared window (NIR-II) imaging. This breakthrough overcomes limitations of current dyes, enabling clearer visualization of biological systems and improved tumor imaging for surgical guidance.

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Area of Science:

  • Biomedical Optics
  • Medical Imaging
  • Organic Chemistry

Background:

  • Second near-infrared window (NIR-II) fluorescent imaging offers deep tissue penetration and high resolution.
  • Existing NIR-II fluorophores exhibit slow excretion and reticuloendothelial system retention, hindering clinical application.
  • Need for novel NIR-II agents with improved pharmacokinetic profiles for safer in vivo imaging.

Purpose of the Study:

  • To develop and characterize a novel, rapidly excreted NIR-II fluorophore for enhanced biological imaging.
  • To evaluate the performance of the new fluorophore in preclinical models, including lymphatic mapping and tumor imaging.
  • To assess the potential of the fluorophore for image-guided surgery.

Main Methods:

  • Synthesis of a novel 970-Da organic molecule (CH1055) as an NIR-II fluorophore.
  • Evaluation of CH1055 excretion profile, with approximately 90% renal excretion within 24 hours.
  • Comparative imaging studies in mice, assessing lymphatic vasculature, sentinel lymph node mapping, brain tumor uptake, and targeted molecular imaging using anti-EGFR Affibody conjugates.

Main Results:

  • CH1055 demonstrated rapid renal excretion, addressing limitations of current NIR-II dyes.
  • The fluorophore outperformed indocyanine green (ICG) in visualizing mouse lymphatic vasculature and mapping sentinel lymph nodes.
  • PEGylated-CH1055 showed significant uptake in brain tumors (approx. 4 mm depth) and enabled targeted molecular imaging, achieving a superior tumor-to-background ratio for image-guided surgery.

Conclusions:

  • CH1055 represents a promising, rapidly excreted NIR-II fluorophore with potential for clinical translation.
  • Its superior performance in preclinical models highlights its utility for deep tissue imaging, lymphatic mapping, and precise tumor visualization.
  • The development of CH1055 paves the way for advanced image-guided diagnostics and therapeutics.