2-Nitroimidazole-Tricarbocyanine Conjugate as a Near-Infrared Fluorescent Probe for in Vivo Imaging of Tumor Hypoxia

• DOI: 10.1021/bc2004704
• Publication Date: 2012-02-16T08:36:28Z
• Authors: Kensuke Okuda; Yasuyuki Okabe; Tetsuya Kadonosono; Takahiro Ueno; Bahaa G. M. Youssif; Shinae Kizaka-Kondoh; Hideko Nagasawa
• Keywords: Tumor Hypoxia; Hypoxia; Ex vivo; Nitroimidazole; Fluorescence-lifetime imaging microscopy; Conjugate; Nitroreductase

We developed a novel near-infrared (NIR) fluorescent probe, GPU-167, for in vivo imaging of tumor hypoxia. GPU-167 comprises tricarbocyanine dye as an NIR fluorophore and two 2-nitroimidazole moieties exogenous hypoxia markers that undergo bioreductive activation then selective entrapment hypoxic cells. After treatment with cells contained significantly higher levels fluorescence than normoxia. In specifically detected tumors 24 h after administration. Ex analysis revealed showed strong correlation inducible factor (HIF)-1 active regions. These data suggest is promising optical probe