Comparison of near-infrared fluorescent deoxyglucose probes with different dyes for tumor diagnosis in vivo

Contrast Media Mol Imaging. May-Jun 2012;7(3):289-301. doi: 10.1002/cmmi.496.


Glucose plays a central role in the cellular energy metabolism. Malignant tumors exhibit an elevated rate of glycolysis over normal tissues. In this study, two near-infrared fluorescent dyes, Cypate and ICG-Der-02, with different water solubility, were conjugated to 2-amino-2-deoxy-D-glucose (2DG) to form Cypate-2DG and ICG-Der-02-2DG, respectively, for NIR fluorescent imaging of tumors in nude mice. The clear routes and tumor targeting abilities of the two NIR fluorescent 2DG probes were compared. Results showed that ICG-Der-02-2DG with higher hydrophilicity was cleared faster by kidneys than the more lipophilic Cypate-2DG. Cypate-2DG had slower but stronger tumor targeting ability compared with ICG-Der-02-2DG. To investigate the correlation between the targeting ability of the probe and the glucose transporter (GLUT1) expression levels of cancer cells, the accumulation of Cypate-2DG in tumors was assessed in MCF-7/estradiol, U87MG, MCF-7 and MDA-MB-435 tumor xenografts, which express different levels of GLUT1. The results show that both Cypate-2DG and ICG-Der-02-2DG possess tumor targeting ability on all the tumors examined, with a proportional correlation to GLUT1 expression. The findings demonstrate the broad applicability of these molecular probes for optical imaging of tumors and glucose-related pathologies.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Carbocyanines* / chemical synthesis
  • Carbocyanines* / pharmacokinetics
  • Coloring Agents*
  • Deoxyglucose* / chemistry
  • Female
  • Fluorescent Dyes* / chemistry
  • Glucosamine / analogs & derivatives*
  • Glucosamine / chemical synthesis
  • Glucosamine / pharmacokinetics
  • Glucose Transporter Type 1 / metabolism
  • Humans
  • Mammary Neoplasms, Experimental / diagnosis*
  • Mammary Neoplasms, Experimental / metabolism
  • Mice
  • Mice, Nude
  • Spectroscopy, Near-Infrared*
  • Tissue Distribution
  • Transplantation, Heterologous
  • Tumor Cells, Cultured


  • Carbocyanines
  • Coloring Agents
  • Fluorescent Dyes
  • Glucose Transporter Type 1
  • ICG-Der-02-2DG
  • cypate-2DG
  • Deoxyglucose
  • Glucosamine