Incongruity of imaging using fluorescent 2-DG conjugates compared to 18F-FDG in preclinical cancer models

Mol Imaging Biol. 2012 Oct;14(5):553-60. doi: 10.1007/s11307-012-0545-3.


Purpose: We compared the use of near-infrared conjugates of 2-deoxyglucose (NIR 2-DG) to 2-deoxy-2-[18F]fluoro-d-glucose (18F-FDG) for the purposes of imaging tumors, as well as response to therapy.

Procedures: Uptake of both 18F-FDG and NIR 2-DG within gastrointestinal stromal tumor xenografts were imaged before and after nilotinib treatment. Confocal microscopy was performed to determine NIR 2-DG distribution in tumors.

Results: Treatment with nilotinib resulted in a rapid reduction in 18F-FDG uptake and reduced tumor cell viability which was predictive of long-term antitumor efficacy. In contrast, optical imaging with NIR 2-DG probes was unable to differentiate control from niltonib-treated animals, and microscopic analysis revealed no change in probe distribution as a result of treatment.

Conclusions: These results suggest that conjugation of large bulky fluorophores to 2-DG disrupts the facilitated transport and retention of these probes in cells. Therefore, optical imaging of NIR 2-DG probes cannot substitute for 18F-FDG positron emission tomography imaging as a biomarker of tumor cell viability and metabolism.

Publication types

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

MeSH terms

  • Animals
  • Deoxyglucose*
  • Fluorescence
  • Fluorodeoxyglucose F18*
  • Gastrointestinal Neoplasms / diagnostic imaging*
  • Gastrointestinal Neoplasms / drug therapy
  • Gastrointestinal Neoplasms / pathology
  • Gastrointestinal Stromal Tumors / diagnostic imaging*
  • Gastrointestinal Stromal Tumors / drug therapy
  • Gastrointestinal Stromal Tumors / pathology
  • Humans
  • Imaging, Three-Dimensional / methods*
  • Luminescent Measurements
  • Mice
  • Mice, Nude
  • Microscopy, Confocal
  • Pyrimidines / pharmacology
  • Pyrimidines / therapeutic use
  • Radionuclide Imaging
  • Spectroscopy, Near-Infrared
  • Xenograft Model Antitumor Assays*


  • Pyrimidines
  • Fluorodeoxyglucose F18
  • Deoxyglucose
  • nilotinib