Novel cancer-targeting SPECT/NIRF dual-modality imaging probe (99m)Tc-PC-1007: synthesis and biological evaluation

Bioorg Med Chem Lett. 2013 Dec 1;23(23):6350-4. doi: 10.1016/j.bmcl.2013.09.074. Epub 2013 Oct 1.

Abstract

Synthesis, characterization, in vitro and in vivo biological evaluation of a heptamethine cyanine based dual-mode single-photon emission computed tomography (SPECT)/near infrared fluorescence (NIRF) imaging probe (99m)Tc-PC-1007 is described. (99m)Tc-PC-1007 exhibited preferential accumulation in human breast cancer MCF-7 cells. Cancer-specific SPECT/CT and NIRF imaging of (99m)Tc-PC-1007 was performed in a breast cancer xenograft model. The probe uptake ratio of tumor to control (spinal cord) was calculated to be 4.02±0.56 at 6 h post injection (pi) and 8.50±1.41 at 20 h pi (P<0.0001). Pharmacokinetic parameters such as blood clearance and organ distribution were assessed.

Keywords: 99m-Technetium; Breast cancer; Dual-modality; Heptamethine cyanine dye; Near infrared fluorescence; SPECT.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Breast Neoplasms / diagnosis*
  • Breast Neoplasms / diagnostic imaging
  • Breast Neoplasms / metabolism
  • Female
  • Heterografts
  • Humans
  • MCF-7 Cells
  • Mice
  • Multimodal Imaging / methods
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / pharmacokinetics
  • Spectroscopy, Near-Infrared
  • Technetium Compounds / chemical synthesis*
  • Technetium Compounds / pharmacokinetics
  • Tomography, Emission-Computed, Single-Photon / methods
  • Xenograft Model Antitumor Assays

Substances

  • Radiopharmaceuticals
  • Technetium Compounds