Detection of apoptosis by PET/CT with the diethyl ester of [¹⁸F]ML-10 and fluorescence imaging with a dansyl analogue

Bioorg Med Chem. 2014 Jan 1;22(1):341-9. doi: 10.1016/j.bmc.2013.11.019. Epub 2013 Nov 20.

Abstract

The diethyl ester of [(18)F]ML-10 is a small molecule apoptotic PET probe for cancer studies. Here we report a novel multi-step synthesis of the diethyl ester of ML-10 in excellent yields via fluorination using Xtal-Fluor-E. In addition, a one-pot radiosynthesis of the diethyl ester of [(18)F]ML-10 from nucleophilic [(18)F]fluoride was completed in 23% radiochemical yield (decay corrected). The radiochemical purity of the product was ≥99%. The diethyl ester of [(18)F]ML-10 was used in vivo to detect apoptosis in the testes of mice. In parallel studies, the dansyl-ML-10 diethyl ester was prepared and used to detect apoptotic cells in an in vitro cell based assay.

Keywords: Apoptosis; Fluorine-18; ML-10; Nucleophilic fluorination; PET/CT; XtalFluor-E.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis
  • Esters
  • Fluorine Radioisotopes*
  • Halogenation
  • Humans
  • Male
  • Mice
  • Positron-Emission Tomography / methods*
  • Radiochemistry
  • Radiopharmaceuticals*
  • Tomography, X-Ray Computed / methods*

Substances

  • Esters
  • Fluorine Radioisotopes
  • Radiopharmaceuticals