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Updated: Jul 10, 2026
A Fluorescence-based Protocol for Preliminary Screening of Protein Synthesis Inhibitors from Natural Sources
Published on: January 27, 2026
Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib
Darren R Veach1, Mohammad Namavari, Nagavarakishore Pillarsetty
1Department of Molecular Pharmacology and Chemistry, Memorial Sloan-Kettering Cancer Center, 1275 York Avenue, New York, NY 10021, USA.
Abstract:
Tyrosine kinases often play pivotal roles in the pathogenesis of cancer and are good candidates for therapeutic intervention and targeted molecular imaging. The precursor synthesis, radiosynthesis, and biological characterization of a fluorine-18 analog of dasatinib, a multitargeted kinase inhibitor, are reported. Compound 5 potently inhibits Abl, Src, and Kit kinases and inhibits K562 and M07e/p210bcr-abl human leukemic cell growth. Using positron emission tomography, we visualized K562 tumor xenografts in mice with [18F]-5.
Insights
Researchers developed a new fluorine-18 labeled dasatinib analog for cancer imaging. This compound effectively targets key kinases and visualizes leukemia tumors in preclinical models using PET imaging.
Area of Science:
- Oncology
- Radiochemistry
- Molecular Imaging
Background:
- Tyrosine kinases are crucial in cancer development.
- Targeted therapies and molecular imaging are vital in oncology.
- Dasatinib is a known multitargeted kinase inhibitor.
Purpose of the Study:
- To synthesize and characterize a novel fluorine-18 analog of dasatinib.
- To evaluate the biological activity and imaging potential of the new compound.
Main Methods:
- Precursor synthesis and radiosynthesis of the fluorine-18 analog.
- In vitro kinase inhibition assays (Abl, Src, Kit).
- Cell growth inhibition assays (K562, M07e/p210bcr-abl).
- Positron Emission Tomography (PET) imaging in tumor xenografts.
Main Results:
- The synthesized compound (Compound 5) potently inhibited Abl, Src, and Kit kinases.
- Compound 5 demonstrated efficacy in inhibiting leukemic cell growth.
- PET imaging successfully visualized K562 tumor xenografts in mice using [18F]-5.
Conclusions:
- The fluorine-18 dasatinib analog is a promising radiotracer for molecular imaging of cancers driven by specific tyrosine kinases.
- This agent shows potential for targeted therapy and imaging applications in leukemia.
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