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Synthesis and Biological Evaluation of a Fluorine-18 Derivative of Dasatinib

descriptionPublicationkeyboard_double_arrow_right Article 23 Oct 2007Publisher:American Chemical Society (ACS)Journal:Journal of Medicinal Chemistry, volume 50, pages 5,853-5,857 (issn: 0022-2623, eissn: 1520-4804,

Authors: Darren R. Veach; Peter Smith-Jones; Nagavarakishore Pillarsetty; Steven M. Larson; Tatiana Beresten-Kochetkov; Mohammad Namavari; Mohammad Namavari; +6 Authors

doi: 10.1021/jm070342g

pmid: 17956080

Synthesis and Biological Evaluation of a Fluorine-18 Derivative of Dasatinib

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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.

Related Organizations

Stanford University
United States
Memorial Sloan Kettering Cancer Center
United States

Keywords

Fluorine Radioisotopes, Transplantation, Heterologous, Dasatinib, Fusion Proteins, bcr-abl, Mice, Nude, Protein-Tyrosine Kinases, Mice, Proto-Oncogene Proteins c-kit, Thiazoles, Pyrimidines, src-Family Kinases, Catalytic Domain, Cell Line, Tumor, Positron-Emission Tomography, Animals, Humans, Radiopharmaceuticals, Cell Proliferation

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BindingDB Entry 50021511: Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib.
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