Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib.

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Veach DR, Namavari M, Pillarsetty N, Santos EB, Beresten-Kochetkov T, Lambek C, Punzalan BJ, Antczak C, Smith-Jones PM, Djaballah H, Clarkson B, Larson SM

Synthesis and biological evaluation of a fluorine-18 derivative of dasatinib.

J Med Chem. 2007 Nov 15;50(23):5853-7. Epub 2007 Oct 23.

PubMed ID

17956080 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Dasatinib	Proto-oncogene tyrosine-protein kinase Src	IC 50 (nM)	1.5	N/A	N/A	Details
Dasatinib	Tyrosine-protein kinase ABL1	IC 50 (nM)	4.2	N/A	N/A	Details