Bafetinib is a substituted benzamide derivative and tyrosine kinase inhibitor structurally related to STI-571 (Imatinib Mesylate). It is a potent Bcr-Abl kinase inhibitor. Also shown to be a potent and selective inhibitor of Lyn tyrosine kinase, an agent of imatinib-resistant leukemia. Bafetinib significantly sensitised ABCB1 and ABCG2 overexpressing MDR cells to their anticancer substrates and increased the intracellular accumulation of anticancer drugs. Eosinophils play a key role in allergic inflammation, bafetinib inhibits oxidative burst and generation of inflammatory mediators and reverses eosinophil survival.

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