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An ointment containing an inhibitor for both Src tyrosine kinase and tubulin polymerization, with potential antineoplastic activity. Unlike other Src kinase inhibitors which bind to the ATP-binding site, Src kinase inhibitor KX2-391 binds to the peptide substrate binding site of Src kinase, upon topical application. This inhibits both downstream signaling and the proliferation of tumor cells overexpressing Src. Src tyrosine kinase, a non-receptor tyrosine kinase upregulated in many tumor cell types, plays an important role in tumor cell proliferation, motility, invasiveness and survival. KX2-391 also binds to tubulin heterodimers and inhibits microtubule polymerization, which disrupts microtubule formation and mitosis, leading to further inhibition of cell proliferation. In addition, KX2-391 inhibits T-cell migration. Check for active clinical trials using this agent. (NCI Thesaurus)
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