Synonyms: KX-02 | KX2 361 | KX2361
Compound class:
Synthetic organic
Comment: KX2-361 is a small molecule with a dual mode of action. It is a Src kinase inhibitor and an inhibitor of tubulin polymerization [1]. It is being investigated for antiproliferative potential. It is closely related to tirbanibulin, and like KX2-391 is a peptide substrate site binder rather than a competitive ATP binding site inhibitor. KX2-361 is orally bioavailable and shows a significant level of brain tissue exposure following oral administration.
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Bioactivity Comments |
KX2-361 has nM level potency against a range of CNS tumour cell lines, and induces 30% long-term complete tumour remission in animal models of glioblastoma [1]. α and β tubulin binding was shown using a photoaffinity analogue of KX2-391 [1]. KX2-361 disrupts tubulin filament formation in GL261 mouse glioma cells at 250 nM. |
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