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Tubulin polymerization-IN-9 is a potent inhibitor of tubulin (IC50: 1.82 μM). Tubulin polymerization-IN-9 arrests the cell cycle of K562 cells in G2/M phase and induces apoptosis and mitochondrial depolarization. Tubulin polymerization-IN-9 exhibits potent anti-vascular and anti-tumour effects.