Fosbretabulin disodium

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Fosbretabulin disodium (Combretastatin A-4 phosphate) is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM. Fosbretabulin disodium inhibits the polymerization of tubulin with IC50 of 2.4 μM, and it also disrupts tumor vasculature. Analyses of cell-cycle distribution showed CA-4 obviously induced G(2)-M phase arrest with sub-G(1) formation. The analyses of apoptosis showed that CA-4 induced caspase-3 activation and decreased BubR1 and Bub3 in cancer cells. Fosbretabulin disodium increases endothelial cell permeability, while inhibiting endothelial cell migration and capillary tube formation predominantly through disruption of VE-cadherin/β-catenin/Akt signaling pathway, thereby leading to rapid vascular collapse and tumor necrosis. Combretastatin A-4 phosphate (fosbretabulin disodium) is a microtubule destabilizing drug, a type of vascular-targeting agent, a drug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis.

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