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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 compound designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis.
| Molecular Weight | 440.29 |
| Formula | C18H19Na2O8P |
| CAS Number | 168555-66-6 |
| Solubility (25°C) | Water 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Microtubule Products |
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CCB02 is a selective CPAP-tubulin interaction inhibitor, binding to tubulin and competing for the CPAP binding site of β-tubulin, with an IC50 of 689 nM, and shows potent anti-tumor activity. |
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20-O-Demethyl-AP3 is a minor metabolite of Ansamitocin P-3. |
| Lisavanbulin dihydrochloride
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