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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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ABT-751 is an orally bioavailable tubulin inhibitor with IC50 of about 1.5 and 3.4 µM in neuroblastoma and non-neuroblastoma cell lines, respectively. |
| Vincristine sulfate
Vincristine, formally known as leurocristine, is a mitotic inhibitor used in cancer chemotherapy. |
| Docetaxel
Docetaxel (Taxotere), a semi-synthetic analog of paclitaxel (Taxol), is a promoter of microtubule polymerization leading to cell cycle arrest at G2/M, apoptosis and cytotoxicity. |
| Paclitaxel
Paclitaxel is a diterpenoid derived from the bark of the plant Picea abies, and is also a microtubule polymer stabilizer, which promotes polymerization of microtubule proteins to inhibit depolymerization, maintains the stability of microtubule proteins, and inhibits cellular mitosis, and acts on human endothelial cells with an IC50 of 0.1 pM. |
| Noscapine hydrochloride
Noscapine, a phthalideisoquinoline alkaloid constituting 1–10% of the alkaloid content of opium, has been used as a cough suppressant. |
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