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Combretastatin A-1 is a microtubule polymerization inhibitor that binds to the colchicine-binding site of tubulin. Combretastatin A-1 inhibits the Wnt/β-catenin pathway through tubulin depolymerization mediated AKT deactivation. Combretastatin A-1 (1-50 nM; 6 h) decreases the mitochondrial membrane potential (MMP) of HepG2 cells. Combretastatin A-1 shows dose-dependently ROS accumulation in HepG2 cells.
Combretastatin A-1 (1-4 mg/kg; i.v. every other day for 4 weeks) significantly reduces the tumor volume in HepG2 subcutaneous xenograft model.
| Molecular Weight | 332.35 |
| Formula | C18H20O6 |
| CAS Number | 109971-63-3 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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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. |
| Fosbretabulin disodium
Fosbretabulin disodium (Combretastatin A-4 phosphate) is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM. |
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