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Combretastatin A4 inhibits tubulin polymerization at the colchicine-binding site of beta-tubulin. Combretastatin A4 has antitumor activity by inhibiting AKT function in human gastric cells. The inhibited AKT activation causes decreased cell proliferation, cell cycle arrest, and reduced in vitro migration/invasiveness and in vivo metastatic ability.
| Cell Experiment | |
|---|---|
| Cell lines | MDA-MB-231, A549, and Hela cells |
| Preparation method | Growing MDA-MB-231, A549, and HeLa cells in DMEM medium (115 units/mL of penicillin G, 115 μg/mL of streptomycin, and 10% fetal bovine serum). Seeding cells in 96-well plates (5000 cells/well) containing 50 μL of growth medium for 24 h. After medium removal, adding 100 μL of fresh medium containing individual analogue compounds at different concentrations to each well and incubating at 37 ℃ for 72 h. After 24 h of culture, supplementing the cells with 50 μL of analogue compounds dissolved in DMSO (less than 0.25% in each preparation). After 72 h of incubation, adding 20 μL of resazurin for 2 h before recording fluorescence at 560 nm (excitation) and 590 nm (emission) using a Victor microtiter plate fluorimeter. Defining the IC50 as the compound concentration required to inhibit cell proliferation by 50% in comparison with cells treated with the maximum amount of DMSO (0.25%) and considered as 100% viability. |
| Concentrations | ~3.8 nM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | FVB/N or nude NMRI female mice bearing NT2 and MDA-MB-231 tumors |
| Formulation | DMSO |
| Dosages | 100 mg/kg |
| Administration | i.p. |
| Molecular Weight | 316.35 |
| Formula | C18H20O5 |
| CAS Number | 117048-59-6 |
| Solubility (25°C) | 100 mM in ethanol 100 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Microtubule Products |
|---|
| ABT-751
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. |
| 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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