| 名稱 | Combretastatin A4 |
| 描述 | Combretastatin A4 (CA4) is a microtubule-targeting agent that binds β-tubulin (Kd: 0.4 μM). |
| 細(xì)胞實(shí)驗(yàn) | MDA-MB-231, A549, and HeLa cells are grown in DMEM medium (115 units/mL of penicillin G, 115 μg/mL of streptomycin, and 10% fetal bovine serum). Cells are seeded in 96-well plates (5000 cells/well) containing 50 μL of growth medium for 24 h. After medium removal, 100 μL of fresh medium containing individual analogue compounds at di?erent concentrations is added to each well and incubated at 37 ℃ for 72 h. After 24 h of culture, the cells are supplemented with 50 μL of analogue compounds dissolved in DMSO (less than 0.25% in each preparation). After 72 h of incubation, 20 μL of resazurin is added for 2 h before recording ?uorescence at 560 nm (excitation) and 590 nm (emission) using a Victor microtiter plate ?uorimeter. The IC50 is de?ned 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.(Only for Reference) |
| 激酶實(shí)驗(yàn) | Competitive binding assay using LC-MS/MS: Colchicine (1.2 μ M) is incubated with tubulin (1.3 mg/mL) in the incubation bu?er (80 mM PIPES, 2.0 mM MgCl2, 0.5 mM EGTA, pH 6.9) at 37℃ for 1 h. Varying concentrations (0.1 ? 125 μ M) of Combretastatin A4 are used to compete with colchicine originally bound to tubulin. After incubation, the ?ltrate is obtained. The ability of the analogue to inhibit the binding of colchicine is expressed as a percentage of control binding in the absence of any competitor. |
| 體外活性 | 在NT2和MDA-MB-231乳腺腫瘤模型中,Combretastatin A4（100 mg/kg,i.p.）誘導(dǎo)脂質(zhì)R1明顯減少,并通過(guò)電子順磁共振血氧定量法測(cè)得pO2下降. Combretastatin A4（100 mg/kg,i.p.）明顯減少雄性NMRI小鼠的Ktrans. |
| 體內(nèi)活性 | Combretastatin A4（1 μM）抑制35%微管蛋白聚合,10 μM幾乎完全可阻斷。Combretastatin A4抑制MDA-MB-231,Hela,A549,HL-60,SF295,HCT-8,MDA-MB435,OVCAR-8,PC3M,NCI-H358M和淋巴細(xì)胞的生長(zhǎng),IC50分別為2.8,0.9,3.8,2.1,6.2,5.3,7.9,0.37,4.7,8和3.2 nM。 |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | Ethanol : 31.6 mg/mL (100 mM)
DMSO : 45 mg/mL (142.25 mM)
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| 關(guān)鍵字 | inhibit | Microtubule/Tubulin | CA 4 | Combretastatin A4 | Combretastatin A-4 | CA-4 | Inhibitor | Combretastatin A 4 |
| 相關(guān)產(chǎn)品 | 4-Isopropoxybenzoic acid | Docetaxel | Mebendazole | Flubendazole | Oxfendazole | Methylene Blue | Thiabendazole | Methylene Blue trihydrate | Griseofulvin | N-Phenylbenzylamine | Paclitaxel | 4'-Demethylepipodophyllotoxin |
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