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受注：045-509-1970 |
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化学情報
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C18H20O5 |
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| 分子量 | 316.35 | CAS No. | 117048-59-6 | |
| Solubility (25°C)* | 体外 | DMSO | 63 mg/mL (199.14 mM) | |
| Ethanol | 34 mg/mL warmed with 50ºC water bath (107.47 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | Combretastatin A4 is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM.Phase 3. |
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| in vitro | Combretastatin A4 inhibits the growth of MDA-MB-231, A549, Hela, HL-60, SF295, HCT-8, MDA-MB435, PC3M, OVCAR-8, NCI-H358M, and lymphocyte cells with IC50 of 2.8, 3.8, 0.9, 2.1, 6.2, 5.3, 7.9, 4.7, 0.37, 8, and 3.2 nM, respectively.[1] [2] 1 μM Combretastatin A4 inhibits tubulin polymerization by 35%, and 10 μM nearly completely blocks tubulin polymerization. Combretastatin A4 demonstrates great relative binding capacity, reaching 78% of colchicine binding.[1] |
| in vivo | In NT2 and MDA-MB-231 mammary tumor model, administration of Combretastatin A4 (100 mg/kg, i.p.) induces a significant decrease in lipids R1 and a reduction in tumor pO2 measured by electron paramagnetic resonance (EPR) oximetry.[2] Combretastatin A4 (100 mg/kg, i.p.) significant decreases the Ktrans in male NMRI mice.[3] |
プロトコル(参考用のみ)
| キナーゼアッセイ | Competitive binding assay using LC-MS/MS | |
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| Colchicine (1.2 μ M) is incubated with tubulin (1.3 mg/mL) in the incubation buffer (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 filtrate 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. | ||
| 細胞アッセイ | 細胞株 | MDA-MB-231, A549, and Hela cells |
| 濃度 | ~3.8 nM | |
| 反応時間 | 72 h | |
| 実験の流れ | 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 different 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 fluorescence at 560 nm (excitation) and 590 nm (emission) using a Victor microtiter plate fluorimeter. The IC50 is defined 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. | |
| 動物実験 | 動物モデル | FVB/N or nude NMRI female mice bearing NT2 and MDA-MB-231 tumors |
| 投薬量 | 100 mg/kg | |
| 投与方法 | i.p. | |
参考
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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| Mechanism of ribosome-associated mRNA degradation during tubulin autoregulation [ Mol Cell, 2023, 83(13):2290-2302.e13] | PubMed: 37295431 |
| Targeting MCL-1 triggers DNA damage and an anti-proliferative response independent from apoptosis induction [ Cell Rep, 2023, 42(10):113176] | PubMed: 37773750 |
| Rigosertib induces mitotic arrest and apoptosis in RAS-driven rhabdomyosarcoma and neuroblastoma [ Mol Cancer Ther, 2020, molcanther.0525.2020] | PubMed: 33158997 |
| The Natural Compound Withaferin A Covalently Binds to Cys239 of β-Tubulin to Promote Tubulin Degradation. [ Mol Pharmacol, 2019, 96(6):711-719] | PubMed: 31585985 |
| Evaluation of the antitumor activity of NOV202, a novel microtubule targeting and vascular disrupting agent [Rickardson L, et al. Drug Des Devel Ther, 2017, 11:1335-1351] | PubMed: 28496304 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。