| 名稱 | Mitoxantrone |
| 描述 | Mitoxantrone (mitozantrone) is an inhibitor of topoisomerase II (Topo II), an inhibitor of protein kinase C (PKC) (IC50=8.5 μM). Mitoxantrone has antitumor activity for the treatment of acute myeloid leukemia, hepatocellular carcinoma, and breast cancer. |
| 細(xì)胞實驗 | The human breast carcinoma cell lines MDA-MB-231 and MCF-7 are seeded in standard 96-well plates. One day after seeding, the culture medium is changed and replaced by medium containing different concentration of Mitoxantrone (10-5 to 5 μM) with or without DHA (30 μM) during 7 days. Viability of cells are measured as a whole by the tetrazolium salt assay[3]. |
| 激酶實驗 | activity-based protein profiling (ABPP): Mouse brains are Dounce-homogenized in PBS, pH7.5, followed by a low-speed spin (1,400×, 5 min) to remove debris. The supernatant is then subjected to centrifugation (64,000×, 45 min) to provide the cytosolic fraction in the supernatant and the membrane fraction as a pellet. The pellet is washed and resuspended in PBS buffer by sonication. Total protein concentration in each fraction is determined using a protein assay kit. Samples are stored at -80 °C until use. Mouse brain membrane proteomes, are diluted to 1 mg/mL in PBS and pre-incubated with varying concentrations of inhibitors (1 nM to 10 mM) for 30 min at 37 °C before the addition of FP-rhodamine at a final concentration of 2 mM in a 50 mL total reaction volume. After 30 min at 25 °C, the reactions are quenched with 4×SDS-PAGE loading buffer, boiled for 5 min at 90 °C, subjected to SDS-PAGE and visualized in-gel using a flatbed fluorescence s |
| 體外活性 | 方法：人乳腺癌細(xì)胞 MCF7 用 Mitoxantrone (0.07-9.36 μM) 處理 48 h，使用 SRB assay 測定細(xì)胞活力。
結(jié)果：MCF7 細(xì)胞在 Mitoxantrone 1.17 μM 劑量下達(dá)到對應(yīng)于 IC50 的抑制作用。[1]
方法：骨肉瘤細(xì)胞 U2OS 用 Mitoxantrone (0.2-1 μM) 處理 48 h，使用 Western Blot 檢測靶點蛋白表達(dá)水平。
結(jié)果：Mitoxantrone 處理增加了 Caspase-3 和 PARP1 的裂解。Mitoxantrone 處理還增加了骨肉瘤細(xì)胞中 Bax 和 Bim EL 的表達(dá)。然而，Mitoxantrone 處理降低了 Bcl-2 的表達(dá)。[2] |
| 體內(nèi)活性 | 方法：為測試對，將 Mitoxantrone (0.4-3.2 mg/kg) 腹腔注射給注射白血病細(xì)胞 L1210 的 CDF1 小鼠，每天一次。
結(jié)果：以最佳劑量 (1.6 mg/kg/天) 給予 Mitoxantrone 產(chǎn)生了具有統(tǒng)計學(xué)意義的 60 天存活率。[3] |
| 存儲條件 | keep away from direct sunlight,store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 5% DMSO+95% Saline : 2.37 mg/mL (5.33 mM), Solution.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 88 mg/mL (197.98 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 0.15 mg/mL (0.34 mM), Solution.
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| 關(guān)鍵字 | Topoisomerase | Topo II | Protein kinase C | PKC | Orthopoxvirus | NSC-301739 | NSC301739 | NSC 301739 | Mitoxantrone | MCF-7 | lymphocytes | leukaemia | Inhibitor | inhibit | HL60 cells | Endogenous Metabolite | breast cancer | B-CLL cells | Apoptosis | antitumor |
| 相關(guān)產(chǎn)品 | Prulifloxacin | Norfloxacin | Ciprofloxacin | Berberine chloride | Etoposide | Cholesteryl Hemisuccinate | Levofloxacin hydrochloride | Ciprofloxacin monohydrochloride | EIDD-1931 | α-Vitamin E | Flumequine | Enoxacin |
| 相關(guān)庫 | 抑制劑庫 | 抗癌活性化合物庫 | 經(jīng)典已知活性庫 | 已知活性化合物庫 | 臨床失敗化合物庫 | 激酶抑制劑庫 | 抗衰老化合物庫 | FDA 上市藥物庫 | 膜蛋白靶向化合物庫 | 藥物功能重定位化合物庫 | 抗癌臨床化合物庫 | 抗癌藥物庫 |