中文名稱:羅米地辛 | 英文名稱:Romidepsin |
CAS:128517-07-7 | 品牌: TargetMol |
產(chǎn)地: 美國(guó) | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 99.67% | 產(chǎn)品類別: 抑制劑 |
貨號(hào): T6006 |
名稱 | Romidepsin |
描述 | Romidepsin (FR 901228) is an HDAC inhibitor that inhibits HDAC1/2/4/6 (IC50=36/47/510/1400 nM). Romidepsin has antitumor activity and can be used for the treatment of peripheral T-cell lymphoma and cutaneous T-cell lymphoma. |
細(xì)胞實(shí)驗(yàn) | Cells are exposed to various concentrations of Romidepsin for 72 hours in 96-well plates. 20 μL of 5 mg/mL MTT solution in PBS is added to each well for 4 hours. After removal of the medium, 170 μL of DMSO is added to each well to dissolve the formazan crystals. The absorbance at 540 nm is determined. In addition, cells are incubated with trypan blue, and the numbers of blue (dead) cells and transparent (live) cells are counted in a hemocytometer. For cell cycle analysis, cells are incubated for 30 minutes in propidium iodide staining solution containing 0.05 mg/mL propidium iodide, 1 mM EDTA, 0.1% Triton X-100, and 1 mg/mL RNase A in PBS. The suspension is then passed through a nylon mesh filter and analyzed on a Becton Dickinson FACScan. (Only for Reference) |
激酶實(shí)驗(yàn) | HDAC-inhibitory activity: For the enzyme assay, 10 μL of [3H]acetyl-labeled histones (25,000 cpm/10 μg) are added to 90 μL of the HDAC enzyme fraction extracted from 293T cells overexpressing HDAC1 or HDAC2 in the presence of increasing concentrations of Romidepsin, and the mixture is incubated at 37 °C for 15 minutes. The enzyme reaction is linear for at least 1 hour. The reaction is stopped by the addition of 10 μL of concentrated HCl. The released [3H]acetic acid is extracted with 1 mL of ethylacetate, and 0.9 mL of the solvent layer is taken into 5 mL of aqueous counting scintillant II solution for determination of radioactivity. The IC50 values are determined from at least three independent dose-response curves. |
體外活性 | 方法:兩種惡性 T 細(xì)胞系 PEER 和 SUPT1 用 Romidepsin (2.5-40 nM) 處理 48 h,使用 MTT Assay 檢測(cè)細(xì)胞活力。 結(jié)果:Romidepsin 抑制 PEER 和 SUPT1細(xì)胞活力,IC50 值為 10.8 nM 和 7.9 nM。[1] 方法:CD20+ rituximab 敏感細(xì)胞 Raji 細(xì)胞和耐藥細(xì)胞 Raji-2R、Raji-4RH 用 Romidepsin (10 ng/mL) 處理 2 天,使用 Flow Cytometry 檢測(cè)胞內(nèi) caspase 3 激活水平。 結(jié)果:Raji 細(xì)胞中,Romidepsin 增加了 active caspase 3。在 Raji-2R 和 Raji-4RH 中未檢測(cè)到 cleaved active caspase 3。[2] |
體內(nèi)活性 | 方法:為檢測(cè)體內(nèi)抗腫瘤活性,將 Romidepsin (4.4 mg/kg) 腹腔注射給攜帶人 Burkitt 淋巴瘤 Raji 和 Raji-2R 的 NSG 小鼠,每周一次,持續(xù)三周。 結(jié)果:Romidepsin 顯著抑制異種移植小鼠中 Raji 和 Raji-2R 細(xì)胞的生長(zhǎng)。[2] 方法:為檢測(cè)體內(nèi)抗腫瘤活性,將 Romidepsin (0.03 mg/mouse,0.5% methylcellulose) 腹腔注射給 DEN 誘導(dǎo)肝癌的 C56BL/6 小鼠,每周兩次,連續(xù)三周。 結(jié)果:Romidepsin 抑制腫瘤進(jìn)展,這種效應(yīng)與腫瘤細(xì)胞增殖減少和凋亡增加有關(guān)。[3] |
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 | H2O : Insoluble DMSO : 100 mg/mL (184.9 mM) |
關(guān)鍵字 | FR-901228 | HDAC | NSC-630176 | Histone deacetylases | FK228 | Apoptosis | NSC630176 | Inhibitor | inhibit | FK-228 | FR901228 | Romidepsin |
相關(guān)產(chǎn)品 | Valproic Acid | L-Glutamic acid | Metronidazole | 5-Fluorouracil | Curcumin | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate |
成立日期 | 2013-04-18 (12年) | 注冊(cè)資本 | 566.2651萬(wàn)人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營(yíng)行業(yè) | 化學(xué)試劑,生物活性小分子 | 經(jīng)營(yíng)模式 | 貿(mào)易,試劑,定制,服務(wù) |
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