Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Romidepsin (FR 901228) 是一种 HDAC 抑制剂,抑制 HDAC1/2/4/6 (IC50=36/47/510/1400 nM)。Romidepsin 具有抗肿瘤活性,可以用于治疗外周 T 细胞淋巴瘤和皮肤 T 细胞淋巴瘤。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 832 | 现货 | ||
2 mg | ¥ 1,330 | 现货 | ||
5 mg | ¥ 2,430 | 现货 | ||
10 mg | ¥ 3,330 | 现货 | ||
25 mg | ¥ 5,440 | 现货 | ||
50 mg | ¥ 7,640 | 现货 | ||
100 mg | ¥ 10,200 | 现货 |
产品描述 | 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. |
靶点活性 | HDAC1:36 nM, HDAC2:47 nM |
体外活性 |
方法:两种恶性 T 细胞系 PEER 和 SUPT1 用 Romidepsin (2.5-40 nM) 处理 48 h,使用 MTT Assay 检测细胞活力。 结果:Romidepsin 抑制 PEER 和 SUPT1细胞活力,IC50 值为 10.8 nM 和 7.9 nM。[1] 方法:CD20+ rituximab 敏感细胞 Raji 细胞和耐药细胞 Raji-2R、Raji-4RH 用 Romidepsin (10 ng/mL) 处理 2 天,使用 Flow Cytometry 检测胞内 caspase 3 激活水平。 结果:Raji 细胞中,Romidepsin 增加了 active caspase 3。在 Raji-2R 和 Raji-4RH 中未检测到 cleaved active caspase 3。[2] |
体内活性 |
方法:为检测体内抗肿瘤活性,将 Romidepsin (4.4 mg/kg) 腹腔注射给携带人 Burkitt 淋巴瘤 Raji 和 Raji-2R 的 NSG 小鼠,每周一次,持续三周。 结果:Romidepsin 显著抑制异种移植小鼠中 Raji 和 Raji-2R 细胞的生长。[2] 方法:为检测体内抗肿瘤活性,将 Romidepsin (0.03 mg/mouse,0.5% methylcellulose) 腹腔注射给 DEN 诱导肝癌的 C56BL/6 小鼠,每周两次,连续三周。 结果:Romidepsin 抑制肿瘤进展,这种效应与肿瘤细胞增殖减少和凋亡增加有关。[3] |
激酶实验 | 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. |
细胞实验 | 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) |
别名 | FR 901228, FK 228, Depsipeptide, 罗米地辛, NSC 630176 |
分子量 | 540.7 |
分子式 | C24H36N4O6S2 |
CAS No. | 128517-07-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (184.9 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8495 mL | 9.2473 mL | 18.4945 mL | 46.2364 mL |
5 mM | 0.3699 mL | 1.8495 mL | 3.6989 mL | 9.2473 mL | |
10 mM | 0.1849 mL | 0.9247 mL | 1.8495 mL | 4.6236 mL | |
20 mM | 0.0925 mL | 0.4624 mL | 0.9247 mL | 2.3118 mL | |
50 mM | 0.037 mL | 0.1849 mL | 0.3699 mL | 0.9247 mL | |
100 mM | 0.0185 mL | 0.0925 mL | 0.1849 mL | 0.4624 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Romidepsin 128517-07-7 Apoptosis Chromatin/Epigenetic DNA Damage/DNA Repair HDAC FR-901228 NSC-630176 FR 901228 Histone deacetylases FK228 FK 228 Depsipeptide NSC630176 Inhibitor inhibit FK-228 罗米地辛 NSC 630176 FR901228 inhibitor