Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Salirasib (Farnesyl Thiosalicylic Acid) 是一种有效的竞争性异戊二烯化蛋白甲基转移酶抑制剂,抑制 Ras 甲基化并具有潜在的抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 249 | 现货 | ||
10 mg | ¥ 391 | 现货 | ||
25 mg | ¥ 772 | 现货 | ||
50 mg | ¥ 1,330 | 现货 | ||
100 mg | ¥ 1,830 | 现货 | ||
200 mg | ¥ 2,720 | 现货 | ||
500 mg | ¥ 4,460 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 386 | 现货 |
产品描述 | Salirasib (Farnesyl Thiosalicylic Acid)(Ki=2.6 μM), an effective competitive prenylated protein methyltransferase (PPMTase) inhibitor, inhibits Ras methylation with potential antineoplastic activity. |
靶点活性 | PPMTase:2.6 μM(Ki) |
体外活性 | Salirasib inhibits the growth of human Ha-ras-transformed Rat1 cells, which correlates well with their inhibition for PPMTase. [1] Salirasib inhibits Ras methylation in Rat-1 fibroblasts, Ras-transformed Rat-1, and B16 melanoma cells. Salirasib also reduces the levels of Ras in cell membranes and inhibits Ras-dependent cell growth, independently of methylation, but via modulation of Ras-Raf communication. [2] In Ras-transformed EJ cells, Salirasib interferes with the activation of Raf-1 and MAPK and inhibits DNA synthesis. [3] |
体内活性 | In Panc-1 xenografted nude mice, Salirasib (5 mg/kg i.p.) markedly inhibits tumor growth without systemic toxicity. [4] In male Wistar rats, Salirasib (5 mg/kg i.p.) markedly inhibits thioacetamide-induced -induced liver cirrhosis. [5] In the dy(2J)/dy(2J) mouse model of congenital muscular dystrophy, Salirasib (5 mg/kg i.p.) attenuates fibrosis and improves muscle strength. [6] |
激酶实验 | PPMTase Assays : Synaptosomal membranes of rat brain cerebellum or total membranes of cultured cell lines (100,000 × g pellet) are used for methyltransferase assays in the cell-free systems. Methyltransferase assays are performed at 37°C in 50 mM Tris-HCl buffer, pH 7.4, using 100 μg of protein, 25 μM [methyl-3H]AdoMet (300,000 cpm/nmol), and 50 μM AFC (prepared as a stock solution in DMSO) in a total volume of 50 μL. DMSO concentration in all assays is 8%. Various AFC concentrations are used in several experiments as indicated in the text. Reactions are terminated after 10 min by addition of 500 μL of chloroform:methanol (1:1) with subsequent addition of 250 μL of Water, mixing, and phase separation. A 125-μL portion of the chloroform phase is dried at 40°C, and 200 μl of 1 N NaOH, 1% SDS solution is added. The methanol thus formed is counted by the vapor phase equilibrium method. Typical background counts (no AFC added) are 50-100 cpm, while typical reactions with AFC yield 500-6,000 cpm. Assays are performed in triplicate, and background counts are subtracted. Methylation of endogenous substrates and gel electrophoresis are performed. Protein carboxyl methylation in intact cells is determined using 100 μCi/mL [methyl-3H]methionine. Cells are assayed in near confluent cultures grown in 10-cm plates with 5 mL of labeling medium. |
细胞实验 | Cells are grown in 24-well plates. 2 h after plating, the cells receive either solvent or FTS freshly prepared from a stock solution to yield the final indicated concentrations in 0.1% DMSO. Media are replaced every 4 days with fresh medium containing the solvent or the drug. Separate experiments indicate that the solvent itself has no effect on cell growth. On the indicated days, the cells are detached from plates by trypsin/EDTA and counted under the light microscope. All assays are performed in quadruplicate. In parallel experiments, cells are stained either with trypan blue or with MTT, and the stained cells are examined under the light microscope. In some MTT-stained cultures, the cells are dissolved in 0.2 mL of 100% DMSO, and the extent of staining is determined spectrophotometrically using an enzyme-linked immunosorbent assay reader.(Only for Reference) |
别名 | 沙利雷塞, 法尼基硫代水杨酸, Farnesyl Thiosalicylic Acid, S-Farnesylthiosalicylic acid, FTS |
分子量 | 358.54 |
分子式 | C22H30O2S |
CAS No. | 162520-00-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 0.1 mg/mL (insoluble)
DMSO: 50 mg/mL (139.45 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.7891 mL | 13.9454 mL | 27.8909 mL | 69.7272 mL |
5 mM | 0.5578 mL | 2.7891 mL | 5.5782 mL | 13.9454 mL | |
10 mM | 0.2789 mL | 1.3945 mL | 2.7891 mL | 6.9727 mL | |
20 mM | 0.1395 mL | 0.6973 mL | 1.3945 mL | 3.4864 mL | |
50 mM | 0.0558 mL | 0.2789 mL | 0.5578 mL | 1.3945 mL | |
100 mM | 0.0279 mL | 0.1395 mL | 0.2789 mL | 0.6973 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。
Salirasib 162520-00-5 Autophagy GPCR/G Protein MAPK Ras 沙利雷塞 inhibit 法尼基硫代水杨酸 Farnesyl Thiosalicylic Acid Inhibitor S-Farnesylthiosalicylic acid FTS inhibitor