Powder: -20°C for 3 years | In solvent: -80°C for 1 year
OTS514 hydrochloride 是一种高效的TOPK 抑制剂,IC50为 2.6 nM。它可强效抑制 TOPK 阳性的肿瘤细胞生长,诱导细胞周期停滞和凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 547 | 现货 | ||
2 mg | ¥ 985 | 现货 | ||
5 mg | ¥ 1,730 | 现货 | ||
10 mg | ¥ 3,130 | 现货 | ||
25 mg | ¥ 5,170 | 现货 | ||
50 mg | ¥ 7,320 | 现货 | ||
100 mg | ¥ 9,860 | 现货 | ||
500 mg | ¥ 19,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,730 | 现货 |
产品描述 | OTS514 hydrochloride is a highly effective TOPK(T-LAK cell-originated protein kinase) inhibitor (IC50: 2.6 nM). |
靶点活性 | TOPK:2.6 nM |
体外活性 | OTS514 can inhibit the growth of kidney cancer cell lines (VMRC-RCW, Caki-1, Caki-2, 769-P, and 786-O), in which TOPK was highly expressed (IC50:19.9-44.1 nM)[1]. OTS514 markedly inhibits the growth of TOPK-positive cancer cells. It also shows the significant growth-inhibitory effect on ovarian cancer cell lines (IC50: 3.0-46 nM)[3]. |
体内活性 | In mouse xenograft studies with human lung cancer cells, OTS514 shows certain efficacy but also caused severe hematopoietic toxicity (reduction of red blood cells and white blood cells associated with marked increase in platelets)[2]. Compared with vehicle control (P < 0.001), OTS514 (p.o.) significantly elongated overall survival in the ES-2 abdominal dissemination xenograft model. |
细胞实验 | Cell lines: CD34+ HSCs. Concentrations: 20 or 40 nM. Incubation Time: 48 h. Method: Cells were cultured in RPMI supplemented with 20% fetal bovine serum and 1×StemSpan CC100.Cells were treated with OTS514 (20 or 40 nM) or OTS964 (100 or 200 nM) for 48 hours.Collected cells were washed with PBS and resuspended in 100 ml of PBS followed by staining with CD41a antibody for 20 min at room temperature.Finally,the cells were washed with PBS again and then analyzed for CD41a staining by flow cytometry.Expression of STAT5 was examined by Western blot with an anti-STAT5 antibody. |
动物实验 | Animal: BALB/cSLC-nu/nu mice. Solvent: 5% glucose (i.v.); 0.5% methylcellulose (p.o.). Dosages: 1,2.5,and 5 mg/kg |
别名 | OTS-514 hydrochloride, OTS514 hydrochloride(1338540-63-8(free base)) |
分子量 | 400.92 |
分子式 | C21H20N2O2S.HCl |
CAS No. | 2319647-76-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 27.5 mg/mL (68.59 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.4943 mL | 12.4713 mL | 24.9426 mL | 62.3566 mL |
5 mM | 0.4989 mL | 2.4943 mL | 4.9885 mL | 12.4713 mL | |
10 mM | 0.2494 mL | 1.2471 mL | 2.4943 mL | 6.2357 mL | |
20 mM | 0.1247 mL | 0.6236 mL | 1.2471 mL | 3.1178 mL | |
50 mM | 0.0499 mL | 0.2494 mL | 0.4989 mL | 1.2471 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。
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