Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CCT 137690是一种有口服活性的极光激酶抑制剂,对极光激酶A、B 和C 的IC50值分别为15、25 和19 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 273 | 现货 | ||
2 mg | ¥ 383 | 现货 | ||
5 mg | ¥ 653 | 现货 | ||
10 mg | ¥ 892 | 现货 | ||
25 mg | ¥ 1,720 | 现货 | ||
50 mg | 特惠询价 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 793 | 现货 |
产品描述 | CCT 137690 is a highly specific and oral-available aurora kinase inhibitor, for aurora A(IC50=15 nM ), B(IC50=25 nM) and C(IC50=19 nM). |
靶点活性 | Aurora A:15 nM, Aurora B:25 nM, Aurora C:19 nM |
体外活性 | 在转基因鼠成神经细胞瘤模型中,CCT137690明显抑制肿瘤细胞生长.在SW620结肠癌移植瘤模型中, 口服CCT137690能够抑制细胞生长. |
体内活性 | 对于hERG离子通道(IC50=3.0 μM),CCT137690能够起到抑制作用。在多种人类不同器官肿瘤细胞系中, CCT137690能够有效抑制细胞生长。对于SW620结肠癌细(GI50=0.3 μM),A2780卵巢癌细胞(GI50=0.14 μM)。 |
激酶实验 | Flashplate assay for identification and evaluation of Aurora inhibitors: On this assay 384-well Basic Flashplate? as solid assay platform is used. The plates are coated overnight at 4 °C with dithiothreitol (DTT) at 100 μg/mL in PBS buffer and used after being washed twice with PBS. 5 μL of CCT137690 in 2% DMSO is added to each well followed by 15 μL master mix of kinase buffer (50 mM Tris pH 7.5, 10 mM NaCl, 2.5 mM MgCl2, 1 mM myelin basic protein (MBP), 20 μM ATP, and 0.025 μCi/μL 33P-ATP). Finally, 250 ng per well of Aurora-A enzyme is added. The plate is shaken for approximately 2 min on a flat-bed plate shaker and incubated for 2 hours at room temperature. The reaction is stopped by washing the plate twice on a 16-pin wash with 10 mM sodium pyrophosphate. The plate is then read on a TopCount-NXTTM. For the determination of the inhibitory activity against Aurora-B or Aurora-C, the same conditions are followed in the assay using Aurora-B or Aurora-C enzymes. |
细胞实验 | The effects of CCT137690 on cell proliferation are analyzed with the colorimetric 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cells such as SW620 and A2780 are plated in 96-well plates at 2.5 × 103 per well and are treated with a range of 0 to 50 μM of CCT137690 for 72 hours. The absorbance is measured at 570 nm using the Wallac VICTOR2TM 1420 Multilabel Counter.(Only for Reference) |
别名 | CCT137690 |
分子量 | 551.48 |
分子式 | C26H31BrN8O |
CAS No. | 1095382-05-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 55.2 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8133 mL | 9.0665 mL | 18.133 mL | 45.3326 mL |
5 mM | 0.3627 mL | 1.8133 mL | 3.6266 mL | 9.0665 mL | |
10 mM | 0.1813 mL | 0.9067 mL | 1.8133 mL | 4.5333 mL | |
20 mM | 0.0907 mL | 0.4533 mL | 0.9067 mL | 2.2666 mL | |
50 mM | 0.0363 mL | 0.1813 mL | 0.3627 mL | 0.9067 mL | |
100 mM | 0.0181 mL | 0.0907 mL | 0.1813 mL | 0.4533 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。
CCT 137690 1095382-05-0 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Aurora Kinase CCT-137690 Inhibitor CCT137690 inhibit inhibitor