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- CAS号:
1095382-05-0
- 规格:
1mg/1mLx10mM(inDMSO)/2mg/5mg/10mg/25mg
| 规格: | 1mg | 产品价格: | ¥234.0 |
|---|---|---|---|
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥634.0 |
| 规格: | 2mg | 产品价格: | ¥322.0 |
| 规格: | 5mg | 产品价格: | ¥522.0 |
| 规格: | 10mg | 产品价格: | ¥713.0 |
| 规格: | 25mg | 产品价格: | ¥1376.0 |
Product Introduction
Bioactivity
| 名称 | CCT 137690 |
| 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). |
| 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) |
| 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. |
| 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)。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (1.81 mM), Sonication is recommended. DMSO : 55.2 mg/mL (100.09 mM), Sonication is recommended. |
| 关键字 | Inhibitor | inhibit | CCT-137690 | CCT 137690 | AuroraKinase | Aurora Kinase | Aurora C | Aurora B | Aurora A | Apoptosis |
| 相关产品 | Formamide | Urea | Sodium Molybdate | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Sildenafil citrate | Citric Acid Triammonium | Stavudine | Tamoxifen |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library | Kinase Inhibitor Library | Apoptosis Compound Library | Highly Selective Inhibitor Library | Anti-Aging Compound Library | NO PAINS Compound Library | Epigenetics Compound Library | Membrane Protein-targeted Compound Library |
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文献和实验网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广,其数量几乎占已知有机化合物的三分之一,用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等,都含有杂环化合物的结构。生物碱多是中草药的有效成分,绝大多数是含氮的杂环化合物。本章内容与医学关系密切,具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式(Ⅰ)和(Ⅱ)两种结构的高能化合物。其作用为贮藏能量(例如 ATP、肌酸磷酸)和作为产生 ATP源的中间代谢产物(例如磷酸烯醇丙酮酸)以及合成反应的中间物质(例如酰基辅酶 A),在蛋白质的结构( conformation)变化周期的第一阶段上(例如钠钾 ATP酶的羧基磷酸中间体)也具有重要作用。多数高等化合物具有磷酸基,但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质,不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开,而必须用化学方法才能分离。
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