Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TCS7010 (Aurora A Inhibitor I) 是一种选择性的 Aurora A 抑制剂,IC50值为 3.4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 266 | 现货 | ||
2 mg | ¥ 378 | 现货 | ||
5 mg | ¥ 619 | 现货 | ||
10 mg | ¥ 993 | 现货 | ||
25 mg | ¥ 1,820 | 现货 | ||
50 mg | ¥ 2,880 | 现货 | ||
100 mg | ¥ 4,290 | 现货 | ||
500 mg | ¥ 8,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 786 | 现货 |
产品描述 | TCS7010 (Aurora A Inhibitor I) is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B. |
靶点活性 | Aurora A:3.4 nM |
体外活性 | Aurora A Inhibitor I is a 2,4-dianilinopyrimidine that selectively and potently inhibits Aurora A. Aurora A Inhibitor I effectively inhibits the proliferation of HCT116 and HT29 cells, with IC50 of 190 nM and 2.9 μM, respectively. The Aurora A selectivity of Aurora A Inhibitor I against Aurora B depends on a single amino acid (Thr217) of Aurora A. [1] In KCL-22 cells, Aurora A Inhibitor I (1-5 μM) increases G2/M cell fraction, induces histone H3 serine 10 phosphorylation, and suppresses mitotic Aurora A autophosphorylation on Thr288. Aurora A Inhibitor I (0.5-5 μM) also suppresses cell proliferation in KCL-22 cells, as well as BCR-ABL-negative leukemia cell lines KG-1 and HL-60. Aurora A Inhibitor I effectively induces apoptosis in KCL-22 cells at 5 μM. [2] In a recent study, Aurora A Inhibitor I is also found to inhibit cell growth of HCT116, HT29, and HeLa cells, with IC50 of 377.6 nM, 5.6 μM, and 416 nM. [3] |
激酶实验 | Auroras A and B Inhibition Assays: Both Auroras A and B are assayed in ELISA format using a GST fusion (pGEX-4T) of the N-terminus of Histone H3 (aa 1?18) as substrate. Plates are coated with 2 μg/mL substrate in PBS then blocked with 1 mg/mL I-block in PBS. Kinase reactions are run for 40 min with 5 ng/mL (0.16 nM) Aurora A or 45 ng/mL (1.1 nM) Aurora B at 30 μM ATP (~ Km) in kinase buffer. Final DMSO concentration is 4%. Product is detected by incubation with antiphosphohistone H3 (Ser10) 6 g3 mouse monoclonal antibody and sheep-anti-mouse HRP conjugate, followed by washing and addition of TMB substrate. After quenching with 1 M phosphoric acid, plates are read at 450 nM. |
细胞实验 | Cells are seeded in 384-well plates on day 0 in 50 μL of complete medium and incubated overnight in a 5% CO2 atmosphere at 37 °C. On day 1, 10 μL of Aurora A Inhibitor I is added. On day 4, plates are allowed to reach room temperature, and 30 μL Cell Titer-Glo reagent is added to each well to measure total ATP levels. Plates are read after shaking 15 min at room temperature.(Only for Reference) |
别名 | Aurora A Inhibitor I |
分子量 | 588.07 |
分子式 | C31H31ClFN7O2 |
CAS No. | 1158838-45-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 58.8 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 | 1.7005 mL | 8.5024 mL | 17.0048 mL | 42.5119 mL |
5 mM | 0.3401 mL | 1.7005 mL | 3.401 mL | 8.5024 mL | |
10 mM | 0.17 mL | 0.8502 mL | 1.7005 mL | 4.2512 mL | |
20 mM | 0.085 mL | 0.4251 mL | 0.8502 mL | 2.1256 mL | |
50 mM | 0.034 mL | 0.17 mL | 0.3401 mL | 0.8502 mL | |
100 mM | 0.017 mL | 0.085 mL | 0.17 mL | 0.4251 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。
TCS7010 1158838-45-9 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Aurora Kinase TCS 7010 inhibit Aurora A Inhibitor I Inhibitor TCS-7010 inhibitor