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TCS7010

TCS7010

产品编号 T6767   CAS 1158838-45-9
别名: Aurora A Inhibitor I

TCS7010 (Aurora A Inhibitor I) 是一种选择性的 Aurora A 抑制剂,IC50值为 3.4 nM。

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TCS7010 Chemical Structure
TCS7010, CAS 1158838-45-9
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
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
Doxorubicin hydrochloride限时半价
产品目录号及名称: TCS7010 (T6767)
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纯度: 99.69%
纯度: 98.49%
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参考文献
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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 58.8 mg/mL (100 mM)

溶液配制表

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

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TargetMol Library Books参考文献

1. Aliagas-Martin I, et al. J Med Chem, 2009, 52(10), 3300-3307. 2. Yuan H, et al. Carcinogenesis, 2012, 33(2), 285-293. 3. Kwiatkowski N, et al. ACS Chem Biol, 2012, 7(1), 185-196. 4. Rawson TE, et al. J Med Chem, 2008, 51(15), 4465-4475.

TargetMol Library Books文献引用

1. Chen H, Hu J, Xiong X, et al.AURKA inhibition induces Ewing’s sarcoma apoptosis and ferroptosis through NPM1/YAP1 axis.Cell Death & Disease.2024, 15(1): 99.
AMAROGENTIN AZA1 Chelerythrine Cholesteryl Hemisuccinate Voreloxin hydrochloride 1-beta-D-Arabinofuranosylthymine Calycosin Cabozantinib S-malate

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 抑制剂库 经典已知活性库 表观遗传库 细胞周期化合物库 抗衰老化合物库 已知活性化合物库 NO PAINS 化合物库 细胞凋亡化合物库 激酶抑制剂库

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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。

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技术支持

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。

Keywords

TCS7010 1158838-45-9 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic Aurora Kinase TCS 7010 inhibit Aurora A Inhibitor I Inhibitor TCS-7010 inhibitor

 

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