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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 (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 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 218 | 现货 | |
5 mg | ¥ 496 | 现货 | |
10 mg | ¥ 787 | 现货 | |
25 mg | ¥ 1,490 | 现货 | |
50 mg | ¥ 2,320 | 现货 | |
100 mg | ¥ 3,480 | 现货 | |
500 mg | ¥ 7,560 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 645 | 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 | TCS7010是一种2,4-二苯胺基嘧啶,具有选择性和高效性地抑制Aurora A的活性。该抑制剂能有效抑制HCT116和HT29细胞的增殖,IC50分别为190 nM和2.9 μM。TCS7010对Aurora A而非Aurora B的选择性,依赖于Aurora A的一个氨基酸(Thr217)。[1] 在KCL-22细胞中,TCS7010(1-5 μM)能增加G2/M期细胞比例,诱导组蛋白H3丝氨酸10位点的磷酸化,抑制有丝分裂期Aurora A在Thr288位点的自磷酸化。在0.5-5 μM浓度下,也能抑制KCL-22细胞及BCR-ABL阴性白血病细胞系KG-1和HL-60的细胞增殖。5 μM浓度下,有效诱导KCL-22细胞凋亡。[2] 近期研究发现,TCS7010还能抑制HCT116、HT29和HeLa细胞的生长,IC50分别为377.6 nM、5.6 μM和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 |
Smiles | CCN1CCN(CC1)C(=O)Cc1ccc(Nc2ncc(F)c(Nc3ccc(cc3)C(=O)Nc3ccccc3Cl)n2)cc1 |
密度 | 1.362g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 55 mg/mL (93.53 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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