化合物Aurora A Inhibitor I T6767
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
100 mg | 1158838-45-9 | ¥4,290.00 | 询底价 |
10 mg | 1158838-45-9 | ¥993.00 | 询底价 |
5 mg | 1158838-45-9 | ¥619.00 | 询底价 |
1 mg | 1158838-45-9 | ¥266.00 | 询底价 |
1 mL | 1158838-45-9 | ¥786.00 | 询底价 |
50 mg | 1158838-45-9 | ¥2,880.00 | 询底价 |
25 mg | 1158838-45-9 | ¥1,820.00 | 询底价 |
500 mg | 1158838-45-9 | ¥8,870.00 | 询底价 |
2 mg | 1158838-45-9 | ¥378.00 | 询底价 |
Product Introduction
Bioactivity
英文名: TCS7010
描述: TCS7010 (Aurora A Inhibitor I) 是一种选择性的 Aurora A 抑制剂,IC50值为 3.4 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)
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.
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]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 55 mg/mL (93.53 mM)
关键字: Aurora Kinase | TCS 7010 | inhibit | TCS7010 | Apoptosis | Inhibitor | TCS-7010
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相关库: Anti-Aging Compound Library | Cell Cycle Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Epigenetics Compound Library | Highly Selective Inhibitor Library | NO PAINS Compound Library | Bioactive Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途