Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TAK-960 是选择性的 polo 样激酶 1 口服有效抑制剂,IC50为 0.8 nM,对 PLK2 和 PLK3 也有抑制作用,IC50分别为 16.9 和 50.2 nM。它抑制多种肿瘤细胞系的增殖,可治疗多种肿瘤异种移植。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 490 | 现货 | ||
2 mg | ¥ 718 | 现货 | ||
5 mg | ¥ 997 | 现货 | ||
10 mg | ¥ 1,490 | 现货 | ||
25 mg | ¥ 2,720 | 现货 | ||
50 mg | ¥ 3,970 | 现货 | ||
100 mg | ¥ 5,790 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,330 | 现货 |
产品描述 | TAK-960 is an orally bioavailable, selective inhibitor of Plks with IC50 values of 0.8, 16.9, and 50.2 nM for Plk1, Plk2, and Plk3, respectively. |
靶点活性 | PLK3:50.2 nM, PLK1:0.8 nM , PLK2:16.9 nM |
体外活性 | CRC cell lines demonstrated a variable anti-proliferative response to TAK-960 with IC50 values ranging from 0.001 to >?0.75 μmol/L. Anti-proliferative effects were sustained after removal of drug. Following TAK-960 treatment a highly variable accumulation of mitotic (indicating cell cycle arrest) and apoptotic markers was observed. TAK-960 treatment induced G2/M arrest and polyploidy. Six out of the eighteen PDX models responded to single agent TAK-960 therapy (TGII20). The addition of TAK-960 to standard of care chemotherapy resulted in largely additive antitumor effects[1]. |
细胞实验 | Fifty-five CRC cell lines and 18 PDX models were exposed to TAK-960 and evaluated for proliferation (IC50) and Tumor Growth Inhibition Index, respectively.?Additionally, 2 KRAS wild type and 2 KRAS mutant PDX models were treated with TAK-960 as single agent or in combination with cetuximab or irinotecan.?TAK-960 mechanism of action was elucidated through immunoblotting and cell cycle analysis[1]. |
分子量 | 561.6 |
分子式 | C27H34F3N7O3 |
CAS No. | 1137868-52-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 35 mg/mL (62.32 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.7806 mL | 8.9031 mL | 17.8063 mL | 44.5157 mL |
5 mM | 0.3561 mL | 1.7806 mL | 3.5613 mL | 8.9031 mL | |
10 mM | 0.1781 mL | 0.8903 mL | 1.7806 mL | 4.4516 mL | |
20 mM | 0.089 mL | 0.4452 mL | 0.8903 mL | 2.2258 mL | |
50 mM | 0.0356 mL | 0.1781 mL | 0.3561 mL | 0.8903 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。
TAK-960 1137868-52-0 Cell Cycle/Checkpoint PLK Polo-like Kinase (PLK) TAK960 cell TAK 960 cancer proliferation Inhibitor mitosis leukemia inhibit phosphorylation lines inhibitor