Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Poloxin 是一种 polo 样激酶 1 的 ATP 非竞争性抑制剂,靶向 polo-box 结构域,IC50值约为 4.8 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 138 | 现货 | ||
5 mg | ¥ 297 | 现货 | ||
10 mg | ¥ 477 | 现货 | ||
25 mg | ¥ 887 | 现货 | ||
50 mg | ¥ 1,490 | 现货 | ||
100 mg | ¥ 2,190 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 397 | 现货 |
产品描述 | Poloxin is a non-ATP competitive Polo-like Kinase 1 inhibitor. It targets the polo-box domain (IC50: appr 4.8 μM). |
靶点活性 | PLK2 (PBD):18.7 μM, PLK1 (PBD):4.8 μM, PLK3 (PBD):53.9 μM |
体外活性 | Poloxin inhibits proliferation in both cell lines with a comparable efficiency through a 72 h period. Poloxin inhibits the polo-box domain (PBD) interaction (apparent IC50: ~4.8 μM). Poloxin (25 μM) causes defects in centrosome integrity, spindle formation, and chromosome alignment in mitosis. Centrosomal fragmentation induced by Poloxin is partially rescued by Kiz T379E. Poloxin (25 μM) activates the mitotic checkpoint, induces apoptosis and inhibits proliferation of MDA-MB-231 cells. Poloxin shows a loose Plk1 PBD specificity with 4-10 times higher IC50 values for Plk2 and Plk3, and does not significantly inhibit other types of phosphopeptide-binding domains such as FHA, WW, and SH2 domains[1][2][3]. |
体内活性 | Poloxin (40 mg/kg) reduces the proliferation of MDA-MB-231 cells. It also suppresses the growth of the tumor nude mice bearing established xenografts of MDA-MB-231[1]. |
分子量 | 297.35 |
分子式 | C18H19NO3 |
CAS No. | 321688-88-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 14 mg/mL (43.72 mM), Sonification is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.363 mL | 16.8152 mL | 33.6304 mL | 84.076 mL |
5 mM | 0.6726 mL | 3.363 mL | 6.7261 mL | 16.8152 mL | |
10 mM | 0.3363 mL | 1.6815 mL | 3.363 mL | 8.4076 mL | |
20 mM | 0.1682 mL | 0.8408 mL | 1.6815 mL | 4.2038 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。
Poloxin 321688-88-4 Cell Cycle/Checkpoint PLK Inhibitor Polo-like Kinase (PLK) inhibit inhibitor