Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GW843682X (GW843682) 是 PLK1 和 PLK3 的特异性和 ATP 竞争性抑制剂,IC50 分别为 2.2 nM 和 9.1 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 248 | 现货 | ||
2 mg | ¥ 355 | 现货 | ||
5 mg | ¥ 567 | 现货 | ||
10 mg | ¥ 873 | 现货 | ||
25 mg | ¥ 1,750 | 现货 | ||
50 mg | ¥ 2,770 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 688 | 现货 |
产品描述 | GW843682X (GW843682) is a selective and ATP-competitive inhibitor of PLK1 and PLK3 (IC50s = 2.2 nM and 9.1 nM). |
靶点活性 | Aurora A:4800 nM, PLK3:9.1 nM, cdk2/cyclin A:7600 nM, PDGFR1β:160 nM, PLK1:2.2 nM, VEGFR2:360 nM |
体外活性 | GW843682X (500 nM) in combination with 5 µM VP-16 suppresses 50% of entry into mitosis in U937 cells. GW843682X inhibits the proliferation of U937 cells with an EC50 of 120 nM[1]. GW843682X (0.06-1 μM) has inhibitory activities against the proliferation of acute leukemia cells and potentiates the anti-proliferative activity of vincristine. GW843682X (0.1-1 μM) induces apoptosis of leukemia cells in a dose- and time-dependent manner. GW843682X (0.5-1 μM) dephosphorylates Bcl-xl in leukemia cells[2]. GW843682X is effective in inhibition of growth of tumor cells, with IC50s of 0.41, 0.57, 0.11, 0.38, and 0.70 μM for A549, BT474, HeLa, H460 and HCT116 cell lines. GW843682X dose-dependently inhibits PLK1 phosphorylation of Ser15-p53 (IC50 = 0.14 μM). GW843682X (3 μM) causes strong G2-M arrest in HDF cells and H460 cells after treatment for 24, 48, and 72 h. GW843682X (5 μM) leads to apoptosis in H460 cells instead of HDF cells[3]. |
别名 | GW843682 |
分子量 | 477.46 |
分子式 | C22H18F3N3O4S |
CAS No. | 660868-91-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (62.83 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 | 2.0944 mL | 10.4721 mL | 20.9442 mL | 52.3604 mL |
5 mM | 0.4189 mL | 2.0944 mL | 4.1888 mL | 10.4721 mL | |
10 mM | 0.2094 mL | 1.0472 mL | 2.0944 mL | 5.236 mL | |
20 mM | 0.1047 mL | 0.5236 mL | 1.0472 mL | 2.618 mL | |
50 mM | 0.0419 mL | 0.2094 mL | 0.4189 mL | 1.0472 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。
GW843682X 660868-91-7 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic Tyrosine Kinase/Adaptors VEGFR PLK CDK PDGFR Aurora Kinase inhibit GW-843682 GW 843682 Polo-like Kinase (PLK) GW843682 Inhibitor inhibitor