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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。
别名 GW843682
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 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 248 | 现货 | |
| 5 mg | ¥ 567 | 现货 | |
| 10 mg | ¥ 873 | 现货 | |
| 25 mg | ¥ 1,750 | 现货 | |
| 50 mg | ¥ 2,770 | 现货 | |
| 100 mg | ¥ 4,120 | 现货 | |
| 1 mL x 10 mM (in DMSO) | ¥ 595 | 现货 |
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| 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 | PLK3:9.1 nM, Aurora A:4800 nM, PDGFR1β:160 nM, CDK2-CyclinA:7600 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 |
| Smiles | COc1cc2ncn(-c3cc(OCc4ccccc4C(F)(F)F)c(s3)C(N)=O)c2cc1OC |
| 密度 | 1.45 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 实际储存温度请以COA为准 | ||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 30 mg/mL (62.83 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+90% Corn Oil: 2 mg/mL (4.19 mM), Sonication is recommended. 请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。 | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
该溶液配制表仅适用于固体产品。对于液体产品,请根据标明的浓度或密度计算稀释方案。 | |||||||||||||||||||||||||||||||
对于不同动物的给药剂量换算,您也可以参考 更多