GW843682X
作者：齊岳
發布時間：2023-08-28
09:02:37
點擊數：
產品名稱：GW843682X
產品描述：
| 產品描述 | GW843682X is a selective and ATP-competitive inhibitor of PLK1 and PLK3 (IC50s = 2.2 nM and 9.1 nM). |
| 靶點活性 | Aurora A:4800 nM, PLK3:9.1 nM, cdk2/cyclin A:7600 nM, PDGFR1β:160 nM, PLK1:2.2 nM, VEGFR2:360 nM |
| 體外活性 | 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]. |
| 別名 | GW843682 |
| 分子量 | 477.46 |
| 分子式 | C22H18F3N3O4S |
| CAS No. | 660868-91-7 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 30 mg/mL (62.83 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介紹：
西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
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