GW843682X
作者：齐岳
发布时间：2023-08-23
09:38:09
点击数：
产品名称：GW843682X
产品描述：
| 产品描述 | GW843682X 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 |
存储
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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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
主营产品：COF、MOF单体系列：三蝶烯衍生物、金刚烷衍生物、四苯甲烷衍生物、peg、上转换、石墨烯、光电材料、点击化学、凝集素、载玻片、蛋白质交联剂、脂质体、蛋白、多肽、氨基酸、糖化学等。
