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GW843682X
CAS No. 660868-91-7
GW843682X ( GW843682 )
产品货号. M21895 CAS No. 660868-91-7
GW843682X 是 PLK1 和 PLK3 的选择性 ATP 竞争性抑制剂，IC50 分别为 2.2 nM 和 9.1 nM，并且对 ～30 种其他激酶的选择性也超过 100 倍。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥539 | 有现货 |
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| 10MG | ￥829 | 有现货 |
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| 25MG | ￥1628 | 有现货 |
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| 50MG | ￥2576 | 有现货 |
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| 100MG | ￥3708 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
| 1 mL x 10 mM in DMSO | ￥565 | 有现货 |
|
生物学信息
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产品名称GW843682X
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注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
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产品简述GW843682X 是 PLK1 和 PLK3 的选择性 ATP 竞争性抑制剂，IC50 分别为 2.2 nM 和 9.1 nM，并且对 ～30 种其他激酶的选择性也超过 100 倍。
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产品描述GW843682X is effective on 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, with an IC50 of 0.14 μM. GW843682X (3 μM) causes a strong G2-M arres 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. GW843682X inhibits proliferation of U937 cells with an EC50 of 120 nM. GW843682X (500 nM) in combination with 5 μM VP-16 suppresses 50% of entry into mitosis in U937 cells. GW843682X (0.06-1?μM) has inhibitory activities against proliferation of acute leukemia cells, and potentiates the anti-proliferative activity of vincristine. Moreover, 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.
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体外实验GW843682X (compound 1) is effective on 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, with an IC50 of 0.14 μM. GW843682X (3 μM) causes a strong G2-M arres 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. GW843682X inhibits proliferation of U937 cells with an EC50 of 120 nM. GW843682X (500 nM) in combination with 5 μM VP-16 suppresses 50% of entry into mitosis in U937 cells. GW843682X (0.06-1?μM) has inhibitory activities against proliferation of acute leukemia cells, and potentiates the anti-proliferative activity of vincristine. Moreover, 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.
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体内实验——
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同义词GW843682
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通路Cell Cycle/DNA Damage
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靶点PLK
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受体PLK1/PDGFR1β/VEGFR2/CDK2/cyclin A
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研究领域——
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适应症——
化学信息
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CAS Number660868-91-7
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分子量477.46
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分子式C??H??F?N?O?S
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纯度>98% (HPLC)
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溶解度DMSO : 33.33 mg/mL (69.81 mM; Need ultrasonic)；H2O : < 0.1 mg/mL (insoluble)
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SMILESO=C(C1=C(OCC2=CC=CC=C2C(F)(F)F)C=C(N3C4=CC(OC)=C(OC)C=C4N=C3)S1)N
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Lansing TJ, et al. In vitro biological activity of a novel small-molecule inhibitor of polo-like kinase 1. Mol Cancer Ther. 2007 Feb;6(2):450-9. Epub 2007 Jan 31.
2. Didier C, et al. Evaluation of Polo-like Kinase 1 inhibition on the G2/M checkpoint in Acute Myelocytic Leukaemia. Eur J Pharmacol. 2008 Sep 4;591(1-3):102-5.
3. Ikezoe T, et al. A novel treatment strategy targeting polo-like kinase 1 in hematological malignancies. Leukemia. 2009 Sep;23(9):1564-76.
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