3-[2-(三氟甲基)苄氧基]-5-(5,6-二甲氧基-1H-苯并[D]咪唑-1-基)-2-噻吩甲酰胺
- CAS号:660868-91-7
- 英文名:GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide
- 中文名:3-[2-(三氟甲基)苄氧基]-5-(5,6-二甲氧基-1H-苯并[D]咪唑-1-基)-2-噻吩甲酰胺
- CBNumber:CB82090977
- 分子式:C22H18F3N3O4S
- 分子量:477.46
- MOL File:660868-91-7.mol
- 沸点 :609.1±65.0 °C(Predicted)
- 密度 :1.45±0.1 g/cm3(Predicted)
- 储存条件 :2-8°C
- 溶解度 :DMSO: >10mg/mL
- 酸度系数(pKa) :15.03±0.50(Predicted)
- 形态 :solid
- 颜色 :off-white
3-[2-(三氟甲基)苄氧基]-5-(5,6-二甲氧基-1H-苯并[D]咪唑-1-基)-2-噻吩甲酰胺性质、用途与生产工艺
- 生物活性 GW843682X 是一种选择性的,ATP-竞争性的 PLK1 and PLK3 抑制剂,IC50 值分别为 2.2 nM and 9.1 nM,选择性是其他 30 种激酶的 100 多倍。
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靶点
PLK1
2.2 nM (IC 50 )
PLK3
9.1 nM (IC 50 )
PDGFR1β
160 nM (IC 50 )
VEGFR2
360 nM (IC 50 )
Aurora A
4800 nM (IC 50 )
CDK2/cyclin A
7600 nM (IC 50 )
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体外研究
GW843682X (compound 1) is effective on inhibition of growth of tumor cells, with IC 50 s 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 IC 50 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 EC 50 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.
- 更新日期:2024/11/08
- 产品编号:HY-11003
- 产品名称:3-[2-(三氟甲基)苄氧基]-5-(5,6-二甲氧基-1H-苯并[D]咪唑-1-基)-2-噻吩甲酰胺 GW843682X
- CAS编号:660868-91-7
- 包装:5mg
- 价格:700元
- 更新日期:2024/11/08
- 产品编号:HY-11003
- 产品名称:3-[2-(三氟甲基)苄氧基]-5-(5,6-二甲氧基-1H-苯并[D]咪唑-1-基)-2-噻吩甲酰胺 GW843682X
- CAS编号:660868-91-7
- 包装:10mM * 1mLin DMSO
- 价格:847元
- 公司名称:SIGMA
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- 国家:瑞士
- 产品数:6896
- 优势度:91