中文名称:

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

中文同义词:

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;PLK1和PLK3抑制剂(GW843682X)

英文名称:

GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide

英文同义词:

GW843682, 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide;GW843682X;3-(2-(Trifluoromethyl)benzyloxy)-5-(5,6-dimethoxy-1H-benzo[d]imidazol-1-yl)thiophene-2-carboxamide;Polo-like Kinase Inhibitor III;5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide;5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-[[2-(trifluoromethyl)phenyl]methoxy]-2-thiophenecarboxamide;GW843682;5-(5,6-dimethoxy-1H-benzo[d]imidazol-1-yl)-3-((2-(trifluoromethyl)benzyl)oxy)thiophene-2-carboxamide

CAS号:

660868-91-7

分子式:

C22H18F3N3O4S

分子量:

477.46

EINECS号:

200-258-5

相关类别:

细胞周期;细胞生物学试剂

Mol文件:

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

形态

solid

酸度系数(pKa)

15.03±0.50(Predicted)

颜色

off-white

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。

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 )

PLK1 2.2 nM (IC 50 )

PLK3 9.1 nM (IC 50 )

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.

危险品标志 

Xi

危险类别码 

36/37/38

安全说明 

26-36/37

WGK Germany 

3