中文名 | GW843682X |
英文名 | GW843682X |
别名 | PLK1和PLK3抑制剂(GW843682X) 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 |
英文别名 | GW843682 GW843682X Polo-like Kinase Inhibitor III 5-(5,6-DIMETHOXYBENZIMIDAZOL-1-YL)-3-[[2-(TRIFLUOROMETHYL)PHENYL]METHOXY]THIOPHENE-2-CARBOXAMIDE 5-(5,6-Dimethoxy-1H-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide 3-(2-(Trifluoromethyl)benzyloxy)-5-(5,6-dimethoxy-1H-benzo[d]imidazol-1-yl)thiophene-2-carboxamide 5-(5,6-dimethoxy-1H-benzo[d]imidazol-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-benzimidazol-1-yl)-3-{[2-(trifluoromethyl)-benzyl]oxy}thiophene-2-carboxamide |
CAS | 660868-91-7 |
EINECS | 200-258-5 |
化学式 | C22H18F3N3O4S |
分子量 | 477.46 |
密度 | 1.45±0.1 g/cm3(Predicted) |
沸点 | 609.1±65.0 °C(Predicted) |
溶解度 | DMSO: >10 mg/mL |
酸度系数 | 15.03±0.50(Predicted) |
存储条件 | 2-8°C |
外观 | 固体 |
颜色 | off-white |
MDL号 | MFCD09971143 |
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 - 刺激性物品 |
风险术语 | 36/37/38 - 刺激眼睛、呼吸系统和皮肤。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S36/37 - 穿戴适当的防护服和手套。 |
WGK Germany | 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.094 ml | 10.472 ml | 20.944 ml |
5 mM | 0.419 ml | 2.094 ml | 4.189 ml |
10 mM | 0.209 ml | 1.047 ml | 2.094 ml |
5 mM | 0.042 ml | 0.209 ml | 0.419 ml |
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