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);5-(5,6-DIMETHOXYBENZIMIDAZOL-1-YL)-3-[[2-(TRIFLUOROMETHYL)PHENYL]METHOXY]THIOPHENE-2-CARBOXAMIDE;5-(5,6-二甲氧基-1H-苯并[D]咪唑-1-基)-3-((2-(三氟甲基)苄基)氧基)噻吩-2-甲酰胺 |
| 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 |
| 结构式 | ![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 结构式](CAS/GIF/660868-91-7.gif) |
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
| 沸点 | 609.1±65.0 °C(Predicted) |
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| 密度 | 1.45±0.1 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：>10mg/mL |
| 酸度系数(pKa) | 15.03±0.50(Predicted) |
| 形态 | 固体 |
| 颜色 | 米白色 |
|
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 ) |
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 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-11003 | 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 | 660868-91-7 | 5mg | 700元 |
| 2024/08/19 | HY-11003 | 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 | 660868-91-7 | 10mM * 1mLin DMSO | 847元 |