英文同义词:
SSE15206;SSE-15206;SSE 15206;SSE15206; SSE-15206; SSE 15206;1370046-40-4;1H-Pyrazole-1-carbothioamide, 4,5-dihydro-3-phenyl-5-(3,4,5-trimethoxyphenyl)-;4,5-Dihydro-3-phenyl-5-(3,4,5-trimethoxyphenyl)-1H-pyrazole-1-carbothioamide;3-Phenyl-5-(3,4,5-trimethoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
沸点
518.7±60.0 °C(Predicted)
密度
1.27±0.1 g/cm3(Predicted)
酸度系数(pKa)
14.12±0.60(Predicted)
生物活性
SSE15206 是一种微管 (microtubule) 聚合抑制剂,其在 HCT116 细胞中的 GI50 值为 197 nM,能克服多重耐药性。引起细胞中纺锤体形成不完全,从而导致 G2/M 阻滞,有丝分裂异常。
靶点
GI50: 197 nM (microtubule).
体外研究
SSE15206 induces apoptosis in cells irrespective of MDR-1 overexpression cell lines (KB-V1, A2780-Pac-Res), highly resistant to paclitaxel cells (HCT116-Pac-Res) and parental cells at the concentration of 5 × and 10 × GI 50 values. To conclude, SSE15206 is able to overcome resistance to chemotherapeutic drugs such as paclitaxel in different cancer cell lines.
Western Blot Analysis
Cell Line: Drug-resistant cell lines (KB-V1, A2780-Pac-Res, HCT116-Pac-Res) and parental cells.
Concentration: 5 × and 10 × GI 50 values (GI 50 =197 nM in HCT-116 cells).
Incubation Time: 24 hours.
Result: Induced apoptosis in cells irrespective of MDR-1 overexpression and HCT116-Pac-Res and parental cells.
Cell Line:
Drug-resistant cell lines (KB-V1, A2780-Pac-Res, HCT116-Pac-Res) and parental cells.
Concentration:
5 × and 10 × GI 50 values (GI 50 =197 nM in HCT-116 cells).
Incubation Time:
24 hours.
Result:
Induced apoptosis in cells irrespective of MDR-1 overexpression and HCT116-Pac-Res and parental cells.