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描述 | Microtubules are highly dynamic structures that form spindle fibres during mitosis and are one of the most validated cancer targets. SSE15206 is a microtubule polymerization inhibitor with GI50 value of 197 nM in HCT116 cells. SSE15206 also exhibited potent antiproliferative activities against several other cancer cell lines of different origins (leukaemia, breast, lung, and cervical) with sub-micromolar GI50 values. Further, dose-dependent increase in phosphorylation of both histone H3 and MPM2 was observed in CT116 cells following treatment with SSE15206 (0.5 μM, 1 μM and 2 μM) for 4 and 8 hours indicating mitotic arrest. Similarly, treatment with SSE15206 for 8 and 24 hours increased mitotic index (percentage mitotic cells) compared to the DMSO control. Within four hours of treatment with 1 μM SSE15206, CT116 cells started accumulating in the G2/M phase of the cell cycle compared to the DMSO control. The G2/M arrest increased in a time-dependent manner and peaked at 12 hours. Moreover, treatment of three different cell types, HCT116, A549 and CAL-51 with SSE15206 (0.5 μM, 1 μM and 2 μM) for 24 hours, resulted in increased expression of p53 and p21 compared to DMSO control[1]. |
作用机制 | SSE15206 inhibits microtubule polymerization by binding to colchicine site in tubulin[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.69mL 0.54mL 0.27mL |
13.46mL 2.69mL 1.35mL |
26.92mL 5.38mL 2.69mL |
CAS号 | 1370046-40-4 |
分子式 | C19H21N3O3S |
分子量 | 371.453 |
别名 | |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
DMSO: 145 mg/mL(390.36 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |