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- 产品描述: OTS514 is a highly potent TOPK inhibitor with an IC50 of 2.6 nM. OTS514 strongly suppresses the growth of TOPK-positive cancer cells[1]. OTS514 induces cell cycle arrest and apoptosis
- 靶点: IC50: 2.6 nM (TOPK);Apoptosis;TOPK
- 体内研究:
OTS514 (1-5 mg/kg; once a day for 2 weeks; intravenous administration) induces tumor regression in a xenograft model of A549 cells (TOPK-positive lung cancer cells). Animal Model: Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells Dosage: 1, 2.5, and 5 mg/kg Administration: Intravenously treated; once every day for 2 weeks Result: Resulted in tumor growth inhibition (TGI) of 5.7, 43.3, and 65.3% on day 15, respectively, without any body weight loss.
- 参考文献:
1. Matsuo Y, et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. Sci Transl Med. 2014 Oct 22;6(259):259ra145. 2. Stefka AT, et al. Potent anti-myeloma activity of the TOPK inhibitor OTS514 in pre-clinical models. Cancer Med. 2020 Jan;9(1):324-334.
- 溶解性: Soluble in DMSO
- 保存条件: -20℃
- 配置溶液浓度参考:
1mg 5mg 10mg 1 mM 2.744 ml 13.719 ml 27.438 ml 5 mM 0.549 ml 2.744 ml 5.488 ml 10 mM 0.274 ml 1.372 ml 2.744 ml 50 mM 0.055 ml 0.274 ml 0.549 ml
- 注意:部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)