產(chǎn)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 |
靶點: |
IC50: 2.6 nM (TOPK);Apoptosis;TOPK |
體內(nèi)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. |
參考文獻: |
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 |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
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: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。 |