| 产品描述： | TH287 is a potent and selective inhibitor of MTH1, with an IC50 of 0.8 nM. TH287 is highly selective towards MTH1, with no relevant inhibition of MTH2, NUDT5, NUDT12, NUDT14, NUDT16, dCTPase, dUTPase and ITPA at 100 μM. TH287 could act as a chemotherapeutic agent for cancer research |
| 靶点： |
IC50: 0.8 nM (MTH1);DNA/RNASynthesis;MTH1 |
| 体外研究： |
TH287 (1-10 μM; 24 h) selectively and effectively kills U2OS and other cancer cell lines, but is considerably less toxic to several primary or immortalized cells |
| 体内研究： |
TH287 (5 mg/kg; i.p.) exhibits Cmax of 0.82 μM and tmax of 0.5 h in mice |
| 参考文献： |
1. Gad H, et al. MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool. Nature. 2014 Apr 10;508(7495):215-21. 2. Saleh A, et, al. Development and validation of method for TH588 and TH287, potent MTH1 inhibitors and new anti-cancer agents, for pharmacokinetic studies in mice plasma. J Pharm Biomed Anal. 2015 Feb;104:1-11. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.716 ml |
18.578 ml |
37.157 ml |
| 5 mM |
0.743 ml |
3.716 ml |
7.431 ml |
| 10 mM |
0.372 ml |
1.858 ml |
3.716 ml |
| 50 mM |
0.074 ml |
0.372 ml |
0.743 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京