| 产品描述： | EPZ011989 is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ011989 has inhibitory inhibition for EZH2 with a Ki value of <3 nM. EPZ011989 shows robust methyl mark inhibition and anti-tumor activity. EPZ011989 can be used for the research of various cancers |
| 靶点： |
Ki: <3 nM (EZH2); IC50: 94 nM (H3K27 methylation inhibition);HistoneMethyltransferase |
| 体外研究： |
EPZ011989 inhibits mutant and wild-type EZH2 with an Ki value of <3 nM. EPZ011989 reduces cellular H3K27 methylation with an IC50 value of 94 nM. EPZ011989 (0-10 μM; 11 days) has anti-proliferation effect in WSU-DLCL2 cells. Cell Proliferation Assay Cell Line: WSU-DLCL2 cells Concentration: 0-10 μM Incubation Time: 11 days Result: Demonstrated an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM. |
| 体内研究： |
EPZ011989 (oral; 30-1000 mg/kg; single or bid; for 7 days or 21 days) can elicit robust methyl mark inhibition and antitumor activity. Animal Model: SCID mice Dosage: 125, 250, 500, and 1000 mg/kg Administration: Oral; single, twice-daily (BID)for 7 days or twice-daily (BID)for 21 days Result: Provided coverage over the LCC for 24 h (1000 mg/kg ), while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h.Observed complete ablation of the methyl mark by the end of day 7.Showed robust tumor growth inhibition, methyl mark reduction and extended total and free plasma exposure time. |
| 参考文献： |
1. Campbell JE, et al. EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity. ACS Med Chem Lett. 2015 Mar 4;6(5):491-495. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.651 ml |
8.253 ml |
16.507 ml |
| 5 mM |
0.33 ml |
1.651 ml |
3.301 ml |
| 10 mM |
0.165 ml |
0.825 ml |
1.651 ml |
| 50 mM |
0.033 ml |
0.165 ml |
0.33 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