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• 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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *