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• 產(chǎn)品描述： EPZ031686 is an effective inhibitor of SMYD3 inhibitor with an IC50 of 3 nM and can be used in studies about cancer.

• 靶點： Histone Methyltransferase;HistoneMethyltransferase

• 體內(nèi)研究：
  In male CD-1 mice, EPZ031686 (1 mg/kg; i.v.) shows a moderate clearance (CL) of 27 ± 3.9 mL/min/kg, in very good agreement with the mouse microsomal data, with a volume of distribution at steady state (Vss) of 2.3 ± 0.29 L/kg, translating to a mean terminal half-life (t1/2) of 1.7 ± 0.13 h. After the treatment of EPZ031686 (5 and 50 mg/kg; p.o.), both Cmax and AUC0?last increased in a slightly higher than dose-proportional manner, while t1/2 remained unchanged. Bioavailability (F) of 48 ± 5.4% and 69 ± 8.2%, respectively, leading to EPZ031686 unbound blood concentration remaining above the SMYD3 ICW IC50 value for more than 12 h after a 50 mg/kg p.o.

• 參考文獻(xiàn)：
  1. Mitchell LH et al. Novel Oxindole Sulfonamides and Sulfamides: EPZ031686, the First Orally Bioavailable Small Molecule SMYD3 Inhibitor. ACS Med Chem Lett. 2015 Aug 27;7(2):134-8.

• 溶解性： soluble  in  DMSO

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	1mg	5mg	10mg
  1 mM	1.692 ml	8.459 ml	16.918 ml
  5 mM	0.338 ml	1.692 ml	3.384 ml
  10 mM	0.169 ml	0.846 ml	1.692 ml
  50 mM	0.034 ml	0.169 ml	0.338 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。

輸入產(chǎn)品批號：

本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

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