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• 产品描述： PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM in a cell-free assay.

• 靶点： IC50: 0.22 μM (BRD4);Apoptosis;EpigeneticReaderDomain;Autophagy

• 体内研究：
  PFI-1 administrated (1 mg/kg, i.v.) in the rat results in the volume of distribution of 1 L/kg, the plasma clearance of 18 mL/min/kg and half-life of 1 hour. PFI-1 oral dosed (2 mg/kg) in the rat results in the oral bioavailability as low as 32%. PFI-1 administrated (2 mg/kg, s.c.) in the mouse results in a Cmax of 58 ng/mL with a Tmax of 1 h and a half-life of approximately 2 hours

• 参考文献：
  1. Picaud S, et al. PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains. Cancer Res. 2013 May 21. [Epub ahead of print] 2. Fish PV, et al. Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. J Med Chem. 2012 Nov 26;55(22):9831-7. 3. Cheng Z, et al. Inhibition of BET bromodomain targets genetically diverse glioblastoma. Clin Cancer Res. 2013 Apr 1;19(7):1748-59. 4. Kate E Lines, et al. Epigenetic modifiers reduce proliferation of human neuroendocrine tumour cell lines. Endocrine Abstracts (2013) 31 P149

• 溶解性： DMSO  :  33.33  mg/mL  (95.94  mM;  Need  ultrasonic)

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.879 ml	14.393 ml	28.786 ml
  5 mM	0.576 ml	2.879 ml	5.757 ml
  10 mM	0.288 ml	1.439 ml	2.879 ml
  50 mM	0.058 ml	0.288 ml	0.576 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。

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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 *