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• 产品描述： PF-670462是有效的、选择性CK1ε和CK1δ抑制剂，IC50分别为90 nM和13 nM

• 靶点： CK1δ(Cell-free assay):13 nM; CK1ε(Cell-free assay):90 nM

• 体外研究： PF-670462 is a 14 nM inhibitor of CK1δ in vitro and also potently inhibits p38 and EGFR[1]. In vitro, PF670462 prevents TGF-β-induced epithelial-mesenchymal transition

• 体内研究： PF670462 administered systemically or locally by inhalation prevents both acute and chronic bleomycin-induced pulmonary fibrosis in mice

• 细胞实验： Cell lines: A549 cells Concentrations: 0.3-10 μM Incubation Time: 48 h Method: A549 cells are left to adhere overnight. Cells are then serum-starved for 16 h prior to pre-incubation with PF670462 (0.3-10 μM) for 30 min then TGF-β (100 pM) for 48 h. Cells are fixed in 10% neutral buffered formalin for 15 min and non-specific binding sites are blocked by incubation with 5% normal goat serum/0.3% Triton X-100 in PBS for 1 h. E-Cadherin expression is detected by immunofluorescence staining.

• 动物实验： Animal Models: Six- to eight-week old 20–25 g C57Bl/6 mice Dosages: 30 mg/kg/day Administration: IP

• 参考文献：
  1. Mathieu Bibian, et al. Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties. Bioorg Med Chem Lett. 2013, 23(15): 4374–4380. 2. Keenan CR, et al. Casein Kinase 1δ/ε Inhibitor, PF670462 Attenuates the Fibrogenic Effects of Transforming Growth Factor-β in Pulmonary Fibrosis. Front Pharmacol. 2018, 9:738.

• 溶解性： Soluble  in  DMSO、H2O、Ethanol

• 保存条件： 2-8℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.437 ml	12.186 ml	24.371 ml
  5 mM	0.487 ml	2.437 ml	4.874 ml
  10 mM	0.244 ml	1.219 ml	2.437 ml
  50 mM	0.049 ml	0.244 ml	0.487 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 分子量 (g/mol)

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