货号	规格	价格	上海	北京	珠海	重庆	武汉
S87509-5mg	99.86%	￥192.00 S87509-5mg ￥192.00 现货	1 1	-	-	-	-
S87509-10mg	99.86%	￥325.00 S87509-10mg ￥325.00 现货	2 2	-	-	-	-
S87509-25mg	≥99%	￥650.00 S87509-25mg ￥650.00 2-3天	0 货期：2-3天	-	-	-	-
S87509-100mg	≥99%	￥1900.00 S87509-100mg ￥1900.00 2-3天	0 货期：2-3天	-	-	-	-

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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;CaseinKinase

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

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。

参考文献

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