基本信息
| 分子式 | C19H22Cl2FN5 |
| 分子量 | 410.32 |
| 存储条件 | Freezer -20℃ |
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（IC50 & Targe）
CK1δ [1]
(Cell-free assay)
13 nM
CK1ε [1]
(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[2].
体内研究
PF670462 administered systemically or locally by inhalation prevents both acute and chronic bleomycin-induced pulmonary fibrosis in mice[2].
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.
(Only for Reference)
动物实验
Animal Models: Six- to eight-week old 20–25 g C57Bl/6 mice
Formulation: initially dissolved in 100% DMSO and prepared for injection by 1:10 dilution in Arachis oil
Dosages: 30 mg/kg/day
Administration: IP
(Only for Reference)
参考文献
[1] Mathieu Bibian, et al. Bioorg Med Chem Lett. 2013, 23(15): 4374–4380.
[2] Keenan CR, et al. Front Pharmacol. 2018, 9:738.
