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PF-670462

品牌
J&K
CAS
950912-80-8
货号
1433443
规格纯度
98%, 一种有效的, 选择性的 casein kinase (CKIε/CKIδ) 抑制剂
参考价格
1167 *本价格含增值税费
促销
服务
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  • 增值税票
数量
-+
产品名称:
950912-80-8
PF-670462
产品介绍:

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.

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