PF-670462

¥680.00

规格: 5mg

CAS 号:950912-80-8
英文名字:PF670462
质量标准:>98%,BR
货号: MB0402-1

PF-670462
分子式:C19H22Cl2FN5分子量:410.32

简介:PF-670462是有效的、选择性CK1ε和CK1δ抑制剂,IC50分别为90 nM和13 nM。
物理性状及指标:
外观:……………………粉末
溶解性:…………………H2O :28 mg/mL (68.24 mM);Ethanol:82 mg/mL (199.84 mM);DMSO: 82 mg/mL (199.84 mM)
含量:……………………>98%
储存温度:-20℃,避光防潮密闭干燥

生物活性

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。

IC50& Target

CK1δ (Cell-free assay) CK1ε (Cell-free assay)
13 nM 90 nM

体外

PF-670462 is a 14 nM inhibitor of CK1δ in vitro and also potently inhibits p38 and EGFR. In vitro, PF670462 prevents TGF-β-induced epithelial-mesenchymal transition.

体内

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.
(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)

储液配置及储存:按表中溶解性配置;如溶解困难,可以通过快速搅拌,超声或温和加热(在45-60°C下水浴)。液体稳定性报道的很少,建议现配现用,如需储存,建议:-20℃1-3月;-80℃ 3-6月。

浓度/体积/质量

1 mg

5 mg

10 mg

1 mM 2.4371 mL 12.1856 mL 24.3712 mL
5 mM 0.4874 mL 2.4371 mL 4.8742 mL
10 mM 0.2437 mL 1.2186 mL 2.4371 mL
50 mM 0.0487 mL 0.2437 mL 0.4874 mL

【注意】
●我司产品为非无菌包装,若用于细胞培养,请提前做预处理,除去热原细菌,否则会导致染菌。

●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,以上数据仅供参考交流研究之用。

规格

5mg

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