PF-670462

For research use only.

Catalog No.S6734

PF-670462 Chemical Structure

CAS No. 950912-80-8

PF-670462 is a potent and selective inhibitor of CK1ε and CK1δ with IC50 value of 90 nM and 13 nM, respectively.

Purity & Quality Control

Choose Selective Casein Kinase Inhibitors

Biological Activity

Description PF-670462 is a potent and selective inhibitor of CK1ε and CK1δ with IC50 value of 90 nM and 13 nM, respectively.
Targets
CK1δ [1]
(Cell-free assay)
CK1ε [1]
(Cell-free assay)
13 nM 90 nM
In vitro

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].

In vivo

PF670462 administered systemically or locally by inhalation prevents both acute and chronic bleomycin-induced pulmonary fibrosis in mice[2].

Protocol

Cell Research:

[2]

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  • 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)
Animal Research:

[2]

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  • Animal Models: Six- to eight-week old 20–25 g C57Bl/6 mice
  • Dosages: 30 mg/kg/day
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 82 mg/mL (199.84 mM)
Water 82 mg/mL (199.84 mM)
Ethanol 28 mg/mL (68.23 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 410.32
Formula

C19H22Cl2FN5

CAS No. 950912-80-8
Storage powder
in solvent
Synonyms N/A
Smiles C1CCC(CC1)N2C=NC(=C2C3=NC(=NC=C3)N)C4=CC=C(C=C4)F.Cl.Cl

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID