Home Metabolism Casein Kinase inhibitor PF-670462 For research use only.

PF-670462

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

PF-670462 Chemical Structure

PF-670462 Chemical Structure

CAS: 950912-80-8

Purity & Quality Control

Batch: Purity: 99.98%
99.98

PF-670462 Related Products

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
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].
Cell Research 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.
In Vivo
In vivo

PF670462 administered systemically or locally by inhalation prevents both acute and chronic bleomycin-induced pulmonary fibrosis in mice[2].
Animal Research Animal Models Six- to eight-week old 20–25 g C57Bl/6 mice
Dosages 30 mg/kg/day
Administration IP

Chemical Information & Solubility

Molecular Weight 410.32 Formula

C19H22Cl2FN5
CAS No. 950912-80-8 SDF --
Smiles C1CCC(CC1)N2C=NC(=C2C3=NC(=NC=C3)N)C4=CC=C(C=C4)F.Cl.Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 82 mg/mL ( (199.84 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 82 mg/mL

Ethanol : 25 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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