PF-670462

Catalog No.S6734 Batch:S673402

Technical Data

Formula	C₁₉H₂₂Cl₂FN₅
Molecular Weight	410.32	CAS No.	950912-80-8
Solubility (25°C)*	In vitro	DMSO	82 mg/mL (199.84 mM)
		Water	82 mg/mL (199.84 mM)
		Ethanol	25 mg/mL (60.92 mM)
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:^{^[2]}	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.
Animal Study:^{^[2]}	Animal Models Six- to eight-week old 20–25 g C57Bl/6 mice Dosages 30 mg/kg/day Administration IP

Cell Assay:^{^[2]}

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.

Animal Study:^{^[2]}

Animal Models
Six- to eight-week old 20–25 g C57Bl/6 mice
Dosages
30 mg/kg/day
Administration
IP

References

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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