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PF-670462 Casein Kinase inhibitor

Name: PF-670462
Brand: Selleck Chemicals
SKU: S6734
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S6734

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

Chemical Structure

Molecular Weight: 410.32

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP (HSP90) Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Amino Acids and Derivatives Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO Hydroxylase PCSK9 OXPHOS ROR
Related Products	Silmitasertib (CX-4945) Silmitasertib (CX-4945) sodium salt D 4476 TBB IC261 (E/Z)-GO289 TTP 22 Longdaysin PF 4800567 Ellagic Acid hydrate 7-Hydroxy-4-methyl-8-nitrocoumarin BTX-A51 SR-3029 DEG-77 DEG-35 CKI-7 SSTC3 BMS-986397 PF-05251749（CK1-IN-2） Casein Kinase 2β Antibody [K14H23] CK1-IN-1 5,6-Dichlorobenzimidazole 1-beta-D-ribofuranoside DMAT Hematein TA-01

Chemical Information, Storage & Stability

Molecular Weight	410.32	Formula	C₁₉H₂₂Cl₂FN₅	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	950912-80-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CCC(CC1)N2C=NC(=C2C3=NC(=NC=C3)N)C4=CC=C(C=C4)F.Cl.Cl

Solubility

In vitro
Batch:

DMSO : 82 mg/mL (199.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 82 mg/mL

Ethanol : 25 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.100mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 82 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.410mg/ml (1.00mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	CK1δ ^[1] (Cell-free assay) 13 nM CK1ε ^[1] (Cell-free assay) 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].
References	[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3783656/ [2] https://pubmed.ncbi.nlm.nih.gov/30042678/

Tech Support

Handling Instructions

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