Biological Activity
Potent and selective casein kinase 1ε (CK1ε) and CK1δ inhibitor (IC50 values are 7.7 and 14 nM respectively) that displays > 30-fold selectivity over 42 other common kinases. Inhibits PER protein nuclear translocation (EC50 = 290 nM) causing phase shifts in circadian rhythms and attenuates methamphetamine-stimulated locomotion in vivo.
Compound Libraries
PF 670462 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 410.32 |
| Formula | C19H20FN5.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 950912-80-8 |
| PubChem ID | 51049607 |
| InChI Key | PSNKGVAXBSAHCH-UHFFFAOYSA-N |
| Smiles | NC1=NC=CC(C2=C(C4=CC=C(F)C=C4)N=CN2C3CCCCC3)=N1.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.03 | 100 | |
| ethanol | 20.52 | 50 | |
| water | 41.03 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 410.32. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.44 mL | 12.19 mL | 24.37 mL |
| 5 mM | 0.49 mL | 2.44 mL | 4.87 mL |
| 10 mM | 0.24 mL | 1.22 mL | 2.44 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Badura et al (2007) An inhibitor of casein kinase Iε induces phase delays in circadian rhythms under free-running and entrained conditions. J.Pharmacol.Exp.Ther. 322 730 PMID: 17502429
Bryant et al (2009) A role for casein kinase 1 epsilon in the locomotor stimulant response to methamphetamine. Psychopharmacology 203 703 PMID: 19050854
Sprose et al (2009) Inhibition of casein kinase I ε/δ produces phase shifts in the circadian rhythms of Cynomolgus monkeys. Psychopharmacology 204 735 PMID: 19277609
Keywords: PF 670462, supplier, Potent, selective, CK1ε, CK1epsilon, CK1δ, CK1delta, inhibitors, inhibits, Casein, Kinases, 1, PF670462, circadian, rhythms, Casein, Kinase, 1, Casein, Kinase, 1, Tocris Bioscience
