Name | 3-[(3-chlorophenoxy)methyl]-1-(oxan-4-yl)pyrazolo[3,4-d]pyrimidin-4-amine |
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Synonyms |
16W
4hnf PF-4800567 4hni |
Description | PF-4800567 is a potent and selective inhibitor of casein kinase 1ϵ (CK1ϵ), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM). |
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Related Catalog | |
Target |
CK1ϵ:32 nM (IC50) CKIδ:711 nM (IC50) |
In Vitro | PF-4800567 is a potent and selective inhibitor of casein kinase 1ϵ (CK1ϵ), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM). PF-4800567 shows inhibitory activity against CK1ϵ and CK1δ in whole cells, with IC50s of 2.65 and 20.38 μM, respectively. PF-4800567 (0.01-10 μM) blocks CK1ϵ-mediated PER3 nuclear localization mediated by CK1ϵ and suppresses PER2 degradation at 1 μM. In addition, PF-4800567 has little effect on the circadian clock at 32 nM[1]. |
In Vivo | PF-4800567 (100 mg/kg, s.c.) is rapidly absorpted and distributed in plasma and brain of mice[1]. |
Cell Assay | For drug treatment, 24 h after synchronization, individual dishes of cells under PMT recording are treated with CK1 inhibitors (PF-4800567 or PF-670462 at a range of doses) or DMSO (vehicle control). The compounds are left continuously with the samples thereafter, and the luminescence patterns are recorded for at least 6 days. Periods are analyzed by use of RAP software[1]. |
References |
Density | 1.5±0.1 g/cm3 |
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Boiling Point | 592.9±50.0 °C at 760 mmHg |
Molecular Formula | C17H18ClN5O2 |
Molecular Weight | 359.810 |
Flash Point | 312.4±30.1 °C |
Exact Mass | 359.114899 |
PSA | 88.08000 |
LogP | 1.97 |
Vapour Pressure | 0.0±1.7 mmHg at 25°C |
Index of Refraction | 1.718 |
Storage condition | 2-8℃ |