PF 4800567

Modify Date: 2024-01-04 09:22:21

PF 4800567 Structure
PF 4800567 structure
Common Name PF 4800567
CAS Number 1188296-52-7 Molecular Weight 359.810
Density 1.5±0.1 g/cm3 Boiling Point 592.9±50.0 °C at 760 mmHg
Molecular Formula C17H18ClN5O2 Melting Point N/A
MSDS N/A Flash Point 312.4±30.1 °C

 Use of PF 4800567


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).

 Names

Name 3-[(3-chlorophenoxy)methyl]-1-(oxan-4-yl)pyrazolo[3,4-d]pyrimidin-4-amine
Synonym More Synonyms

 PF 4800567 Biological Activity

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).
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

[1]. Walton KM, et al. Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. J Pharmacol Exp Ther. 2009 Aug;330(2):430-9.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
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℃

 Synonyms

16W
4hnf
PF-4800567
4hni
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Price: ¥990/10 mM * 1 mL in DMSO

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