PF-4800567 |
Katalog-Nr.GC44612
One-Click Copy Product Info
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PF-4800567 ist ein potenter und selektiver Inhibitor der Caseinkinase 1ε (CK1ε) mit einem IC50 von 32 nM, was eine mehr als 20-fache SelektivitÄt gegenÜber CK1δ (IC50, 711 nM) bedeutet.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1188296-52-7
Sample solution is provided at 25 µL, 10mM.
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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 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].
PF-4800567 (100 mg/kg, s.c.) is rapidly absorpted and distributed in plasma and brain of mice[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.
Cell experiment: | 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. | |
| Cas No. | 1188296-52-7 | SDF | |
| Canonical SMILES | ClC1=CC(OCC2=NN(C3CCOCC3)C4=NC=NC(N)=C42)=CC=C1 | ||
| Formula | C17H18ClN5O2 | M.Wt | 359.8 |
| Löslichkeit | DMF: 25 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 10 mg/ml,Ethanol: 1 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7793 mL | 13.8966 mL | 27.7932 mL |
| 5 mM | 555.9 μL | 2.7793 mL | 5.5586 mL |
| 10 mM | 277.9 μL | 1.3897 mL | 2.7793 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)