PF-4800567
Based on 2 publication(s) in Google Scholar
PF-4800567 is a potent and selective inhibitor of casein kinase 1? (CK1?), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM).
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- Purity: 99.69%
- CAS No.: 1188296-52-7
- 화학식: C17H18ClN5O2
- 분자량:359.81
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PF-4800567
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Biological Activity
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CK1δ 711 nM (IC50) |
PF-4800567 is a potent and selective inhibitor of casein kinase 1 (CK1 ), with an IC50 of 32 nM, which is greater than 20-fold selectivity over CK1δ (IC50, 711 nM). PF-4800567 shows inhibitory activity against CK1 and CK1δ in whole cells, with IC50s of 2.65 and 20.38 μM, respectively. PF-4800567 (0.01-10 μM) blocks CK1 -mediated PER3 nuclear localization mediated by CK1 and suppresses PER2 degradation at 1 μM. In addition, PF-4800567 has little effect on the circadian clock at 32 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1188296-52-7
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Appearance Solid
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분자량 359.81
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화학식 C17H18ClN5O2
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Color White to light yellow
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SMILES
NC1=C2C(N(C3CCOCC3)N=C2COC4=CC=CC(Cl)=C4)=NC=N1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
EMBO J
2024 Oct;43(20):4752-4785. PMID: 39256562
용액&용해도
1 M HCl : 50 mg/mL (138.96 mM; Need ultrasonic)
DMSO : 40 mg/mL (111.17 mM; ultrasonic and adjust pH to 3 with 1 M HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / 1 M HCl | 1 mM | 2.7792 mL | 13.8962 mL | 27.7924 mL | 69.4811 mL |
| 5 mM | 0.5558 mL | 2.7792 mL | 5.5585 mL | 13.8962 mL | |
| 10 mM | 0.2779 mL | 1.3896 mL | 2.7792 mL | 6.9481 mL | |
| 15 mM | 0.1853 mL | 0.9264 mL | 1.8528 mL | 4.6321 mL | |
| 20 mM | 0.1390 mL | 0.6948 mL | 1.3896 mL | 3.4741 mL | |
| 25 mM | 0.1112 mL | 0.5558 mL | 1.1117 mL | 2.7792 mL | |
| 30 mM | 0.0926 mL | 0.4632 mL | 0.9264 mL | 2.3160 mL | |
| 40 mM | 0.0695 mL | 0.3474 mL | 0.6948 mL | 1.7370 mL | |
| 50 mM | 0.0556 mL | 0.2779 mL | 0.5558 mL | 1.3896 mL | |
| 60 mM | 0.0463 mL | 0.2316 mL | 0.4632 mL | 1.1580 mL | |
| 80 mM | 0.0347 mL | 0.1737 mL | 0.3474 mL | 0.8685 mL | |
| 100 mM | 0.0278 mL | 0.1390 mL | 0.2779 mL | 0.6948 mL |
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