PF-719
PF-719 is a highly selective Pyk2 inhibitor with an IC50 value of 17 nM. PF-719 promotes the activation of LKB1 and p38 MAPK. PF-719 blocks synaptic deficits induced by Amyloid-beta oligomers and reverses the inhibition of long-term potentiation induced by β-amyloid oligomers. PF-719 can be used in research related to Alzheimer's disease and autoimmune diseases.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.52%
- No. CAS: 1404454-02-9
- Fòrmula: C22H27F3N6O
- Peso molecular:448.48
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Immunology/Inflammation Compound Library
HY-L007
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Kinase Inhibitor Library
HY-L009
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MAPK Compound Library
HY-L010
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Neuronal Signaling Compound Library
HY-L013
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Protein Tyrosine Kinase Compound Library
HY-L016
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Oxygen Sensing Compound Library
HY-L045
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Pyroptosis Compound Library
HY-L059
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Anti-Alzheimer's Disease Compound Library
HY-L069
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Anti-Lung Cancer Compound Library
HY-L075
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Anti-Blood Cancer Compound Library
HY-L079
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Anti-Cancer Metabolism Compound Library
HY-L083
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HY-L086
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Angiogenesis-Related Compound Library
HY-L088
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HY-L131
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Highly Selective Inhibitors Library
HY-L158
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Highly Selective Activators Library
HY-L159
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Anti-Hematopathy Compound Library
HY-L171
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Cell Proliferation Compound Library
HY-L201
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High-Throughput Bioactive Compound Library
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Lactylation Compound Library
HY-L249
Actividad biológica
PF-719 (2 h) inhibits the activity of Pyk2 and significantly increases the phosphorylation levels of Tau at the S396/S404 and S202/T205 sites in mature iPSC-derived cortical neurons, without altering the activity of GSK3β[1].
Pretreatment of acute hippocampal slices from wild-type mice with PF-719 (500 nM; 30 min) completely reverses the β-amyloid oligomer-induced inhibition of long-term potentiation[2].
PF-719 is a highly selective inhibitor of purified Pyk2 kinase in vitro, with an IC50 value of 17 nM[3].
PF-719 (1 μM; 1 h pre-incubation, 3 h chemokinesis assay) inhibits CXCL13-induced chemotaxis of primary mouse splenic B-2 cells and marginal zone (MZ) B cells, as well as S1P-induced chemotaxis of MZ B cells at a concentration of 1 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A20 murine B-lymphoma cells
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Concentration:0.5-2.5 μM
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Incubation Time:1 h (pre-incubation); 3 min (S1P stimulation)
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Result:Completely inhibited S1P-induced tyrosine phosphorylation of Pyk2 at 1 μM.
Showed little to no effect on FAK tyrosine phosphorylation at 1 μM.
Blocked both Pyk2 and FAK tyrosine phosphorylation at 2.5 μM.
Chemical Information
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No. CAS 1404454-02-9
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Appearance Solid
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Peso molecular 448.48
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Fòrmula C22H27F3N6O
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Color White to off-white
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SMILES
O=C(NC1CC1)C2=CC=C(NC3=NC=C(C(F)(F)F)C(N[C@H]4[C@H](N(C)C)CCC4)=N3)C=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 50 mg/mL (111.49 mM; ultrasonic and warming and heat to 60°C; 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.08 mg/mL (4.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Brody AH, et al. Alzheimer risk gene product Pyk2 suppresses tau phosphorylation and phenotypic effects of tauopathy. Mol Neurodegener. 2022;17(1):32. Published 2022 May 3. [Content Brief]
[2]. Salazar SV, et al. Alzheimer's Disease Risk Factor Pyk2 Mediates Amyloid-β-Induced Synaptic Dysfunction and Loss. J Neurosci. 2019;39(4):758-772. [Content Brief]
[3]. Tse KW, et al. Small molecule inhibitors of the Pyk2 and FAK kinases modulate chemoattractant-induced migration, adhesion and Akt activation in follicular and marginal zone B cells. Cell Immunol. 2012 Jan-Feb;275(1-2):47-54. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2298 mL | 11.1488 mL | 22.2975 mL | 55.7438 mL |
| 5 mM | 0.4460 mL | 2.2298 mL | 4.4595 mL | 11.1488 mL | |
| 10 mM | 0.2230 mL | 1.1149 mL | 2.2298 mL | 5.5744 mL | |
| 15 mM | 0.1487 mL | 0.7433 mL | 1.4865 mL | 3.7163 mL | |
| 20 mM | 0.1115 mL | 0.5574 mL | 1.1149 mL | 2.7872 mL | |
| 25 mM | 0.0892 mL | 0.4460 mL | 0.8919 mL | 2.2298 mL | |
| 30 mM | 0.0743 mL | 0.3716 mL | 0.7433 mL | 1.8581 mL | |
| 40 mM | 0.0557 mL | 0.2787 mL | 0.5574 mL | 1.3936 mL | |
| 50 mM | 0.0446 mL | 0.2230 mL | 0.4460 mL | 1.1149 mL | |
| 60 mM | 0.0372 mL | 0.1858 mL | 0.3716 mL | 0.9291 mL | |
| 80 mM | 0.0279 mL | 0.1394 mL | 0.2787 mL | 0.6968 mL | |
| 100 mM | 0.0223 mL | 0.1115 mL | 0.2230 mL | 0.5574 mL |
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