PF-431396
Based on 6 publication(s) in Google Scholar
PF-431396 is an orally active dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with IC50 values of 2 nM and 11 nM, respectively.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.74%
- CAS. Nr.: 717906-29-1
- Formel: C22H21F3N6O3S
- Molecular Weight:506.50
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) PF-431396
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
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| BT-20 | IC50 |
6.2 μM
Compound: 97; PF431396
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Anticancer activity against human BT-20 cells assessed as cell growth inhibition by MTT assay
Anticancer activity against human BT-20 cells assessed as cell growth inhibition by MTT assay
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[PMID: 33650861] |
PF-431396 has a Kd value of 445 nM for BRD4[2].
PF-431396 appeares to selectively inhibit BCR-induced tyrosine phosphorylation of Pyk2 and FAK[3].
PF-431396 (2.5, 5 μM, 45 min) inhibits the phosphorylation of Pyk2 and FAK induced by clustering LFA-1 with plate-bound Abs[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A20 cells ((105 cells in 0.5 ml of RPMI 1640 medium with 2% fetal calf serum and 50 μM 2-mercaptoethanol)).
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Concentration:0.15, 1, 2.5, 5 μM.
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Incubation Time:45 min.
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Result:The phosphorylation of Pyk2 and FAK induced by clustering LFA-1 with plate-bound Abs was also inhibited.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague–Dawley female rats (ovariectomized (OVX) Rats)[4].
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Dosage:10 or 30 mg/kg.
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Administration:Oral gavage, for 28 consecutive days.
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Result:Counteracted OVX-induced bone loss, completely preserving total bone content and total bone density.
Promoted osteoblast recruitment and activity.
Chemical Information
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CAS. Nr. 717906-29-1
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Appearance Solid
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Molecular Weight 506.50
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Formel C22H21F3N6O3S
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Color Light yellow to yellow
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SMILES
CS(=O)(N(C)C1=CC=CC=C1CNC2=NC(NC3=CC4=C(C=C3)NC(C4)=O)=NC=C2C(F)(F)F)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Death Differ
Functional genomic screens uncover FERMT2 as a critical regulator of YAP/TAZ-driven tumorigenicity. [Abstract]2026 Mar 6. PMID: 41792242 -
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 -
Mucosal Immunol
ADP/P2Y1 aggravates inflammatory bowel disease through ERK5-mediated NLRP3 inflammasome activation. [Abstract]2020 Nov;13(6):931-945. PMID: 32518369 -
J Periodontal Res
Periostin of human periodontal ligament fibroblasts promotes migration of human mesenchymal stem cell through the αvβ3 integrin/FAK/PI3K/Akt pathway. [Abstract]2015 Dec;50(6):855-863. PMID: 25900259
PF-431396 purchased from MedChemExpress. Usage Cited in: J Periodontal Res. 2015 Dec;50(6):855-863. [Abstract]
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Biomed Res Int
1'H-Indole-3'-Carbonyl-Thiazole-4-Carboxylic Acid Methyl Ester Blocked Human Glioma Cell Invasion via Aryl Hydrocarbon Receptor's Regulation of Cytoskeletal Contraction. [Abstract]2020 Oct 3;2020:2616930. PMID: 33083460 -
Lösungsmittel & Löslichkeit
DMSO : ≥ 100 mg/mL (197.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (4.94 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.
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.
Reinheit & Dokumentation
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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)
Verweise
[1]. Seungil Han, et al. Structural Characterization of Proline-rich Tyrosine Kinase 2 (PYK2) Reveals a Unique (DFG-out) Conformation and Enables Inhibitor Design. J Biol Chem. 2009 May 8; 284(19): 13193–13201. [Content Brief]
[2]. Ciceri P, et al. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nat Chem Biol. 2014 Mar 2. [Content Brief]
[3]. Tse KW, et al. B cell receptor-induced phosphorylation of Pyk2 and focal adhesion kinase involves integrins and the Rap GTPases and is required for B cell spreading. J Biol Chem. 2009 Aug 21;284(34):22865-77. [Content Brief]
[4]. Leonard Buckbinder, et al. Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis. Proc Natl Acad Sci U S A. 2007 Jun 19;104(25):10619-24. [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 | 1.9743 mL | 9.8717 mL | 19.7433 mL | 49.3583 mL |
| 5 mM | 0.3949 mL | 1.9743 mL | 3.9487 mL | 9.8717 mL | |
| 10 mM | 0.1974 mL | 0.9872 mL | 1.9743 mL | 4.9358 mL | |
| 15 mM | 0.1316 mL | 0.6581 mL | 1.3162 mL | 3.2906 mL | |
| 20 mM | 0.0987 mL | 0.4936 mL | 0.9872 mL | 2.4679 mL | |
| 25 mM | 0.0790 mL | 0.3949 mL | 0.7897 mL | 1.9743 mL | |
| 30 mM | 0.0658 mL | 0.3291 mL | 0.6581 mL | 1.6453 mL | |
| 40 mM | 0.0494 mL | 0.2468 mL | 0.4936 mL | 1.2340 mL | |
| 50 mM | 0.0395 mL | 0.1974 mL | 0.3949 mL | 0.9872 mL | |
| 60 mM | 0.0329 mL | 0.1645 mL | 0.3291 mL | 0.8226 mL | |
| 80 mM | 0.0247 mL | 0.1234 mL | 0.2468 mL | 0.6170 mL | |
| 100 mM | 0.0197 mL | 0.0987 mL | 0.1974 mL | 0.4936 mL |
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