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Submit ReviewPF 431396
Description: Dual FAK/PYK2 inhibitor
Chemical Name: N-Methyl-N-[2-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]phenyl]methanesulfonamide
Purity: ≥98% (HPLC)
Biological Activity for PF 431396
PF 431396 is a dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor (IC50 values are 2 and 11 nM respectively). Promotes osteoblast recruitment and activity, and stimulates bone formation in ovariectomized rats.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Compound Libraries for PF 431396
PF 431396 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for PF 431396
| M. Wt | 506.5 |
| Formula | C22H21F3N6O3S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 717906-29-1 |
| PubChem ID | 11598628 |
| InChI Key | POJZIZBONPAWIV-UHFFFAOYSA-N |
| Smiles | O=C2NC1=CC=C(NC3=NC=C(C(F)(F)F)C(NCC4=CC=CC=C4N(C)S(=O)(C)=O)=N3)C=C1C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PF 431396
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 25.32 | 50 |
Preparing Stock Solutions for PF 431396
The following data is based on the product molecular weight 506.5. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 3.95 mL | 19.74 mL | 39.49 mL |
| 2.5 mM | 0.79 mL | 3.95 mL | 7.9 mL |
| 5 mM | 0.39 mL | 1.97 mL | 3.95 mL |
| 25 mM | 0.08 mL | 0.39 mL | 0.79 mL |
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Product Datasheets for PF 431396
References for PF 431396
References are publications that support the biological activity of the product.
Buckbinder et al (2007) Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis. Proc.Natl.Acad.Sci.USA 104 10619 PMID: 17537919
Han et al (2009) Structural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design. J.Biol.Chem. 284 13193 PMID: 19244237
Allen et al (2010) Emerging targets in osteoporosis disease modification. J.Med.Chem. 53 4332 PMID: 20218623
If you know of a relevant reference for PF 431396, please let us know.
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Keywords: PF 431396, PF 431396 supplier, PF431396, focal, adhesion, kinase, fak, proline-rich, tyrosine, 2, pyk2, inhibitors, inhibits, pfizer, Focal, Adhesion, Kinase, Other, Kinases, 4278, Tocris Bioscience
10 Citations for PF 431396
Citations are publications that use Tocris products. Selected citations for PF 431396 include:
Pasquier et al (2018) CCL2/CCL5 secreted by the stroma induce IL-6/PYK2 dependent chemoresistance in ovarian cancer. Mol Cancer 17 47 PMID: 29455640
Cheng et al (2015) IgE-activated basophils regulate eosinophil tissue entry by modulating endothelial function. BMC Neurosci 212 513 PMID: 25779634
Chapman et al (2015) Proline-rich tyrosine kinase 2 controls PI3-kinase activation downstream of the T cell antigen receptor in human T cells. Sci Rep 97 285 PMID: 25387834
Brian et al (2019) Unique-region phosphorylation targets LynA for rapid degradation, tuning its expression and signaling in myeloid cells. Elife 8 PMID: 31282857
Kotla and Rao (2015) Reactive Oxygen Species (ROS) Mediate p300-dependent STAT1 Protein Interaction with Peroxisome Proliferator-activated Receptor (PPAR)-γ in CD36 Protein Expression and Foam Cell Formation. J Biol Chem 290 30306 PMID: 26504087
Jing et al (2018) Methods for High-throughput Drug Combination Screening and Synergy Scoring. Methods Mol Biol 1711 351-398 PMID: 29344898
Winter et al (2012) Systems-pharmacology dissection of a drug synergy in imatinib-resistant CML. Nat Chem Biol 8 905 PMID: 23023260
Mishra and Singh (2014) HIV-1 Tat C phosphorylates VE-cadherin complex and increases human brain microvascular endothelial cell permeability. J Leukoc Biol 15 80 PMID: 24965120
Santiago et al (2020) Cx43 and Associated Cell Signaling Pathways Regulate Tunneling Nanotubes in Breast Cancer Cells. Cancers (Basel) 12 PMID: 33003486
Kundumani-Sridharan et al (2013) 12/15-Lipoxygenase mediates high-fat diet-induced endothelial tight junction disruption and monocyte transmigration: a new role for 15(S)-hydroxyeicosatetraenoic acid in endothelial cell dysfunction. J Biol Chem 288 15830 PMID: 23589307
Do you know of a great paper that uses PF 431396 from Tocris? Please let us know.
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