PF 431396

Cat. No. 4278

PF 431396 C22H21F3N6O3S [717906-29-1]

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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

Biological Activity

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.

Technical Data

M.Wt:
506.5
Formula:
C22H21F3N6O3S
Solubility:
Soluble to 50 mM in DMSO
Purity:
>98 %
Storage:
Store at +4°C
CAS No:
717906-29-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Allen et al (2010) Emerging targets in osteoporosis disease modification. J.Med.Chem. 53 4332. PMID: 20218623.

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.

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.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for PF 431396 include:

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.

Cheng et al (2015) IgE-activated basophils regulate eosinophil tissue entry by modulating endothelial function. BMC Neurosci 212 513. PMID: 25779634.

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.

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.

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Keywords: PF 431396, supplier, PF431396, focal, adhesion, kinase, fak, proline-rich, tyrosine, kinase, 2, pyk2, inhibitors, inhibits, pfizer, Tocris Bioscience, Focal Adhesion Kinase Inhibitor products

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