PF 431396

Pricing Availability   Qty
Cat.No. 4278 - PF 431396 | C22H21F3N6O3S | CAS No. 717906-29-1
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)
Datasheet
Citations (8)
Reviews
Literature (2)

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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.

View Related Products by Product Action

View all Focal Adhesion Kinase Inhibitors

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

8 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

Winter et al (2012) Systems-pharmacology dissection of a drug synergy in imatinib-resistant CML. Nat Chem Biol 8 905 PMID: 23023260

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

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


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