PF 431396

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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 (4)
Literature

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.

Compound Libraries

PF 431396 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 25.32 50

Preparing Stock Solutions

The following data is based on the product molecular weight 506.5. Batch specific molecular weights may vary from batch to batch due to solvent 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
1 mM 1.97 mL 9.87 mL 19.74 mL
5 mM 0.39 mL 1.97 mL 3.95 mL
10 mM 0.2 mL 0.99 mL 1.97 mL
50 mM 0.04 mL 0.2 mL 0.39 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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: PF431396 focal adhesion kinase fak proline-rich tyrosine kinase 2 pyk2 inhibitors inhibits pfizer Focal Adhesion Kinase

4 Citations for PF 431396

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

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

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


Do you know of a great paper that uses PF 431396 from Tocris? If so please let us know.

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

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Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
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  • MAPK Signaling
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Pathways for PF 431396

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