PF-431396

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[1][2][3][4].

Product Specifications

CAS Number

[717906-29-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

FAK; Pyk2

Type

Reference compound

Related Pathways

Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/PF-431396.html

Purity

99.74

Solubility

DMSO : ≥ 100 mg/mL

Smiles

CS(=O)(N(C)C1=CC=CC=C1CNC2=NC(NC3=CC4=C(C=C3)NC(C4)=O)=NC=C2C(F)(F)F)=O

Molecular Formula

C22H21F3N6O3S

Molecular Weight

506.50

Precautions

H302, H315, H319, H335

References & Citations

[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.|[2]Ciceri P, et al. Dual kinase-bromodomain inhibitors for rationally designed polypharmacology. Nat Chem Biol. 2014 Mar 2.|[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.|[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.