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PF 431396
- Soluble in DMSO
- MF: C22H21F3N6O3S
- MW: 506.5
Description
PF 431396 is a dual focal adhesion kinase (FAK/PTK2) and proline-rich tyrosine kinase 2 (PYK2/PTK2B) inhibitor with IC50 values of 1.5 nM for FAK and 11 nM for PYK2. It has been reported to increase bone formation and protect against bone loss in ovariectomized rats.
FAK and PYK2 regulate integrin signaling, adhesion-dependent survival, cytoskeletal remodeling and bone cell function. PF 431396 is pharmacologically relevant for studying kinase control of cell adhesion, migration and skeletal remodeling.
Key Features
- Dual FAK and PYK2 kinase inhibitor
- Nanomolar potency against FAK and PYK2
- Modulates focal adhesion and cytoskeletal signaling
- Reported activity in bone-loss models
Applications
- FAK/PYK2 pathway studies
- Cell adhesion and migration assays
- Bone remodeling and osteogenesis research
- Cancer invasion and metastasis models
More Information
| Parent CAS No. | 717906-29-1 |
|---|---|
| Chemical Name | N-methyl-N-(2-((2-(2-oxoindolin-5-ylamino)-5-(trifluoromethyl)pyrimidin-4-ylamino)methyl)phenyl)methanesulfonamide |
| extra_info | . |
| SMILES | CS(N(C1=CC=CC=C1CNC1C(C(F)(F)F)=CN=C(NC2C=CC3=C(C=2)CC(=O)N3)N=1)C)(=O)=O |
| MFCD | MFCD16038300 |
| InChi | InChI=1S/C22H21F3N6O3S/c1-31(35(2,33)34)18-6-4-3-5-13(18)11-26-20-16(22(23,24)25)12-27-21(30-20)28-15-7-8-17-14(9-15)10-19(32)29-17/h3-9,12H,10-11H2,1-2H3,(H,29,32)(H2,26,27,28,30) |
| InChiKey | POJZIZBONPAWIV-UHFFFAOYSA-N |
| CID | 11598628 |
| Short Description | FAK/PYK2 inhibitor |
References
- L Buckbinder et al. Proline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis. Proc. Nat. Acad. Sci. 2007, 104(25), 10619-10624.
- S 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, 19, 13193-13201.
- DP Walker et al. Sulfoximine-substituted trifluoromethylpyrimidine analogs as inhibitors of proline-rich tyrosine kinase 2 (PYK2) show reduced hERG activity. Bioorg. Med. Chem. Let. 2009, 19(12), 3253-3258.


