A FAK/PYK2 dual inhibitor
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PF-431396

Item No. 17665

Technical Information
Formal Name
N-[2-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]phenyl]-N-methyl-methanesulfonamide
CAS Number
717906-29-1
Molecular Formula
C22H21F3N6O3S
Formula Weight
Purity
≥98%
A crystalline solid
DMF: 20 mg/mlDMSO: 15 mg/ml
λmax
236, 286 nm
SMILES
CN(S(C)(=O)=O)C1=C(CNC2=C(C(F)(F)F)C=NC(NC3=CC=C(NC(C4)=O)C4=C3)=N2)C=CC=C1
InChi Code
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)
InChi Key
POJZIZBONPAWIV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    PF-431396 is a pyrimidine-based dual inhibitor of FAK and PYK2 (IC50s = 2 and 11 nM, respectively).1 In ovariectomized rats, it has been shown to increase bone formation, promoting osteoblast recruitment and activity.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Han, S., Mistry, A., Chang, J.S., et alStructural characterization of proline-rich tyrosine kinase 2 (PYK2) reveals a unique (DFG-out) conformation and enables inhibitor design. The Journal of Biological Chemisty 284(19), 13193-13201 (2009).

    2. Buckbinder, L., Crawford, D.T., Qi, H., et alProline-rich tyrosine kinase 2 regulates osteoprogenitor cells and bone formation, and offers an anabolic treatment approach for osteoporosis. Proc. Natl. Acad. Sci. USA 104(25), 10619-10624 (2007).