A selective FAK/PYK2 inhibitor
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PF-562271 (besylate)

Item No. 18499

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[[[2-[(2,3-dihydro-2-oxo-1H-indol-5-yl)amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]methyl]-2-pyridinyl]-N-methyl-methanesulfonamide, monobenzenesulfonate
CAS Number
939791-38-5
Molecular Formula
C21H20F3N7O3S • C6H6O3S
Formula Weight
665.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 0.25 mg/mlDMSO: 1 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
204, 262 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=N1.OS(C5=CC=CC=C5)(=O)=O
InChi Code
InChI=1S/C21H20F3N7O3S.C6H6O3S/c1-31(35(2,33)34)19-12(4-3-7-25-19)10-26-18-15(21(22,23)24)11-27-20(30-18)28-14-5-6-16-13(8-14)9-17(32)29-16;7-10(8,9)6-4-2-1-3-5-6/h3-8,11H,9-10H2,1-2H3,(H,29,32)(H2,26,27,28,30);1-5H,(H,7,8,9)
InChi Key
LKLWTLXTOVZFAE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $178

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    10 mg

    $293

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    50 mg

    $853

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    Product Description

    PF-562271 is an ATP-competitive, reversible inhibitor of FAK (IC50 = 1.5 nM) that demonstrates 10-fold reduced potency for PYK2 (IC50 = 14 nM) and >100-fold selectivity against other protein kinases.1 PF-562271 inhibits FAK phosphorylation with an EC50 value of 93 ng/ml in glioblastoma-bearing mice and has been shown to regress tumors in multiple xenograft models.1,2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Roberts, W.G., Ung, E., Whalen, P., et al. Antitumor activity and pharmacology of a selective focal adhesion kinase inhibitor, PF-562,271. Cancer Res. 68(6), 1935-1944 (2008).

    2. Stokes, J.B., Adair, S.J., Slack-Davis, J.K., et al. Inhibition of focal adhesion kinase by PF-562,271 inhibits the growth and metastasis of pancreatic cancer concomitant with altering the tumor microenvironment. Mol. Cancer Ther. 10(11), 2135-2145 (2011).