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    PF-562271
    PF-562271

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V2696
    CAS #: 717907-75-0 (free base)Purity ≥98%

    Description: PF-562271 is a novel, potent, ATP-competitive, orally bioavailable, reversible inhibitor of FAK (focal adhesion kinase) and Pyk2 catalytic activity with a IC50 of 1.5 and 14 nmol/L, respectively. it has >100-fold selectivity against other protein kinases. Additionally, PF-562,271 displayed robust inhibition in an inducible cell-based assay measuring phospho-FAK with an IC(50) of 5 nmol/L. PF-562,271 was evaluated against multiple kinases and displays >100x selectivity against a long list of nontarget kinases. PF-562,271 inhibits FAK phosphorylation in vivo in a dose-dependent fashion (calculated EC(50) of 93 ng/mL, total) after p.o. administration to tumor-bearing mice. In vivo inhibition of FAK phosphorylation (>50%) was sustained for >4 hours with a single p.o. dose of 33 mg/kg. Antitumor efficacy and regressions were observed in multiple human s.c. xenograft models. PF-562271 is a potential therapeutic agent either alone or in combination with other agents for the treatment of cancer. 

    References: Cancer Res. 2008 Mar 15;68(6):1935-44; Cancer Biol Ther. 2010 Jul 1;10(1):38-43.

    Related CAS #: 939791-39-6 (mesylate); 939791-41-0 (HCl); 939791-40-9 (tosylate); 939791-38-5 (besylate); 717907-75-0 (free base);

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    Molecular Weight (MW)507.49
    FormulaC21H20F3N7O3S
    CAS No.717907-75-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: >25.4mg/mL
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O
    SynonymsPF562271; PF-562271; PF562,271; PF562,271; PF-562,271; PF-00562271; PF00562271; PF 00562271; PF271, PF-271, PF 271; PF562271 PhSO3H; PF562271 benzesulfonate salt; PF562271 besylate;

    Chemical Name: N-methyl-N-(3-(((2-((2-oxoindolin-5-yl)amino)-5-(trifluoromethyl)pyrimidin-4-yl)amino)methyl)pyridin-2-yl)methanesulfonamide

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


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    In Vitro

    In vitro activity: PF-562271 shows the selective inhibitory effects on FAK and Pyk2 tyrosine kinase activity with IC50 of 1.5 nM and 14 nM, respectively. And in cell-based assays, the IC50 of PF-562271 is shown to be 5 nM for FAK, which is more selective compared to other kinase targets. In 2 dimensional (2D) cultures, PF-562271 results in a dose-dependent cell proliferation inhibition in FAK WT, FAK−/− and FAK kinase-deficient (KD) cells with IC50 of 3.3 μM, 2.08 μM and 2.01 μM, respectively.


    Kinase Assay: PF-562271 shows the selective inhibitory effects on FAK and Pyk2 tyrosine kinase activity with IC50 of 1.5 nM and 14 nM, respectively. And in cell-based assays, the IC50 of PF-562271 is shown to be 5 nM for FAK, which is more selective compared to other kinase targets. In 2 dimensional (2D) cultures, PF-562271 results in a dose-dependent cell proliferation inhibition in FAK WT, FAK−/− and FAK kinase-deficient (KD) cells with IC50 of 3.3 μM, 2.08 μM and 2.01 μM, respectively.


    Cell Assay: Cells (Squamous cell carcinoma (SCC) are plated for 48 hours before addition of PF-562271. After 3 days cells are fixed by addition of ice cold 25% trichloroacetic acid (TCA) solution prior to staining with Sulforhodamine B (SRB) dye solution. Plates are washed with 1% glacial acetic acid, air-dried and resuspended in 10 mM Tris buffer, pH 10.5 before reading absorbance at 540 nm. Curve fitting and generation of IC50 values is carried out using GraphPad Prism 4 software from six replicates.

    In VivoIn several human s.c. xenograft models, PF-562271 exhibits dose-dependent tumor growth inhibition, and produces maximum tumor inhibition for PC-3M, BT474, BxPc3, and LoVo ranging from 78% to 94% inhibition at doses of 25 to 50 mg/kg twice daily, without weight loss, morbidity, or death. PF-562271 (25 mg/kg by p.o.) leads to a significant decrease in tumor progression in both subcutaneous and bone metastasis PC3M-luc-C6 xenograft models. In a Huh7.5 hepatocellular carcinoma xenograft model, combination therapy of sunitinib and PF-562271 targets angiogenesis and tumor aggressiveness, and produces more significant anti-tumor effect than single agent by blocking tumor growth and impacting the ability of the tumor to recover upon withdrawal of the therapy.
    Animal modelPC-3M, BT474, BxPc3, LoVo, U87MG, H125 and H460 cells are injected s.c. into the right flank of athymic female mice
    Formulation & DosageDissolved in in 5% Gelucire; 100 mg/kg; Oral gavage
    References

    Cancer Res. 2008 Mar 15;68(6):1935-44; Cancer Biol Ther. 2010 Jul 1;10(1):38-43.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    PF-562271

    Efficacy of PF-562,271 in PC3M-luc-C6 subcutaneuous local implant xenograft model: PF-562,271 was administered at 25 mg/kg P.O. BID 5x/wk for two weeks. Cancer Biol Ther. 2010 Jul 1;10(1):38-43.

    PF-562271

    (A) Bioluminescent image time course of a subcutaneously inoculated vehicle control mouse. PF-562,271 was administered at 25 mg/kg P.O. BID 5x/wk for two weeks. (B) Bioluminescent image time course of a subcutaneously inoculated mouse treated with PF-562,271. PF-562,271 was administered at 25 mg/kg P.O. BID 5x/wk for two weeks. Cancer Biol Ther.2010 Jul 1;10(1):38-43.

    PF-562271

    (A) Bioluminescent image time course of an intracardiac inoculated vehicle control mouse. Vehicle was administered P.O. BID 5x/wk for three weeks. (B) Bioluminescent image time course of an intracardiac inoculated treated with PF-562,271. PF-562,271 was administered at 25 mg/kg P.O. BID 5x/wk for three weeks. Cancer Biol Ther. 2010 Jul 1;10(1):38-43.


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