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    PF-573228
    PF-573228

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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 #: V0658
    CAS #: 869288-64-2Purity ≥98%

    Description: PF-573228 (PF573228) is a selective and ATP-competitive FAK (focal adhesion kinase) inhibitor with potential antitumor activity. It inhibits FAK with an IC50 of 4 nM in a cell-free assay, and is ~50- to 250-fold more selective for FAK over other kinases including Pyk2, CDK1/7 and GSK-3β. PF-573228 shows high in vivo antitumor efficacy in PC3M-luc-C6 xenograft models. FAK is a non-receptor protein-tyrosine kinase that regulates integrin and growth factor signaling pathways involved in cell migration, proliferation, and survival. FAK is over expressed in many cancers, including breast and prostate cancer. 

    References: J Biol Chem. 2007 May 18;282(20):14845-52.


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    Molecular Weight (MW)491.49
    FormulaC22H20F3N5O3S
    CAS No.869288-64-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 26 mg/mL (52.9 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
    Synonyms

    PF573,228; PF 573,228; PF-573,228; PF573228; PF 573228; PF-573228;

    Chemical Name: 3,4-Dihydro-6-[[4-[[[3-(methylsulfonyl)phenyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]-2(1H)-quinolinone 


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    In Vitro

    In vitro activity: PF 573228 blocks the phosphorylation of FAK Tyr397 in REF52 cells, PC3 cells, SKOV-3 cells, L3.6p1 and F-G, MDCK cells with IC50 of 30-500 nM. However, PF 573228 (1 μM) with 80% inhibition of FAK phosphorylation fails to inhibit cell growth or apoptosis. Similar treatment of cells with PF-228 resulted in inhibition of serum or FN-directed migration and decreased focal adhesion turnover.


    Kinase Assay: Purified activated FAK kinase domain (amino acids 410–689) is reacted with 50 μM ATP, and 10 μg/well of a random peptide polymer of Glu and Tyr (molar ratio of 4:1), poly(Glu/Tyr) in kinase buffer (50 mM HEPES, pH 7.5, 125 mM NaCl, 48 mM MgCl2) for 15 min. Phosphorylation of poly(Glu/Tyr) is challenged with serially diluted compounds at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is run in triplicate. Phosphorylation of poly(Glu/Tyr) is detected with a general anti-phospho-tyrosine (PY20) antibody, followed by horseradish peroxidase-conjugated goat anti-mouse IgG antibody. The standard horseradish peroxidase substrate 3, 3', 5, 5'-tetramethylbenzidine is added, and Optical Density readings at 450 nm are obtained following the addition of stop solution (2 M H2SO4). The IC50 values are determined using the Hill slope model.


    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 modelPC3M-luc-C6 xenograft models
    Formulation & Dosage25 mg/kg; Oral gavage
    References

    J Biol Chem. 2007 May 18;282(20):14845-52.


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

    PF-573228

    Inhibition of cellular FAK Tyr397 phosphorylation by PF-228. J Biol Chem. 2007 May 18;282(20):14845-52. 

    PF-573228

    The effects of PF-228 on adhesion-dependent FAK activation. J Biol Chem. 2007 May 18;282(20):14845-52. 

    PF-573228

    Effect of PF-228 on focal adhesion turnover. J Biol Chem. 2007 May 18;282(20):14845-52.  


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