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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 is a novel, potent, selective, and ATP-competitive inhibitor of FAK (focal adhesion kinase) with IC50 of 4 nM in a cell-free assay, it is about 50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β. When tested with HUVEC (primary human umbilical vein endothelial cells), PF573228 treatment increased the proportion of cell apoptosis, reduced the ability of endothelial cell migration and sprout formation via inhibiting the autophosphorylation of FAK. Focal adhesion kinase (FAK) is a member of a family of non-receptor protein-tyrosine kinases that regulates integrin and growth factor signaling pathways involved in cell migration, proliferation, and survival. FAK expression is increased 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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