1. Protein Tyrosine Kinase/RTK
  2. FAK

PF-573228 

Cat. No.: HY-10461 Purity: 98.72%
Data Sheet SDS Handling Instructions

PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK.

For research use only. We do not sell to patients.
PF-573228 Chemical Structure

PF-573228 Chemical Structure

CAS No. : 869288-64-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 134 In-stock
10 mg USD 122 In-stock
50 mg USD 479 In-stock
100 mg USD 900 In-stock
200 mg   Get quote  
500 mg   Get quote  

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    PF-573228 purchased from MCE. Usage Cited in: Cell Adh Migr. 2016 Sep 2:1-11.

    BAC1.2F5 cells are cultured in the absence of CSF-1 for 18 hours and then kept in suspension for 45 minutes and lysed (0) or plated on FN-coated dishes (10 mg/mL) for 30 minutes in the presence or the absence of PF-573228 (1 mM) before lysis. Proteins are subjected to immunoblotting with the indicated antibodies.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    PF-573228 is a potent and selective FAK inhibitor with IC50 of 4 nM for purified recombinant catalytic fragment of FAK.

    IC50 & Target

    IC50: 4 nM (FAK)[1]

    In Vitro

    PF-573228 inhibits purified recombinant catalytic fragment of FAK with an IC50 of 4 nM. In cultured cells, PF-573228 inhibits FAK phosphorylation on Tyr397 with an IC50 of 30-100 nM. Treatment of cells with concentrations of PF-573228 that significantly decreased FAK Tyr397 phosphorylation fails to inhibit cell growth or induce apoptosis. In contrast, treatment with PF-573228 inhibits both chemotactic and haptotactic migration concomitant with the inhibition of focal adhesion turnover[1].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.0346 mL 10.1731 mL 20.3463 mL
    5 mM 0.4069 mL 2.0346 mL 4.0693 mL
    10 mM 0.2035 mL 1.0173 mL 2.0346 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    Purified activated FAK kinase domain 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 for 15 min. Phosphorylation of poly(Glu/Tyr) is challenged with s MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    REF52 or PC3 cells are seeded into a 24-well plate in triplicate 24 h prior to daily treatment with the indicated concentrations of each inhibitor (PF-573228) for 3 days. Subsequently, the cells are harvested and counted. Apoptosis assays are performed using a cell death detection ELISA. REF52, PC3 or MDCKcells are treated for 24 h (16 h for MDCK) with the indicated concentrations of each inhibitor prior to lysis. Cells suspended for 16-24 h in serum-free medium served as a positive control. The cell lysates are incubated in duplicate in the ELISA system. The data represent the means±standard deviation of one of three experiments performed in duplicate[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    491.49

    Formula

    C₂₂H₂₀F₃N₅O₃S

    CAS No.

    869288-64-2

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 51 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Inquiry Information

    Product Name:
    PF-573228
    Cat. No.:
    HY-10461
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