2. Protein Tyrosine Kinase/RTK Apoptosis
  3. FAK Apoptosis
  4. PF-573228

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 59 In-stock
Solution
10 mM * 1 mL in DMSO USD 59 In-stock
Solid
5 mg USD 55 In-stock
10 mg USD 88 In-stock
50 mg USD 275 In-stock
100 mg USD 440 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 20 publication(s) in Google Scholar

PF-573228 Related Antibodies

Top Publications Citing Use of Products

    PF-573228 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2020 Jun 17;7(15):1903583.  [Abstract]

    Expression of CTC cluster-related (plakoglobin and CD44) and EMT-related (vimentin and E-cadherin, 4 days) proteins in LNCaP cells grown on different substrates after treatment with different inhibitors (Cytoskeleton B (CB), Nocodazole (NO), PF-573288 (PF), Y-27632 (Y), and (-)-Blebbistatin ((-) Bl)).

    PF-573228 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2020 Jun 17;7(15):1903583.  [Abstract]

    Immunofluorescence imaging of LNCaP cells treated with the Cytoskeleton B (CB), Nocodazole (NO), PF-573288 (PF), Y-27632 (Y), and (-)-Blebbistatin ((-) Bl). After the cells are cultured on different substrates for 3 days, inhibitors are added and incubated for 24 h.

    PF-573228 purchased from MedChemExpress. Usage Cited in: Cell Adh Migr. 2017 Jul 4;11(4):327-337.  [Abstract]

    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.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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 value of 4 nM[1].
    PF-573228 inhibits FAK phosphorylation on Tyr397 with an IC50 value of 30-100 nM[1].
    PF-573228 significantly decreased FAK Tyr397 phosphorylation[1].
    PF-573228 inhibits both chemotactic and haptotactic migration concomitant with the inhibition of focal adhesion turnover[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    PF-573228 Related Antibodies
    Molecular Weight

    491.49

    Formula

    C22H20F3N5O3S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C1NC2=C(C=C(NC3=NC=C(C(F)(F)F)C(NCC4=CC=CC(S(=O)(C)=O)=C4)=N3)C=C2)CC1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 25 mg/mL (50.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.09 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.23 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.66%

    COA (247 KB) HNMR (289 KB) LCMS (118 KB)

    Handling Instructions (2659 KB)
    References
    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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0346 mL 10.1731 mL 20.3463 mL 50.8657 mL
    5 mM 0.4069 mL 2.0346 mL 4.0693 mL 10.1731 mL
    10 mM 0.2035 mL 1.0173 mL 2.0346 mL 5.0866 mL
    15 mM 0.1356 mL 0.6782 mL 1.3564 mL 3.3910 mL
    20 mM 0.1017 mL 0.5087 mL 1.0173 mL 2.5433 mL
    25 mM 0.0814 mL 0.4069 mL 0.8139 mL 2.0346 mL
    30 mM 0.0678 mL 0.3391 mL 0.6782 mL 1.6955 mL
    40 mM 0.0509 mL 0.2543 mL 0.5087 mL 1.2716 mL
    50 mM 0.0407 mL 0.2035 mL 0.4069 mL 1.0173 mL
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    PF-573228 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    PF-573228869288-64-2PF573228PF 573228FAKApoptosisPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseInhibitorinhibitorinhibit

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