2. Protein Tyrosine Kinase/RTK
  3. FAK Pyk2
  4. PF-562271 besylate

PF-562271 besylate  (Synonyms: VS-6062 besylate)

Cat. No.: HY-10458 Purity: 99.17%
COA Handling Instructions

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PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively.

For research use only. We do not sell to patients.

PF-562271 besylate Chemical Structure

PF-562271 besylate Chemical Structure

CAS No. : 939791-38-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 232 In-stock
Solution
10 mM * 1 mL in DMSO USD 232 In-stock
Solid
1 mg USD 46 In-stock
5 mg USD 158 In-stock
10 mg USD 198 In-stock
50 mg USD 495 In-stock
100 mg   Get quote  
200 mg   Get quote  

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

Customer Review

Based on 24 publication(s) in Google Scholar

Other Forms of PF-562271 besylate:

PF-562271 besylate Related Antibodies

Top Publications Citing Use of Products

    PF-562271 besylate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2023 Feb 24;14(2):157.  [Abstract]

    PF-562271 (250 nM; 6 h) largely inhibits Akt-S6 phosphorylation in OE-MXRA5 priPC-1 cells.

    PF-562271 besylate purchased from MedChemExpress. Usage Cited in: Int J Cancer. 2015 Oct 1;137(7):1549-59.  [Abstract]

    786-O (a) and Caki-1 (b) are treated for 24 and 48h with increasing concentrations of PF-562,271 and adherent cells were counted. Cell lysates are evaluated through immunoblotting for total FAK following treatment for 24h.

    PF-562271 besylate purchased from MedChemExpress. Usage Cited in: Practical Oncology Journal. 2015, 29(5): 444-449.

    Effects and mechanism of Biglycan and FAK signaling pathway on the invasion and metastasis of colon cancer cells.

    PF-562271 besylate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2013 May 1;73(9):2873-83.  [Abstract]

    FAK inhibition downregulates the AKT/mTOR pathway and CAS activity. A, protein levels measured by Western immunoblotting for AKT/mTOR pathway proteins in A673 and TC32 cells serum-starved overnight, treated with PF-562271 for 6 hours, and then stimulated with IGF-1 for 2 hours. Vinculin is used as the loading control. B, Western immunoblots showing downregulation of phospho-CAS but not phospho-ERK in A673 and TC32 cells after treatment with PF-562271.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively[1].

    IC50 & Target

    IC50: 1.5 nM (FAK), 13 nM (Pyk2), 30 nM (CDK2), 47 nM (CDK3), 58 nM (CDK1), 97 nM (CDK7), 97 nM (Flt3)[1]
    In Vitro

    PF-562271 (VS-6062) besylate is a 30- to 120-nM (15.2 to 60.1 ng/mL) inhibitor of cdk2/E, cdk5/p35, cdk1/B, and cdk3/E in recombinant enzyme assays[1]. PF-562,271 blocks bFGF-stimulated blood vessel angiogenesis as performed in chicken chorioallantoic membrane assays[2]. Treatment of cells with PF-562,271 or knock-down of FAK by siRNA is observed to increase cell-cell adhesion strength[3].

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

    PF-562271 besylate Related Antibodies
    In Vivo

    PF-562,271 (33 mg/kg, p.o.) inhibits FAK phosphorylation in tumors in a dose- and time-dependent manner in tumor-bearing mice. FAK phosphorylation inhibition relative to total blood concentration of PF-562,271 results in a calculated EC50 of 93 ng/mL. PF-562,271 (25 mg/kg, p.o.) induces apoptosis 2-fold greater in treated tumors compared with vehicle-treated control tumors on day 3[1]. PF-562,271 (33 mg/kg, p.o.) and dasatinib extensively inhibit the movement of tumor cells in the animals. Inhibition of FAK kinase activity following treatment with PF-562,271 results in altered E-cadherin dynamics in vivo[3].

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

    665.66

    Formula

    C27H26F3N7O6S2
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    CS(=O)(N(C)C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)=O.O=S(C5=CC=CC=C5)(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 21.4 mg/mL (32.15 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5023 mL 7.5113 mL 15.0227 mL
    5 mM 0.3005 mL 1.5023 mL 3.0045 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
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    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

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    Volume (start)

    V1

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    C2

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    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.67 mg/mL (2.51 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
    • Protocol 2

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

      Solubility: ≥ 1.67 mg/mL (2.51 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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.
    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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: 99.17%

    COA (254 KB) HNMR (209 KB) LCMS (252 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    Briefly, purified-activated FAK kinase domain (amino acid 410-689) is reacted with 50 μM ATP and 10 μg per well of a random peptide polymer of Glu and Tyr, p(Glu/Tyr), in kinase buffer [50 mM HEPES (pH 7.5), 125 mM NaCl, and 48 mM MgCl2] for 15 min. Phosphorylation of p(Glu/Tyr) is challenged with serially diluted compound at 1/2-Log concentrations starting at a top concentration of 1 μM. Each concentration is tested in triplicate. Phosphorylation of p(Glu/Tyr) is detected with a general antiphospho-tyrosine (PY20) antibody followed by horseradish peroxidase (HRP)-conjugated goat anti-mouse IgG antibody. HRP substrate is added, and absorbance readings at 450 nm are obtained after addition of stop solution (2mol/LH2SO4). IC50 values are determined using the Hill-Slope Model.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Exponentially growing cells are trypsinized and resuspended in sterile PBS and inoculated s.c. (1×106 cells per mouse in 200 μL) into the right flank of mice. Animals bearing tumors of appr 150 mm3 in size are divided into groups receiving either vehicle (5% Gelucire) or PF-562,271 (diluted in vehicle), and dosed by p.o. gavage. Animal body weight and tumor measurements are obtained every 2 d. Tumor volume (mm3) is measured with Vernier calipers and calculated. For all tumor growth inhibition experiments, 8 to 10 mice per dose group are used.

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.5023 mL 7.5113 mL 15.0227 mL 37.5567 mL
    5 mM 0.3005 mL 1.5023 mL 3.0045 mL 7.5113 mL
    10 mM 0.1502 mL 0.7511 mL 1.5023 mL 3.7557 mL
    15 mM 0.1002 mL 0.5008 mL 1.0015 mL 2.5038 mL
    20 mM 0.0751 mL 0.3756 mL 0.7511 mL 1.8778 mL
    25 mM 0.0601 mL 0.3005 mL 0.6009 mL 1.5023 mL
    30 mM 0.0501 mL 0.2504 mL 0.5008 mL 1.2519 mL
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    PF-562271 besylate 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-562271 besylate939791-38-5VS-6062 besylateFAKPyk2PTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseProline-rich tyrosine kinase 2Inhibitorinhibitorinhibit

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