1. Protein Tyrosine Kinase/RTK
  2. Pyk2 FAK
  3. PF-431396

PF-431396 is an orally active dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with IC50 values of 2 nM and 11 nM, respectively.

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

PF-431396 Chemical Structure

PF-431396 Chemical Structure

CAS No. : 717906-29-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 75 In-stock
Solution
10 mM * 1 mL in DMSO USD 75 In-stock
Solid
5 mg USD 67 In-stock
10 mg USD 108 In-stock
50 mg USD 336 In-stock
100 mg USD 540 In-stock
200 mg USD 1020 In-stock
500 mg   Get quote  
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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    PF-431396 purchased from MedChemExpress. Usage Cited in: J Periodontal Res. 2015 Dec;50(6):855-863.  [Abstract]

    PF431396 inhibits the phosphorylation of FAK and Akt.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PF-431396 is an orally active dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with IC50 values of 2 nM and 11 nM, respectively[1][2][3][4].

    IC50 & Target

    IC50: 2 nM (FAK); 11 nM (PYK2)[1].
    Kd: 445 nM (BRD4)[1].

    In Vitro

    PF-431396 has a Kd value of 445 nM for BRD4[2].
    PF-431396 appeares to selectively inhibit BCR-induced tyrosine phosphorylation of Pyk2 and FAK[3].
    PF-431396 (2.5, 5 μM, 45 min) inhibits the phosphorylation of Pyk2 and FAK induced by clustering LFA-1 with plate-bound Abs[3].

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

    Western Blot Analysis[3]

    Cell Line: A20 cells ((105 cells in 0.5 ml of RPMI 1640 medium with 2% fetal calf serum and 50 μM 2-mercaptoethanol)).
    Concentration: 0.15, 1, 2.5, 5 μM.
    Incubation Time: 45 min.
    Result: The phosphorylation of Pyk2 and FAK induced by clustering LFA-1 with plate-bound Abs was also inhibited.
    In Vivo

    PF-431396 (10 or 30 mg/kg, orally) prevents bone loss induced by estrogen deficiency in rats primarily by stimulating bone formation, providing independent pharmacological confirmation for the function of PYK2 in regulating bone formation[4].

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

    Animal Model: Sprague–Dawley female rats (ovariectomized (OVX) Rats)[4].
    Dosage: 10 or 30 mg/kg.
    Administration: Oral gavage, for 28 consecutive days.
    Result: Counteracted OVX-induced bone loss, completely preserving total bone content and total bone density.
    Promoted osteoblast recruitment and activity.
    Molecular Weight

    506.50

    Formula

    C22H21F3N6O3S

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (197.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9743 mL 9.8717 mL 19.7433 mL
    5 mM 0.3949 mL 1.9743 mL 3.9487 mL
    View the Complete Stock Solution Preparation Table
    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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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: ≥ 2.5 mg/mL (4.94 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.94 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    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
    References

    Complete Stock Solution Preparation Table

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9743 mL 9.8717 mL 19.7433 mL 49.3583 mL
    5 mM 0.3949 mL 1.9743 mL 3.9487 mL 9.8717 mL
    10 mM 0.1974 mL 0.9872 mL 1.9743 mL 4.9358 mL
    15 mM 0.1316 mL 0.6581 mL 1.3162 mL 3.2906 mL
    20 mM 0.0987 mL 0.4936 mL 0.9872 mL 2.4679 mL
    25 mM 0.0790 mL 0.3949 mL 0.7897 mL 1.9743 mL
    30 mM 0.0658 mL 0.3291 mL 0.6581 mL 1.6453 mL
    40 mM 0.0494 mL 0.2468 mL 0.4936 mL 1.2340 mL
    50 mM 0.0395 mL 0.1974 mL 0.3949 mL 0.9872 mL
    60 mM 0.0329 mL 0.1645 mL 0.3291 mL 0.8226 mL
    80 mM 0.0247 mL 0.1234 mL 0.2468 mL 0.6170 mL
    100 mM 0.0197 mL 0.0987 mL 0.1974 mL 0.4936 mL
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    PF-431396 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.

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    Product Name:
    PF-431396
    Cat. No.:
    HY-10460
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