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

PF-431396 

Cat. No.: HY-10460 Purity: 98.86%
COA Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 119 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 336 In-stock
Estimated Time of Arrival: December 31
100 mg USD 540 In-stock
Estimated Time of Arrival: December 31
200 mg USD 1020 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   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 MCE. 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].

    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].

    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

    Appearance

    Solid

    Formula

    C22H21F3N6O3S
    CAS No.
    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)

    *"≥" 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
    10 mM 0.1974 mL 0.9872 mL 1.9743 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    *All of the co-solvents are available by MCE.
    Purity & Documentation
    References
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    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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    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    PF-431396717906-29-1PF431396PF 431396Pyk2FAKProline-rich tyrosine kinase 2PTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseInhibitorinhibitorinhibit

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