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

PF-431396 

Cat. No.: HY-10460 Purity: 99.15%
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 Stock
10 mM * 1  mL in DMSO Get quote
10 mg USD 108 Get quote
50 mg USD 336 Get quote
100 mg USD 540 Get quote
200 mg USD 1020 Get quote

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Top Publications Citing Use of Products

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

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

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    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].

    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].

    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.

    717906-29-1

    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
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    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 provided by MCE.
    References
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    Keywords:

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

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