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

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

Cat. No.: HY-20403 Purity: 98.10%
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PF-562271 (VS-6062) hydrochloride is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively.

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

PF-562271 hydrochloride

PF-562271 hydrochloride Chemical Structure

CAS No. : 939791-41-0

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Customer Review

Based on 29 publication(s) in Google Scholar

Other Forms of PF-562271 hydrochloride:

PF-562271 hydrochloride Related Antibodies

Top Publications Citing Use of Products

    PF-562271 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PF-562271 (VS-6062) hydrochloride is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s 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) hydrochloride is shown to be a 30- to 120-nM inhibitor of CDK2/E, CDK5/p35, CDK1/B, and CDK3/E in recombinant enzyme assays, in cell-based assays evaluating the role of CDKs, a 48-hour exposure of 3.3 μM PF-562271 is required to alter cell cycle progression. PF-562271 is potent in an inducible cell-based assay measuring phospho-FAK with a IC50 of 5 nM[1].
    PF-562271, a selective inhibitor of both FAK and proline-rich tyrosine kinase 2 (PYK2), a FAK-related family member, on cell growth and colony formation in Ewing sarcoma cell lines. Seven cell lines are treated for 5 days with PF-562271 across a range of concentrations using 2-fold serial dilutions. Treatment with PF-562271 impaires cell viability in all cell lines, with an average IC50 of 2.4 μM after 3 days of treatment. TC32 and A673 are the 2 most sensitive cell lines, with IC50 concentrations of 2.1 and 1.7 μM, respectively[2].

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

    PF-562271 hydrochloride Related Antibodies
    In Vivo

    PF-562271 inhibits FAK phosphorylation in vivo in a dose-dependent fashion (calculated EC50 of 93 ng/mL, total) after p.o. administration to tumor-bearing mice[1]. Rats that receive PF-562271 demonstrate a decrease in tumor growth after 2 weeks of treatment with signs of bone healing as evidenced by the deposition of new bone (cortical and cancellous) at sites previously damaged by the tumor[3].

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

    543.95

    Formula

    C21H21ClF3N7O3S
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CS(=O)(N(C1=NC=CC=C1CNC2=NC(NC3=CC4=C(NC(C4)=O)C=C3)=NC=C2C(F)(F)F)C)=O.[H]Cl
    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 : 100 mg/mL (183.84 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 1.8384 mL 9.1920 mL 18.3840 mL
    5 mM 0.3677 mL 1.8384 mL 3.6768 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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

    Dosage

    mg/kg

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    (per animal)

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    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation
    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 1.8384 mL 9.1920 mL 18.3840 mL 45.9601 mL
    5 mM 0.3677 mL 1.8384 mL 3.6768 mL 9.1920 mL
    10 mM 0.1838 mL 0.9192 mL 1.8384 mL 4.5960 mL
    15 mM 0.1226 mL 0.6128 mL 1.2256 mL 3.0640 mL
    20 mM 0.0919 mL 0.4596 mL 0.9192 mL 2.2980 mL
    25 mM 0.0735 mL 0.3677 mL 0.7354 mL 1.8384 mL
    30 mM 0.0613 mL 0.3064 mL 0.6128 mL 1.5320 mL
    40 mM 0.0460 mL 0.2298 mL 0.4596 mL 1.1490 mL
    50 mM 0.0368 mL 0.1838 mL 0.3677 mL 0.9192 mL
    60 mM 0.0306 mL 0.1532 mL 0.3064 mL 0.7660 mL
    80 mM 0.0230 mL 0.1149 mL 0.2298 mL 0.5745 mL
    100 mM 0.0184 mL 0.0919 mL 0.1838 mL 0.4596 mL
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    PF-562271 hydrochloride 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-562271939791-41-0VS-6062(hydrochloride)PF562271PF 562271FAKPyk2PTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseProline-rich tyrosine kinase 2AntitumorEwingSarcomaBreastCancerInhibitorinhibitorinhibit

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