2. TGF-beta/Smad
  3. TGF-β Receptor
  4. PF-06952229

PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction.?PF-06952229 is a promising antineoplastic?agent for the study solid tumors, especifically metastatic breast cancer.

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

CAS No. : 1801333-55-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 4 publication(s) in Google Scholar

PF-06952229 Related Antibodies

Top Publications Citing Use of Products

    PF-06952229 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 20;8(1):94.  [Abstract]

    Treatment with four TGF-βR1 inhibitors (LY364947, Vactosertib, PF06952229, and YL-13027; used at 100 μM [++] or 10 μM [+]) for 48 h repressed the p-EMT-like program, as evidenced by decreased ZEB2 and TGFBI protein levels in the UM‑Chor1 cell line.

    PF-06952229 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 20;8(1):94.  [Abstract]

    Treatment with four TGF-βR1 inhibitors (LY364947, Vactosertib, PF06952229, and YL-13027; used at 100 μM [++] or 10 μM [+]) for 48 h repressed the p-EMT-like program, as evidenced by decreased ZEB2 and TGFBI mRNA levels in the UM‑Chor1 cell line.

    PF-06952229 purchased from MedChemExpress. Usage Cited in: Cell Discov. 2022 Sep 20;8(1):94.  [Abstract]

    Treatment with four TGF-βR1 inhibitors (LY364947, Vactosertib, PF06952229, and YL-13027; used at 100 μM [++] or 10 μM [+]) for 48 h attenuated the invasiveness of UM‑Chor1 cells.

    View All TGF-β Receptor Isoform Specific Products:

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    ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PF-06952229 is a potent, selective and orally active TGFbR1 inhibitor. PF-06952229 specifically binds to TGFbR1 and prevents TGFbR1-mediated signal transduction.?PF-06952229 is a promising antineoplastic?agent for the study solid tumors, especifically metastatic breast cancer[1].

    IC50 & Target

    IC50: transforming growth factor-beta receptor 1 (TGFbR1)[1]
    In Vivo

    PF-06952229 (oral gavage; 30 mg/kg; twice daily; 21 days) combines with Palbociclib 21 days results in an improved inhibition of pSMAD2 in the MCF7 ER+?xenograft breast cancer tumor model. This combination also leads to a significant increase in survival relative to PF-06952229 monotherapy[1].

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

    Animal Model: MCF-7 ER+ HER2-xenograft breast cancer tumor model[1]
    Dosage: 30 mg/kg
    Administration: Oral gavage; twice daily; 44 days
    Result: Resulted in an increase in tumor growth inhibition when combined with Palbociclib.
    Clinical Trial
    Molecular Weight

    458.91

    Formula

    C23H24ClFN4O3
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC(CO)CO)C1=CN=CC=C1NC2=CC(C3=CC(Cl)=CC=C3F)=NC=C2C(C)C
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (108.95 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 2.1791 mL 10.8954 mL 21.7908 mL
    5 mM 0.4358 mL 2.1791 mL 4.3582 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 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 (5.45 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: ≥ 2.08 mg/mL (4.53 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

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    Dosing volume
    (per animal)

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    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).
    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: 99.92%

    SDS (251 KB)

    COA (249 KB) LCMS (92 KB)

    Handling Instructions (2659 KB)
    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1791 mL 10.8954 mL 21.7908 mL 54.4769 mL
    5 mM 0.4358 mL 2.1791 mL 4.3582 mL 10.8954 mL
    10 mM 0.2179 mL 1.0895 mL 2.1791 mL 5.4477 mL
    15 mM 0.1453 mL 0.7264 mL 1.4527 mL 3.6318 mL
    20 mM 0.1090 mL 0.5448 mL 1.0895 mL 2.7238 mL
    25 mM 0.0872 mL 0.4358 mL 0.8716 mL 2.1791 mL
    30 mM 0.0726 mL 0.3632 mL 0.7264 mL 1.8159 mL
    40 mM 0.0545 mL 0.2724 mL 0.5448 mL 1.3619 mL
    50 mM 0.0436 mL 0.2179 mL 0.4358 mL 1.0895 mL
    60 mM 0.0363 mL 0.1816 mL 0.3632 mL 0.9079 mL
    80 mM 0.0272 mL 0.1362 mL 0.2724 mL 0.6810 mL
    100 mM 0.0218 mL 0.1090 mL 0.2179 mL 0.5448 mL
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    PF-06952229 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-069522291801333-55-0PF06952229PF 06952229TGF-β ReceptorTransforming growth factor beta receptorsbreastcancerCT26cellsMCF-7SolidtumorsMetastaticdifferentiationapoptosismotilityinvasionangiogenesisInhibitorinhibitorinhibit

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