2. Metabolic Enzyme/Protease
  3. PDHK
  4. AZD7545

AZD7545 is a potent, competitive, selective PDHK2 (pyruvate dehydrogenase kinase 2) inhibitor with IC50s of 36.8 nM, 6.4 nM for PDHK1 and PDHK2, respectively.

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

CAS No. : 252017-04-2

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Customer Review

Based on 4 publication(s) in Google Scholar

AZD7545 Related Antibodies

Top Publications Citing Use of Products

    AZD7545 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Dec 23;23(1):1412.  [Abstract]

    CCK-8 assay revealed decreased cell viability under high lactate conditions after AZD7545 (AZD) (10 μM) treatment.

    AZD7545 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Dec 23;23(1):1412.  [Abstract]

    Western blot showed reduced protein expression of target genes after AZD7545 (AZD) (10 μM) treatment.

    AZD7545 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Dec 23;23(1):1412.  [Abstract]

    ELISA showed reduced protein expression of target genes after AZD7545 (AZD) (10 μM) treatment.

    AZD7545 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Dec 23;23(1):1412.  [Abstract]

    qPCR confirmed decreased mRNA levels of PDK1 and inflammatory factors after AZD7545 (AZD) (10 μM) treatment.

    AZD7545 purchased from MedChemExpress. Usage Cited in: J Transl Med. 2025 Dec 23;23(1):1412.  [Abstract]

    Mitochondrial morphology alterations were observed by MitoTracker staining after AZD7545 (AZD) (10 μM) treatment.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AZD7545 is a potent, competitive, selective PDHK2 (pyruvate dehydrogenase kinase 2) inhibitor with IC50s of 36.8 nM, 6.4 nM for PDHK1 and PDHK2, respectively[1].

    IC50 & Target

    IC50: 6.4 nM (PDHK2), 36.8 nM (PDHK1)[1]
    In Vitro

    AZD7545 (10 μM; 90 hours for BRAFV600E human melanoma cells and 120 hours for NRAS mut human melanoma cells) specifically suppresses growth of cells harboring BRAF and NRAS mutations as well as in inhibitor-resistant human melanoma[2].

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

    AZD7545 Related Antibodies

    Cell Proliferation Assay[2]

    Cell Line: Human melanoma cells lines of BRAFV600E (A375, IGR37) and NRASmut (SKMel30, IPC298, MelJuso)
    Concentration: 10 μM
    Incubation Time: 90 hours (BRAFV600E human melanoma cells) and 120 hours (NRAS mut human melanoma cells)
    Result: Mediated growth suppression of BRAFV600E mutant and NRAS mut human melanoma cells.
    In Vivo

    A single dose of AZD7545 (Oral administration; 10 mg/kg once a day (08:00 h) or Twice a day (08:00 and 18:00 h); for 7 days) to Wistar rats increases the proportion of liver PDH in its active, dephosphorylated form in a dose-related manner. A single dose of 10 mg/kg also significantly elevates muscle PDH activity in obese Zucker (fa/fa) rats[3].

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

    Animal Model: Obese male (fa/fa) Zucker rats [3]
    Dosage: 10 mg/kg
    Administration: Oral administration; once a day (08:00 h) or Twice a day ( 08:00 and 18:00 h); for 7 days
    Result: Improved the control of blood glucose levels.
    Molecular Weight

    478.87

    Formula

    C19H18ClF3N2O5S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N(C)C)C1=CC=C(S(=O)(C2=CC=C(NC([C@@](C)(O)C(F)(F)F)=O)C(Cl)=C2)=O)C=C1
    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 : ≥ 46 mg/mL (96.06 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 2.0882 mL 10.4412 mL 20.8825 mL
    5 mM 0.4176 mL 2.0882 mL 4.1765 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)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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 (5.22 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.22 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    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
    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 2.0882 mL 10.4412 mL 20.8825 mL 52.2062 mL
    5 mM 0.4176 mL 2.0882 mL 4.1765 mL 10.4412 mL
    10 mM 0.2088 mL 1.0441 mL 2.0882 mL 5.2206 mL
    15 mM 0.1392 mL 0.6961 mL 1.3922 mL 3.4804 mL
    20 mM 0.1044 mL 0.5221 mL 1.0441 mL 2.6103 mL
    25 mM 0.0835 mL 0.4176 mL 0.8353 mL 2.0882 mL
    30 mM 0.0696 mL 0.3480 mL 0.6961 mL 1.7402 mL
    40 mM 0.0522 mL 0.2610 mL 0.5221 mL 1.3052 mL
    50 mM 0.0418 mL 0.2088 mL 0.4176 mL 1.0441 mL
    60 mM 0.0348 mL 0.1740 mL 0.3480 mL 0.8701 mL
    80 mM 0.0261 mL 0.1305 mL 0.2610 mL 0.6526 mL
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    AZD7545 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:

    AZD7545252017-04-2AZD 7545AZD-7545PDHKPyruvate dehydrogenase kinasePDH kinaseInhibitorinhibitorinhibit

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