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> AZD7545 [252017-04-2]

AZD7545 [252017-04-2]

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Cat# HY-16082-1ml

Size : 10mM/1mL

Brand : MedChemExpress

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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.

AZD7545 Chemical Structure

AZD7545 Chemical Structure

CAS No. : 252017-04-2

This product is a controlled substance and not for sale in your territory.

Based on 1 publication(s) in Google Scholar

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.

252017-04-2
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

  • [1]. Morrell JA, et al. AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2. Biochem Soc Trans. 2003 Dec;31(Pt 6):1168-70.  [Content Brief]

    [2]. Mayers RM, et al. AZD7545, a novel inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2), activates pyruvate dehydrogenase in vivo and improves blood glucose control in obese (fa/fa) Zucker rats. Biochem Soc Trans. 2003 Dec;31(Pt 6):1165-7.  [Content Brief]

    [3]. Cesi G et al. ROS production induced by BRAF inhibitor treatment rewires metabolic processes affecting cell growth of melanoma cells. Mol Cancer. 2017 Jun 8;16(1):102.  [Content Brief]

  • [1]. Morrell JA, et al. AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2. Biochem Soc Trans. 2003 Dec;31(Pt 6):1168-70.

    [2]. Mayers RM, et al. AZD7545, a novel inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2), activates pyruvate dehydrogenase in vivo and improves blood glucose control in obese (fa/fa) Zucker rats. Biochem Soc Trans. 2003 Dec;31(Pt 6):1165-7.

    [3]. Cesi G et al. ROS production induced by BRAF inhibitor treatment rewires metabolic processes affecting cell growth of melanoma cells. Mol Cancer. 2017 Jun 8;16(1):102.

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

Keywords:

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

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