AZD7545 [252017-04-2]
Cat# HY-16082-1ml
Size : 10mM/1mL
Brand : MedChemExpress
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
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] |
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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. Cell Proliferation Assay[2]
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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.
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Molecular Weight |
478.87 |
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Formula |
C19H18ClF3N2O5S |
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CAS No. |
252017-04-2 |
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Appearance |
Solid |
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Color |
White to off-white |
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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 |
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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
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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
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 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:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume 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
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.
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Purity & Documentation |
Purity: 99.81% |
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References |
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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 |
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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 |
AZD7545 Related Classifications
- Metabolic Enzyme/Protease
- PDHK