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

AZD7545 

Cat. No.: HY-16082 Purity: 99.84%
Handling Instructions

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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 284 In-stock
Estimated Time of Arrival: December 31
5 mg USD 258 In-stock
Estimated Time of Arrival: December 31
10 mg USD 432 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1026 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1596 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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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].

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].

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

SMILES

O=C(N(C)C)C1=CC=C(S(=O)(C2=CC=C(NC([[email protected]@](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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 46 mg/mL (96.06 mM)

*"≥" 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
10 mM 0.2088 mL 1.0441 mL 2.0882 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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AZD7545
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HY-16082
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