AZD7545 MedChemExpress (MCE)

Product Name	AZD7545
Synonyms	AZD7545;AZD4575;AZD7547;CS-1842;AZD 7547;AZD-7547;4-[[3-Chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl-1-oxopropyl]amino]phenyl]sulfonyl]-N,N-dimethylbenzamide
CAS	252017-04-2
EINECS
Chemical Formula	C19H18ClF3N2O5S
Molecular Weight	478.87
inchi
Package	10 mM * 1 mL;1 mg;5 mg;10 mg;25 mg;50 mg;100 mg
Price	Email to quote
Descriptions	AZD7545 AZD7545 MedChemExpress (MCE) HY-16082 252017-04-2 99.81% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions AZD7545 AZD7545 MedChemExpress (MCE) HY-16082 252017-04-2 99.81% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. 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. 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]. 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]. 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. 0 --> AZD7545 Related Antibodies Cell Proliferation Assay[2] Cell Line: Human melanoma cells lines of BRAFV600E (A375, IGR37) and NRASmut (SKMel30, IPC298, MelJuso) \| \| \| \| \| \| \| \| \| \| [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]
Last Update	2025-04-01 14:45:47

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