AZD7545

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AZD7545

CAS No. : 252017-04-2

MCE 国际站：AZD7545

产品活性：AZD7545 是一种有效，竞争性和选择性的 PDHK2 抑制剂，对 PDHK1 和 PDHK2 的 IC₅₀ 分别为 36.8 nM 和 6.4 nM。

研究领域：Metabolic Enzyme/Protease

作用靶点：PDHK

In Vitro: AZD7545 (10 μM; 90 hours for BRAF^V600E 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.

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.

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