AZD7545


CAS No. : 252017-04-2

252017-04-2
Price and Availability of CAS No. : 252017-04-2
Size Price Stock
5mg $113 In-stock
10mg $170 In-stock
25mg $290 In-stock
50mg $450 In-stock
100mg $620 In-stock
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Cat. No. : HY-16082
M.Wt: 478.87
Formula: C19H18ClF3N2O5S
Purity: >98 %
Solubility: DMSO : ≥ 46 mg/mL
Introduction of 252017-04-2 :

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].
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].

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