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CAS No. : 252017-04-2
|Size||Stock||Price||Quantity||Add to Cart||Quotation Online|
|5mg||In-stock||USD 128.0 128.0|
|10mg||In-stock||USD 190.0 190.0|
|50mg||In-stock||USD 670.0 670.0|
|100mg||In-stock||USD 1030.0 1030.0|
|Cat. No. :||CS-1740|
|CAS No. :||252017-04-2|
|M. Wt. :||478.87|
|Solubility:||DMSO : ≥ 46 mg/mL|
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.
IC50 & Target: IC50: 6.4 nM (PDHK2), 36.8 nM (PDHK1)
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.
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.
Protocol:nimal administration  AZD7545 is given orally to Wistar rats and 3 h later tissues are removed to assay for PDH activity. Total PDH activity is measured following incubation of extracts with PDH phosphatase and bivalent cations and PDH activity is expressed as a percentage of the total activity. Fasted rats are deprived of food for 14 h prior to administration of the compound. Results are means±S.E.M. from six animals. *, ** and *** indicate significant differences (P<0.05, P<0.01, P<0.001 respectively) from the corresponding values for control animals.
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.
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.
Morrell JA, et al. AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2. Biochem Soc Trans. 2003 Dec;31(Pt 6):1168-70.
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