Formulation: A crystalline solid
Formal Name: 3-[3-[(2-benzothiazolylthio)methyl]-4-hydroxy-5-methoxyphenyl]-2-cyano-2-propenamide
Purity: ≥98%
Formula Markup: C19H15N3O3S2
Formula Weight: 397,5
Shelf life (days): 1460
CAS Number: 149092-50-2
Notes: The HER2/Neu proto-oncogene is a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases (RTK) which includes EGFR, HER2/Neu, HER3 and HER4.{15161} Overexpression of HER2/Neu occurs in 25-30% of human breast and ovarian cancer. AG-825 is a selective ATP-competitive inhibitor of the tyrosine kinase activity of HER2/Neu. In cell-free assays, AG-825 inhibits Her2/Neu, EGFR, and PDGFR autophosphorylation with IC50 values of 0.35, 19, and 40 µM, respectively.{15151} However, in select whole cells, the high concentration of ATP prevents inhibition of kinase activity by AG-825.{15151} Concentrations of 50 µM AG-825, however, consistently inhibit Her2/Neu signalling and promote killing of human LNCaP, C4, and C4-2 prostate cancer cells.{15152}
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