AG-825

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. 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. However, in select whole cells, the high concentration of ATP prevents inhibition of kinase activity by AG-825. 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.Formal Name: 3-[3-[(2-benzothiazolylthio)methyl]-4-hydroxy-5-methoxyphenyl]-2-cyano-2-propenamide. CAS Number: 149092-50-2. Synonyms: Tyrphostin AG-825. Molecular Formula: C19H15N3O3S2. Formula Weight: 397.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO: PBS (pH 7.2)(1:3): 0.1 mg/ml, Ethanol: 0.2 mg/ml. lambdamax: 225, 361 nm. SMILES: OC(C(OC)=CC(C=C(C#N)C(N)=O)=C1)=C1CSC2=NC3=CC=CC=C3S2. InChi Code: InChI=1S/C19H15N3O3S2/c1-25-15-8-11(6-12(9-20)18(21)24)7-13(17(15)23)10-26-19-22-14-4-2-3-5-16(14)27-19/h2-8,23H,10H2,1H3,(H2,21,24). InChi Key: KXDONFLNGBQLTN-UHFFFAOYSA-N. Origin: Synthetic.