Tyrphostin AG 879

• CAT Number: I001825
• CAS Number: 148741-30-4
• Molecular Formula: C18H24N2OS
• Molecular Weight: 316.5
• Purity: ≥95%
• Target: HER2
• Solubility: DMSO ≥ 36 mg/mL
• Storage: 3 years -20C powder
• InChI: InChI=1S/C18H24N2OS/c1-17(2,3)13-8-11(7-12(10-19)16(20)22)9-14(15(13)21)18(4,5)6/h7-9,21H,1-6H3,(H2,20,22)/b12-7+
• InChIKey: XRZYELWZLNAXGE-KPKJPENVSA-N
• SMILES: CC(C)(C)C1=C(O)C(C(C)(C)C)=CC(/C=C(C(N)=S)C#N)=C1

TyrphostinAG879 (Cat.No:I001825) is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation, but not TrKB and TrKC.[1] also a ErbB2 kinase inhibitor, has at least 500-fold higher selectivity to ErbB2 (IC50 = 1 μmol/L) than EGFR (IC50 >500 μmol/L).

Reference

1:Cell Mol Life Sci. 2004 Oct;61(19-20):2624-31. Novel actions of tyrphostin AG 879: inhibition of RAF-1 and HER-2 expression combined with strong antitumoral effects on breast cancer cells.Larsson LI, PMID: 15526167 DOI: 10.1007/s00018-004-4279-5 Abstract: Binding of growth factors to cell surface receptors activates protein tyrosine kinases (PTKs) that initiate cascades of downstream signaling events including the mitogen-activated protein (MAP) kinase cascade. This study reports that the PTK inhibitor AG 879 inhibits proliferation of human breast cancer cells through an effect involving inhibition of MAP kinase activation, but which cannot be explained by effects of AG 879 on its known PTK targets. Instead, AG 879 markedly inhibits expression of the RAF-1 gene, which encodes an upstream MAP kinase kinase kinase. Additionally, expression of HER-2, but not of other genes tested, is inhibited by this compound. These novel effects have to be considered when using AG 879 as a TRK-A and HER-2 inhibitor but may have useful therapeutic implications.