AG-879

Protein tyrosine kinase (PTK) inhibitors are potential antiproliferative agents for diseases caused by the hyperactivity of PTKs. Tyrphostins are a class of antiproliferative compounds which selectively inhibit PTKs of key growth factors. AG-879 is a tyrphostin compound that inhibits nerve growth factor (NGF)-dependent TrkA tyrosine phosphorylation in PC-12 cells (IC50 = ~40 µM), HER2-ErbB2 kinase in several breast and ovarian cancer cell lines (IC50 = ~0.5 µM), and the VEGF receptor FLK1 (IC50 = ~1 µM). Additionally, AG-879 inhibits the activation of ETK with an IC50 value of ~5 nM, which blocks tyrosine phosphorylation of PAK1, suppressing Ras transformation of NIH 3T3 fibroblasts. AG-879 has also been shown to suppress IL-6-induced tyrosine phosphorylation of STAT3 (IC50 = 15 µM) in schwannoma cells.Formal Name: 3-[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]-2-cyano-2E-propenethioamide. CAS Number: 148741-30-4. Synonyms: Tyrphostin AG-879. Molecular Formula: C18H24N2OS. Formula Weight: 316.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:5): 0.17 mg/ml, Ethanol: 10 mg/ml. lambdamax: 203, 248, 355, 377, 498 nm. SMILES: CC(C)(C)C1=C(O)C(C(C)(C)C)=CC(/C=C(C(N)=S)\C#N)=C1. InChi Code: 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+. InChi Key: XRZYELWZLNAXGE-KPKJPENVSA-N.