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Chemical Compound Review

Lopac-T-2067     (E)-3-amino-2-[(4-oxo-3,5- ditert-butyl-1...

Synonyms: AC1NUPK6, CHEMBL539947, AG-879, T2067_SIGMA, BMK1-D4, ...
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Disease relevance of AG-879

  • Novel actions of tyrphostin AG 879: inhibition of RAF-1 and HER-2 expression combined with strong antitumoral effects on breast cancer cells [1].
  • However, pretreatment with anti-NGF antibody or TrkA inhibitor AG-879 profoundly raised KA toxicity [2].
  • Furthermore, we and others have demonstrated that the growth of mouse RAS-induced sarcomas allografts in mice is almost completely suppressed by either FK228 or a combination of two complimentary Tyr-kinase inhibitors, PP1 and AG 879, all of which block the RAS-induced activation of PAK1 [3].
  • Since, so far no effective therapeutic is available for the treatment of pancreatic cancer patients, we have examined the therapeutic potential of either FK228, the combination of these two Tyr-kinase inhibitors or GL-2003, a water-soluble derivative of AG 879, on human pancreatic cancer (Capan-1) xenograft in mice [3].

High impact information on AG-879

  • Instead, AG 879 markedly inhibits expression of the RAF-1 gene, which encodes an upstream MAP kinase kinase kinase [1].
  • 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 [1].
  • 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 [1].
  • Inhibition of p140(trkA) receptor by AG-879 prevents extracellular signal-regulated kinase 1/2 phosphorylation and suppresses the increase of SM [4].
  • The specific tyrphostins AG 1478, AG 527 and AG 879 inhibited the RLX-stimulated cAMP response in human ESC and THP-1 cells in a dose-dependent manner, though the potent broad range tyrphostin AG 213 had no effect [5].

Biological context of AG-879

  • Furthermore, KA stimulation resulted in an increase of TrkA expression and phosphorylation, which was blocked not only by the AMPA/KA receptor antagonist 6-cyano-7-nitroquinoxaline-2,3-dione and AG-879, but also by the phospholipase C inhibitor U73122 and the intracellular calcium chelator BAPTA [2].

Associations of AG-879 with other chemical compounds


Gene context of AG-879

  • AG 879, in combination of PP1 (an inhibitor specific for Src kinase family), suppresses almost completely the growth of RAS-induced sarcomas in nude mice [8].


  1. Novel actions of tyrphostin AG 879: inhibition of RAF-1 and HER-2 expression combined with strong antitumoral effects on breast cancer cells. Larsson, L.I. Cell. Mol. Life Sci. (2004) [Pubmed]
  2. Kainic acid-induced neurotrophic activities in developing cortical neurons. Lee, Y.H., Fang, K.M., Yang, C.M., Hwang, H.M., Chiu, C.T., Tsai, W. J. Neurochem. (2000) [Pubmed]
  3. Signal therapy of human pancreatic cancer and NF1-deficient breast cancer xenograft in mice by a combination of PP1 and GL-2003, anti-PAK1 drugs (Tyr-kinase inhibitors). Hirokawa, Y., Levitzki, A., Lessene, G., Baell, J., Xiao, Y., Zhu, H., Maruta, H. Cancer Lett. (2007) [Pubmed]
  4. Nerve growth factor induces sphingomyelin accumulation in pheochromocytoma cells. Piccinotti, A., Benaglia, G., Bresciani, R., Zizioli, D., Presta, M., Preti, A., Marchesini, S. FEBS Lett. (2000) [Pubmed]
  5. Relaxin signalling links tyrosine phosphorylation to phosphodiesterase and adenylyl cyclase activity. Bartsch, O., Bartlick, B., Ivell, R. Mol. Hum. Reprod. (2001) [Pubmed]
  6. Synergistic effects of corticosterone and kainic acid on neurite outgrowth in axotomized dorsal root ganglion. Tsai, S.Y., Chiu, P.Y., Yang, C.P., Lee, Y.H. Neuroscience (2002) [Pubmed]
  7. Epidermal growth factor stimulates 3-hydroxy-3-methylglutaryl-coenzyme A reductase expression via the ErbB-2 pathway in human breast adenocarcinoma cells. Asslan, R., Pradines, A., Pratx, C., Allal, C., Favre, G., Le Gaillard, F. Biochem. Biophys. Res. Commun. (1999) [Pubmed]
  8. The Tyr-kinase inhibitor AG879, that blocks the ETK-PAK1 interaction, suppresses the RAS-induced PAK1 activation and malignant transformation. He, H., Hirokawa, Y., Gazit, A., Yamashita, Y., Mano, H., Kawakami, Y., Kawakami, n.u.l.l., Hsieh, C.Y., Kung, H.J., Lessene, G., Baell, J., Levitzki, A., Maruta, H. Cancer Biol. Ther. (2004) [Pubmed]
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