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Chemical Compound Review

Nilotinib     4-methyl-N-[3-(4- methylimidazol-1-yl)-5...

Synonyms: Tasigna, Nilotinib;, SureCN7901, PubChem18272, AMN-107, ...
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Disease relevance of AMN107


High impact information on AMN107


Biological context of AMN107


Anatomical context of AMN107

  • We show that the novel TK-targeting drugs PKC412 and AMN107 counteract TK activity of D816V KIT and inhibit the growth of Ba/F3 cells with doxycycline-inducible expression of KIT D816V as well as the growth of primary neoplastic mast cells and HMC-1 cells harboring this KIT mutation [4].
  • In an in vivo bone marrow transplantation assay, AMN107 effectively treated myeloproliferative disease induced by TEL-PDGFRbeta and FIP1L1-PDGFRalpha, significantly increasing survival and disease latency and reducing disease severity as assessed by histopathology and flow cytometry [6].
  • The effects of AMN107 were compared with those of imatinib on imatinib-sensitive (KBM5 and KBM7) and imatinib-resistant CML cell lines (KBM5-STI571R1.0 and KBM7-STI571R1.0) [10].

Associations of AMN107 with other chemical compounds


Gene context of AMN107


Analytical, diagnostic and therapeutic context of AMN107

  • In this review, the early characterisation and development of AMN107 is discussed, as is the current status of AMN107 in clinical trials for imatinib-resistant CML and Ph+ ALL [17].
  • Simultaneous determination of AMN107 and Imatinib (Gleevec((R)), Glivec((R)), STI571) in cultured tumour cells using an isocratic high-performance liquid chromatography procedure with UV detection [18].
  • A reversed phase high-performance liquid chromatographic (HPLC) method with UV detection was developed for the simultaneous determination of imatinib (Gleevec((R)), Glivec((R)), STI571) and AMN107 in cultured tumour cells, using clozapine as an internal standard [18].


  1. Dasatinib (BMS-354825) is active in Philadelphia chromosome-positive chronic myelogenous leukemia after imatinib and nilotinib (AMN107) therapy failure. Quintas-Cardama, A., Kantarjian, H., Jones, D., Nicaise, C., O'brien, S., Giles, F., Talpaz, M., Cortes, J. Blood (2007) [Pubmed]
  2. Inhibition of PDGF, TGF-β, and Abl signaling and reduction of liver fibrosis by the small molecule Bcr-Abl tyrosine kinase antagonist Nilotinib. Liu, Y., Wang, Z., Kwong, S.Q., Lui, E.L., Friedman, S.L., Li, F.R., Lam, R.W., Zhang, G.C., Zhang, H., Ye, T. J. Hepatol. (2011) [Pubmed]
  3. Combined effects of novel tyrosine kinase inhibitor AMN107 and histone deacetylase inhibitor LBH589 against Bcr-Abl-expressing human leukemia cells. Fiskus, W., Pranpat, M., Bali, P., Balasis, M., Kumaraswamy, S., Boyapalle, S., Rocha, K., Wu, J., Giles, F., Manley, P.W., Atadja, P., Bhalla, K. Blood (2006) [Pubmed]
  4. PKC412 inhibits in vitro growth of neoplastic human mast cells expressing the D816V-mutated variant of KIT: comparison with AMN107, imatinib, and cladribine (2CdA) and evaluation of cooperative drug effects. Gleixner, K.V., Mayerhofer, M., Aichberger, K.J., Derdak, S., Sonneck, K., Böhm, A., Gruze, A., Samorapoompichit, P., Manley, P.W., Fabbro, D., Pickl, W.F., Sillaber, C., Valent, P. Blood (2006) [Pubmed]
  5. OCT-1-mediated influx is a key determinant of the intracellular uptake of imatinib but not nilotinib (AMN107): reduced OCT-1 activity is the cause of low in vitro sensitivity to imatinib. White, D.L., Saunders, V.A., Dang, P., Engler, J., Zannettino, A.C., Cambareri, A.C., Quinn, S.R., Manley, P.W., Hughes, T.P. Blood (2006) [Pubmed]
  6. The small molecule tyrosine kinase inhibitor AMN107 inhibits TEL-PDGFRbeta and FIP1L1-PDGFRalpha in vitro and in vivo. Stover, E.H., Chen, J., Lee, B.H., Cools, J., McDowell, E., Adelsperger, J., Cullen, D., Coburn, A., Moore, S.A., Okabe, R., Fabbro, D., Manley, P.W., Griffin, J.D., Gilliland, D.G. Blood (2005) [Pubmed]
  7. Bcr-Abl resistance screening predicts a limited spectrum of point mutations to be associated with clinical resistance to the Abl kinase inhibitor nilotinib (AMN107). von Bubnoff, N., Manley, P.W., Mestan, J., Sanger, J., Peschel, C., Duyster, J. Blood (2006) [Pubmed]
  8. Comparison of imatinib mesylate, dasatinib (BMS-354825), and nilotinib (AMN107) in an N-ethyl-N-nitrosourea (ENU)-based mutagenesis screen: high efficacy of drug combinations. Bradeen, H.A., Eide, C.A., O'hare, T., Johnson, K.J., Willis, S.G., Lee, F.Y., Druker, B.J., Deininger, M.W. Blood (2006) [Pubmed]
  9. Activity of AMN107, a novel aminopyrimidine tyrosine kinase inhibitor, against human FIP1L1-PDGFR-alpha-expressing cells. Verstovsek, S., Giles, F.J., Quint??s-Cardama, A., Manshouri, T., Huynh, L., Manley, P., Cortes, J., Tefferi, A., Kantarjian, H. Leuk. Res. (2006) [Pubmed]
  10. AMN107, a novel aminopyrimidine inhibitor of Bcr-Abl, has in vitro activity against imatinib-resistant chronic myeloid leukemia. Golemovic, M., Verstovsek, S., Giles, F., Cortes, J., Manshouri, T., Manley, P.W., Mestan, J., Dugan, M., Alland, L., Griffin, J.D., Arlinghaus, R.B., Sun, T., Kantarjian, H., Beran, M. Clin. Cancer Res. (2005) [Pubmed]
  11. Nilotinib (formerly AMN107), a highly selective BCR-ABL tyrosine kinase inhibitor, is active in patients with imatinib-resistant or -intolerant accelerated-phase chronic myelogenous leukemia. le Coutre, P., Ottmann, O.G., Giles, F., Kim, D.W., Cortes, J., Gattermann, N., Apperley, J.F., Larson, R.A., Abruzzese, E., O'Brien, S.G., Kuliczkowski, K., Hochhaus, A., Mahon, F.X., Saglio, G., Gobbi, M., Kwong, Y.L., Baccarani, M., Hughes, T., Martinelli, G., Radich, J.P., Zheng, M., Shou, Y., Kantarjian, H. Blood (2008) [Pubmed]
  12. Nilotinib hampers the proliferation and function of CD8+ T lymphocytes through inhibition of T cell receptor signalling. Chen, J., Schmitt, A., Chen, B., Rojewski, M., Rübeler, V., Fei, F., Yu, Y., Yu, X., Ringhoffer, M., von Harsdorf, S., Greiner, J., Götzz, M., Guillaume, P., Döhner, H., Bunjes, D., Schmitt, M. J. Cell. Mol. Med. (2008) [Pubmed]
  13. Effects of AMN107, a novel aminopyrimidine tyrosine kinase inhibitor, on human mast cells bearing wild-type or mutated codon 816 c-kit. Verstovsek, S., Akin, C., Manshouri, T., Quintás-Cardama, A., Huynh, L., Manley, P., Tefferi, A., Cortes, J., Giles, F.J., Kantarjian, H. Leuk. Res. (2006) [Pubmed]
  14. Cellular Uptake of the Tyrosine Kinase Inhibitors Imatinib and AMN107 in Gastrointestinal Stromal Tumor Cell Lines. Prenen, H., Guetens, G., de Boeck, G., Debiec-Rychter, M., Manley, P., Schoffski, P., van Oosterom, A.T., de Bruijn, E. Pharmacology (2006) [Pubmed]
  15. AMN107, a novel aminopyrimidine inhibitor of p190 Bcr-Abl activation and of in vitro proliferation of Philadelphia-positive acute lymphoblastic leukemia cells. Verstovsek, S., Golemovic, M., Kantarjian, H., Manshouri, T., Estrov, Z., Manley, P., Sun, T., Arlinghaus, R.B., Alland, L., Dugan, M., Cortes, J., Giles, F., Beran, M. Cancer (2005) [Pubmed]
  16. UGT1A1 promoter polymorphism increases risk of nilotinib-induced hyperbilirubinemia. Singer, J.B., Shou, Y., Giles, F., Kantarjian, H.M., Hsu, Y., Robeva, A.S., Rae, P., Weitzman, A., Meyer, J.M., Dugan, M., Ottmann, O.G. Leukemia (2007) [Pubmed]
  17. AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL. Weisberg, E., Manley, P., Mestan, J., Cowan-Jacob, S., Ray, A., Griffin, J.D. Br. J. Cancer (2006) [Pubmed]
  18. Simultaneous determination of AMN107 and Imatinib (Gleevec((R)), Glivec((R)), STI571) in cultured tumour cells using an isocratic high-performance liquid chromatography procedure with UV detection. Guetens, G., Prenen, H., De Boeck, G., van Oosterom, A., Schöffski, P., Highley, M., de Bruijn, E.A. J. Chromatogr. B Analyt. Technol. Biomed. Life Sci. (2007) [Pubmed]
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