Chemical Compound Review:
Nilotinib 4-methyl-N-[3-(4- methylimidazol-1-yl)-5...
Synonyms:
Tasigna, Nilotinib;, SureCN7901, PubChem18272, AMN-107, ...
Dong-Wook Kim,
Dang,
Manley,
F. Giles,
Andreas Hochhaus,
Norbert Gattermann,
van Oosterom,
Debiec-Rychter,
Tefferi,
Ming Zheng,
Jerald P. Radich,
M. Dugan,
Timothy Hughes,
Marco Gobbi,
de Bruijn,
Y. Shou,
J.M. Meyer,
Verstovsek,
Peschel,
P. Rae,
de Boeck,
Jorge Cortes,
Guetens,
Prenen,
A.S. Robeva,
van Oosterom,
Kantarjian,
Jane F. Apperley,
Kazimierz Kuliczkowski,
Giovanni Martinelli,
Philipp le Coutre,
Guetens,
Quint??s-Cardama,
Oliver G. Ottmann,
Michele Baccarani,
Francis Giles,
J.B. Singer,
Duyster,
Huynh,
De Boeck,
Manshouri,
Manley,
Schöffski,
Schoffski,
Cortes,
Giles,
Elisabetta Abruzzese,
Francois-Xavier Mahon,
Hughes,
Quintás-Cardama,
Zannettino,
de Bruijn,
Richard A. Larson,
von Bubnoff,
Giles,
Y. Hsu,
Sanger,
Giuseppe Saglio,
O.G. Ottmann,
Stephen G. O'Brien,
Highley,
Mestan,
Manshouri,
Prenen,
Akin,
Engler,
White,
Cortes,
Manley,
Verstovsek,
Manley,
Kantarjian,
Tefferi,
A. Weitzman,
Saunders,
H.M. Kantarjian,
Yok-Lam Kwong,
Quinn,
Cambareri,
Hagop Kantarjian,
Manley,
Yaping Shou,
Huynh,
- 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)
- 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)
- 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)
- 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)
- 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)
- 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)
- 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)
- 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)
- 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)
- 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)
- 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)
- 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)
- 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)
- 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)
- 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)
- 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)
- 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)
- 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)