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Chemical Compound Review

Imatinib     4-[(4-methylpiperazin-1- yl)methyl]-N-[4...

Synonyms: Glamox, CHEMBL941, SureCN3827, QCR-269, sti-571, ...
Jörg H. W. Distler, Bernhard Manger, Bernd M. Spriewald, Oliver Distler, Georg Schett,  Gleich,  Leiferman,  Roeder,  Loeffler,  Horn,  Glauche,  Mueller,  Hochhaus,  Barst, Andreas Hochhaus, Jeffrey H. Lipton, Hagop M. Kantarjian, Michele Baccarani, Martin C. Muller, Dietger Niederwieser, Rana Ezzeddine, Richard T. Silver, Brian J. Druker, Neil P. Shah, Thierry Facon, Jane F. Apperley, Richard M. Stone, Timothy P. Hughes, Athena M. Countouriotis, Francisco Cervantes, Stuart L. Goldberg, Hagop M. Kantarjian, Kapil Bhalla, Ariful Haque, Franck-Emmanuel Nicolini, Mark Litzow, Stephen G. O'Brien, Norbert Gattermann, Aaron Weitzman, Debra J. Resta, Francisco Cervantes, Ravi Bhatia, Francesca Palandri, Giuliana Alimena, Philipp le Coutre, Gert J. Ossenkoppele, Yaping Shou, Francis Giles, Andreas Hochhaus,  Goldstein,  Dixon,  Tan,  Rossleigh,  Haindl,  Walker,  Druker,  Sawyers,  Capdeville,  Talpaz,  Ford,  Reese,  Kantarjian,  Resta,  Schermuly,  Grimminger,  Pullamsetti,  Ghofrani,  Dony,  Roth,  Savai,  Seeger,  Lai,  Weissmann,  Sydykov,  Druker,  Talpaz,  Lydon,  Capdeville,  Sawyers,  Kantarjian,  Ohno-Jones,  Ford,  Buchdunger,  Resta,  Peng,  Merchant,  Thiele,  Woo,  Mackall, Michael C. Heinrich, Denis Soulieres, Stephan Dirnhofer, Ajia Town, Shane G. Supple, Zariana Nikolova, Jane Apperley, George D. Demetri, Arin McKinley, Amy Harlow, Jonathan A. Fletcher, Heikki Joensuu, Lilla Di Scala, And Grant McArthur, Allan van Oosterom, John Seymour, Richard Herrmann, Christopher L. Corless, Evangelia Razis, Jeremy L. Norris, Mei-Jun Zhu, David D. Song, Anna Kalogera-Fountzila, George Fountzilas, Panayotis Selviaridis, Sofia Karanastasi, Stephanos Labropoulos, George Karkavelas, Thea Kalebic, Michael Torrens, Jonathan A. Fletcher, John M. Goldman,  Deininger,  Druker, Hagop Kantarjian, Ricardo Pasquini, Saengsuree Jootar, Andrzej Hellmann, Philippe Rousselot, Jerzy Holowiecki, Nina Khoroshko, Tadeusz Robak, Athena Countouriotis, Anatoly Golenkov, Neil Shah, Tamas Masszi, Andrey Zaritsky, Timothy Hughes, Jerald Radich, Aleksander Skotnicki, Nelson Hamerschlak,  
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Disease relevance of benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-


Psychiatry related information on benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-


High impact information on benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-


Chemical compound and disease context of benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-


Biological context of benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-

  • Aspects of disease monitoring and side effects are covered as well as resistance to imatinib and strategies to overcome resistance, such as alternative signal transduction inhibitors and drug combinations [24].
  • We report here that treatment of Abelson virus-transformed pre-B cell lines with the small molecule Abl kinase inhibitor (STI571) results in their differentiation to a late pre-B cell-like state characterized by induction of immunoglobulin (Ig) light chain gene rearrangement [25].
  • STI571 prevented phosphorylation of the PDGF receptor and suppressed activation of downstream signaling pathways [26].
  • Mice treated with STI571 or STI571 plus paclitaxel had less phosphorylated PDGF-R on tumor cells and tumor-associated endothelial cells, less tumor cell proliferation, statistically significantly more apoptotic tumor cells (all P<.001), and fewer tumor-associated endothelial cells (P<.001) than control mice [27].
  • The effect of imatinib on cell growth and apoptosis was examined with an MTT [3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide] assay and with a morphologic test and Annexin V staining, respectively [28].

Anatomical context of benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-

  • Based on a mathematical modeling approach that quantitatively explains a broad range of phenomena, we show for two independent datasets that clinically observed BCR-ABL1 transcript dynamics during imatinib treatment of CML can consistently be explained by a selective functional effect of imatinib on proliferative leukemia stem cells [5].
  • The combined treatment with STI571 and LMB also preferentially eliminates mouse bone marrow cells that express BCR-ABL [29].
  • Transmission electron micrographs from humans and mice treated with imatinib show mitochondrial abnormalities and accumulation of membrane whorls in both vacuoles and the sarco- (endo-) plasmic reticulum, findings suggestive of a toxic myopathy [17].
  • Conversely, leukemia subclones surviving inhibition of BCR-ABL1 by STI571 restore responsiveness to antigen receptor engagement and differentiate into immature B cells expressing immunoglobulin light chains [30].
  • Thoraces of C57BL/6 mice were irradiated (20 Gy), and mice were treated with three distinct PDGF RTKIs (SU9518, SU11657, or Imatinib) [31].

Associations of benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]- with other chemical compounds


Gene context of benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-


Analytical, diagnostic and therapeutic context of benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-


Disease relevance of Imatinib

  • Caspase cascade activation and mitochondria also play a key role in the imatinib-mediated sensitization of melanoma cells to the proapoptotic action of TRAIL [47].

Associations of Imatinib with other chemical compounds

  • In our studies, imatinib attenuated PDGFR signaling in fibroblast-like synoviocytes (FLSs) and TNF-alpha production in synovial fluid mononuclear cells (SFMCs) derived from human RA patients [48].


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  14. A cell-surface receptor for lipocalin 24p3 selectively mediates apoptosis and iron uptake. Devireddy, L.R., Gazin, C., Zhu, X., Green, M.R. Cell (2005) [Pubmed]
  15. Structural basis for the autoinhibition of c-Abl tyrosine kinase. Nagar, B., Hantschel, O., Young, M.A., Scheffzek, K., Veach, D., Bornmann, W., Clarkson, B., Superti-Furga, G., Kuriyan, J. Cell (2003) [Pubmed]
  16. Mechanisms of autoinhibition and STI-571/imatinib resistance revealed by mutagenesis of BCR-ABL. Azam, M., Latek, R.R., Daley, G.Q. Cell (2003) [Pubmed]
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  20. 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]
  21. Survival advantage from imatinib compared with the combination interferon-alpha plus cytarabine in chronic-phase chronic myelogenous leukemia: historical comparison between two phase 3 trials. Roy, L., Guilhot, J., Krahnke, T., Guerci-Bresler, A., Druker, B.J., Larson, R.A., O'Brien, S., So, C., Massimini, G., Guilhot, F. Blood (2006) [Pubmed]
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