Drug name: Dasatinib


Related CSCTT Targets

Bcr/Abl fusion [ref.1, 2 3]A9UF02

Dasatinib, BMS-354825

Cas.no PubChem ID
302962-49-8 3062316
Known Target
Tyrosine-protein kinase ABL1P00519
Proto-oncogene tyrosine-protein kinase SrcP12931
Ephrin type-A receptor 2P29317
Tyrosine-protein kinase LckP06239
Tyrosine-protein kinase YesP07947
Mast/stem cell growth factor receptor KitP10721
Platelet-derived growth factor receptor betaP09619
Signal transducer and activator of transcription 5BP51692
Abelson tyrosine-protein kinase 2P42684
Tyrosine-protein kinase FynP06241
Introduction
Dasatinib, at nanomolar concentrations, inhibits the following kinases: BCR-ABL, SRC family (SRC, LCK, YES, FYN), c-KIT, EPHA2, and PDGFRβ. Based on modeling studies, dasatinib is predicted to bind to multiple conformations of the ABL kinase. In vitro, dasatinib was active in leukemic cell lines representing variants of imatinib mesylate sensitive and resistant disease. Dasatinib inhibited the growth of chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cell lines overexpressing BCR-ABL. Under the conditions of the assays, dasatinib was able to overcome imatinib resistance resulting from BCR-ABL kinase domain mutations, activation of alternate signaling pathways involving the SRC family kinases (LYN, HCK), and multi-drug resistance gene overexpression.

Dasatinib, BMS-354825-Structure

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Reference

  • [1] Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. Talpaz, M., et al. (2006).N Engl J Med.354(24):2531-41.
    16775234. [ 16775234 ]
  • [2] Dasatinib (BMS-354825) targets an earlier progenitor population than imatinib in primary CML but does not eliminate the quiescent fraction. Copland, M., et al. (2006).Blood. 107(11):4532-9.
    16469872. [ 16469872 ]
  • [3] Characterization of cancer stem cells in chronic myeloid leukaemia. Jorgensen, H. G., et al. (2007).Biochem Soc Trans.35(Pt 5):1347-51.
    17956348. [ 17956348 ]

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