Imatinib mesylate

  • Chemical Properties
CAS No. 220127-57-1 Cat. No. BCP01255
Name Imatinib mesylate
Synonyms STI571 Mesylate; CGP-57148B Mesylate;CGP 57148; CGP57148; CGP-57148; CGP57148B; CGP-57148B; CGP 57148B; STI571; STI-571; STI 571;
Formula C29H31N7O.CH4O3S M. Wt 589.71
  • Biological Activity
Description Imatinib Mesylate is the mesylate salt of imatinib, a tyrosine kinase inhibitor with antineoplastic activity. Imatinib binds to an intracellular pocket located within tyrosine kinases (TK), thereby inhibiting ATP binding and preventing phosphorylation and the subsequent activation of growth receptors and their downstream signal transduction pathways. This agent inhibits TK encoded by the bcr-abl oncogene as well as receptor TKs encoded by the c-kit and platelet-derived growth factor receptor (PDGFR) oncogenes. Inhibition of the bcr-abl TK results in decreased proliferation and enhanced apoptosis in malignant cells of Philadelphia-positive (Ph+) hematological malignancies such as CML and ALL; effects on c-kit TK activity inhibit mast-cell and cellular proliferation in those diseases overexpressing c-kit, such as mastocytosis and gastrointestinal stromal tumor (GIST).
Pathways Angiogenesis/Protein Tyrosine Kinase 
Targets Src/Bcr Abl PDGFR c Kit 

Structure

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