NCIt definition : 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).;
Alternative definition : NCI-GLOSS: A drug used to treat different types of leukemia and other cancers of the
blood, gastrointestinal stromal tumors, skin tumors called dermatofibrosarcoma protuberans,
and a rare condition called systemic mastocytosis. It is also being studied in the
treatment of other types of cancer. Imatinib mesylate blocks the protein made by the
bcr/abl oncogene. It is a type of tyrosine kinase inhibitor.;
UNII : 8A1O1M485B;
InChIKey : YLMAHDNUQAMNNX-UHFFFAOYSA-N;
CAS number : 220127-57-1;
Drug name : Glivec; Gleevec;
Molecule name : CGP-57148B; STI-571; CGP 57148; CGP 57148B; CGP-57148;
Chemical formula : C29H31N7O.CH4O3S;
NSC code : 716051;
ChEBI ID : CHEBI:31690;
Codes from synonyms : NSC0716051; 50363; CDR0000258252; CDR0000044893; CDR0000043975;