loading...| Preferred Name |
Imatinib Mesylate |
|
| Synonyms |
imatinib mesylate 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide Monomethanesulfonate IMATINIB MESYLATE Imatinib Mesylate CGP 57148 CGP57148B Gleevec Glivec STI 571 STI-571 STI571 |
|
| Definitions |
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). |
|
| ID |
http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C1687 |
|
| Accepted_Therapeutic_Use_For |
Philadelphia chromosome-positive chronic myelogenous leukemia and acute lymphocytic leukemia, gastrointestinal stromal tumor, hypereosinophillic syndrome, dermatofibrosarcoma protuberans, mutated-PDGFR myelodysplastic/myeloproliferative diseases. |
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| ALT_DEFINITION |
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. |
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| CAS_Registry |
220127-57-1 |
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| CHEBI_ID |
CHEBI:31690 |
|
| Chemical_Formula |
C29H31N7O.CH4O3S |
|
| code |
C1687 |
|
| Concept_In_Subset |
http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C176424 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157711 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C173381 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C157712 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C173383 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116978 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C116977 http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C128784 |
|
| Contributing_Source |
CTRP FDA GDC |
|
| 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). |
|
| Display_Name |
Imatinib Mesylate |
|
| FDA_UNII_Code |
8A1O1M485B |
|
| FULL_SYN |
imatinib mesylate 4-[(4-Methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide Monomethanesulfonate IMATINIB MESYLATE Imatinib Mesylate CGP 57148 CGP57148B Gleevec Glivec STI 571 STI-571 STI571 |
|
| Has_Free_Acid_Or_Base_Form | ||
| Has_Target |
http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C16325 |
|
| Is_Value_For_GDC_Property | ||
| label |
Imatinib Mesylate |
|
| Legacy Concept Name |
Imatinib |
|
| Maps_To |
Imatinib Mesylate |
|
| NCI_Drug_Dictionary_ID |
37862 |
|
| NSC Number |
716051 |
|
| PDQ_Closed_Trial_Search_ID |
37862 |
|
| PDQ_Open_Trial_Search_ID |
37862 |
|
| Preferred_Name |
Imatinib Mesylate |
|
| prefixIRI |
Thesaurus:C1687 |
|
| Semantic_Type |
Organic Chemical Pharmacologic Substance |
|
| UMLS_CUI |
C0939537 |
|
| subClassOf |
http://ncicb.nci.nih.gov/xml/owl/EVS/Thesaurus.owl#C159199 |