imatinib mesylate

CGP 57148

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). Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C1687" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C1687" NCI Thesaurus)

http://purl.bioontology.org/ontology/PDQ/CDR0000037862

CGP 57148

4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-phenyl]benzamide methanesulfonate

Glivec

Gleevec

STI-571

CGP-57148

CGP57148B

CGP57148

STI571

152459-95-5

http://purl.bioontology.org/ontology/PDQ/CDR0000361546

http://purl.bioontology.org/ontology/PDQ/CDR0000038399

http://purl.bioontology.org/ontology/PDQ/CDR0000258376

http://purl.bioontology.org/ontology/PDQ/CDR0000355818

http://purl.bioontology.org/ontology/PDQ/CDR0000038398

http://purl.bioontology.org/ontology/PDQ/CDR0000346482

http://purl.bioontology.org/ontology/PDQ/CDR0000410685

http://purl.bioontology.org/ontology/PDQ/CDR0000387811

http://purl.bioontology.org/ontology/PDQ/CDR0000257171

http://purl.bioontology.org/ontology/PDQ/CDR0000038396

http://purl.bioontology.org/ontology/PDQ/CDR0000361547

http://purl.bioontology.org/ontology/PDQ/CDR0000258241

http://purl.bioontology.org/ontology/PDQ/CDR0000269719

http://purl.bioontology.org/ontology/PDQ/CDR0000271297

http://purl.bioontology.org/ontology/PDQ/CDR0000334951

http://purl.bioontology.org/ontology/PDQ/CDR0000038200

http://purl.bioontology.org/ontology/PDQ/CDR0000315584

http://purl.bioontology.org/ontology/PDQ/CDR0000355823

http://purl.bioontology.org/ontology/PDQ/CDR0000391021

http://purl.bioontology.org/ontology/PDQ/CDR0000038194

http://purl.bioontology.org/ontology/PDQ/CDR0000038519

http://purl.bioontology.org/ontology/PDQ/CDR0000361544

http://purl.bioontology.org/ontology/PDQ/CDR0000335282

http://purl.bioontology.org/ontology/PDQ/CDR0000441242

http://purl.bioontology.org/ontology/PDQ/CDR0000038397

http://purl.bioontology.org/ontology/PDQ/CDR0000334946

http://purl.bioontology.org/ontology/PDQ/CDR0000318798

http://purl.bioontology.org/ontology/PDQ/CDR0000374717

http://purl.bioontology.org/ontology/PDQ/CDR0000258413

http://purl.bioontology.org/ontology/PDQ/CDR0000270390

http://purl.bioontology.org/ontology/PDQ/CDR0000356029

http://purl.bioontology.org/ontology/PDQ/CDR0000370025

http://purl.bioontology.org/ontology/PDQ/CDR0000038400

C0939537

C0385728

C0935987

C0906802

2010-06-03

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). Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C1687" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C1687" NCI Thesaurus)

61135

10266

TRD

C1687

CDR0000037862

716051

Drug/agent

imatinib mesylate

T109

T121