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nilotinib

Ligand Summary
Ligand Structure
Rendered image for the query structure
Description
Nilotinib is an inhibitor of the BCR-ABL kinase. Nilotinib binds to and stabilizes the inactive conformation of the kinase domain of ABL protein. In vitro, nilotinib inhibited BCR-ABL mediated proliferation of murine leukemic cell lines and human cell lines derived from patients with Ph+ CML. Under the conditions of the assays, nilotinib was able to overcome imatinib resistance resulting from BCR-ABL kinase mutations, in 32 out of 33 mutations tested. In vivo, nilotinib reduced the tumor size in a murine BCR-ABL xenograft model.
Synonyms & Links
Guide to Pharmacology: 5697
DrugCentral: 1932
LyCHI:  HBA97ATR7TC8


Target Activities