Nilotinib hcl monohydrate

  • Chemical Properties
CAS No. 923288-90-8 Cat. No. BCP11142
Name Nilotinib hcl monohydrate
Synonyms Nilotinib HCl hydrate;AMN 107; AMN107; AMN-107; Nilotinib;Nilotinib monohydrochloride monohydrate;
Formula C28H22F3N7O.H2O M. Wt 584
  • Biological Activity
Description Nilotinib monohydrochloride monohydrate is a second generation tyrosine kinase inhibitor (TKI), is significantly more potent against BCR-ABL than Imatinib, and is active against many Imatinib-resistant BCR-ABL mutants.Nilotinib, also known as AMN-107, is an orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. Designed to overcome imatinib resistance, nilotinib binds to and stabilizes the inactive conformation of the kinase domain of the Abl protein of the Bcr-Abl fusion protein, resulting in the inhibition of the Bcr-Abl-mediated proliferation of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) cells. This agent also inhibits the receptor tyrosine kinases platelet-derived growth factor receptor (PDGF-R) and c-kit, a receptor tyrosine kinase mutated and constitutively activated in most gastrointestinal stromal tumors (GISTs).
Pathways Angiogenesis/Protein Tyrosine Kinase 
Targets Src/Bcr Abl 

Structure

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