About: Nilotinib Hydrochloride Anhydrous     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • Nilotinib Hydrochloride Anhydrous
rdfs:subClassOf
Has_Free_Acid_Or_Base_Form
Concept_In_Subset
Semantic_Type
  • Pharmacologic Substance
Preferred_Name
  • Nilotinib Hydrochloride Anhydrous
UMLS_CUI
  • C2987005
CAS_Registry
  • 923288-95-3
FDA_UNII_Code
  • K37N7BYX3X
Contributing_Source
  • FDA
Chemical_Formula
  • C28H22F3N7O.HCl
FULL_SYN
  • Nilotinib Hydrochloride AnhydrousPTNCI
  • NILOTINIB HYDROCHLORIDE ANHYDROUSPTFDAK37N7BYX3X
DEFINITION
  • The hydrochloride salt of nilotinib, 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). With a binding mode that is energetically more favorable than that of imatinib, nilotinib has been shown to have an approximately 20-fold increased potency in kinase and proliferation assays compared to imatinib.NCI
code
  • C95223
is Has_Salt_Form of
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