Nilotinib（CAS No.:641571-10-0） may be a selective aminoalkanoic acid enzyme substance that targets BCR-ABL enzyme, c-KIT and blood platelet derived protein receptor (PDGFR); it doesn't have activity against the SRC family. Nilotinib inhibits BCR-ABL mediate proliferation of leukemic cell lines by binding to the ATP-binding website of BCR-ABL and inhibiting aminoalkanoic acid enzyme activity. Nilotinib has activity in imatinib-resistant BCR-ABL enzyme mutations.
Nilotinib is Associate in Nursing orally bioavailable aminopyrimidine-derivative Bcr-Abl aminoalkanoic acid enzymesubstance with antineoplastic activity. Designed to beat imatinib resistance, nilotinib binds to and stabilizes the inactive conformation of the enzyme domain of the Abl macromolecule of the Bcr-Abl fusion macromolecule, leading to the inhibition of the Bcr-Abl-mediated proliferation of urban center chromosome-positive (Ph+) chronic granulocytic leukemia (CML) cells. This agent conjointly inhibits the receptor aminoalkanoic acid kinases platelet-derived protein receptor (PDGF-R) and c-kit, a receptor aminoalkanoic acid enzyme mutated and constitutively activated in most epithelial duct stromal tumors (GISTs). With a binding mode that's energetically a lot offavorable than that of imatinib, nilotinib has been shown to possess Associate in Nursing close to 20-fold hyperbolic efficiency in enzyme and proliferation assays compared to imatinib.
