CAS Number: 923288-90-8

Formula: C28H25ClF3N7O2.

Molecular Weight: 583.99 g/mol

Method of Analysis:In house Monograph

Application: Nilotinib is an orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor (TKI) with antineoplastic activity. It is a second-generation, selective TKI, approximately 30-fold more potent than imatinib. It is used in the therapy of chronic myelogenous leukemia, and was designed to overcome imatinib resistance.

Mechanism:

Because BCR-ABL is a key cause of Philadelphia chromosome-positive chronic myeloid leukemia (Ph+ CML) and remains the driver of the disease throughout the chronic phase, BCR-ABL inhibition is the focus of CML treatment. Nilotinib was rationally designed to antagonize the aberrant tyrosine kinase activity of Bcr-Abl-positive cells. 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 drug 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 30-fold increased potency in kinase and proliferation assays compared to imatinib.

Storage conditions: Room Temprature

Packaging: Polyethylene nylon plastic bag