Nilotinib, 50 mg

A second-generation tyrosine kinase inhibitor supplied by STEMCELL Technologies, Nilotinib targets the oncogenic kinase BCR-ABL. It binds to the ATP binding pocket of ABL with higher affinity than Imatinib and demonstrates activity below 1 µM against discoidin domain receptors (DDR)-1 and -2, platelet-derived growth factor receptors (PDGFR)-α and -β, stem cell factor receptor (c-KIT), and colony-stimulating factor 1 receptor (CSF-1R).

Reported IC₅₀ values are 19, 140, and 9,200 nM for wild-type, E255K, and T315I mutant forms of BCR-ABL, respectively. Published applications include inhibition of cellular proliferation in wild-type and mutant forms of Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL) and chronic myeloid leukemia (CML) cells, inhibition of cell proliferation and S-phase progression in the human lung cell line A549, and reduction of muscle fibrosis by promoting TNF-mediated apoptosis of fibro/adipogenic progenitors.

Nilotinib (AMN107; also known as Tasigna) has a molecular formula of C₂₈H₂₂F₃N₇O, a molecular weight of 529.5 g/mol, and CAS number 641571-10-0. It is supplied as a crystalline solid with a stated purity of ≥ 95%. The compound is soluble in DMSO at concentrations up to 3.8 mM but has low solubility in aqueous media. As supplied, the product is stable at -20°C for 12 months from date of receipt when protected from prolonged exposure to light. For research use only.