Nilotinib, 10 mg

A second-generation tyrosine kinase inhibitor supplied by STEMCELL Technologies, this compound targets the oncogenic kinase BCR-ABL and is also referenced by the synonyms AMN107 and Tasigna. It binds to the ATP binding pocket of ABL with higher affinity than imatinib and prevents the growth of Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) and acute lymphoblastic leukemia (ALL) cells.

The inhibitor shows IC₅₀ values of 19, 140, and 9,200 nM for wild-type, E255K, and T315I mutant forms of BCR-ABL, respectively. It also has 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). Published applications include reducing fibrosis by promoting TNF-mediated apoptosis of mesenchymal stem cells, and inhibiting cellular proliferation in wild-type and mutant forms of Ph+ ALL and CML cells.

The chemical name is 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide, with CAS Number 641571-10-0, molecular formula C₂₈H₂₂F₃N₇O, and molecular weight 529.5 g/mol. The product is supplied as a crystalline solid with a purity of ≥ 95% and is stable at -20°C for 12 months from the date of receipt when protected from prolonged exposure to light. Solubility is approximately 3 mg/mL in DMF and 10 mg/mL in DMSO, and the product information sheet lists a DMSO stock solubility limit of 3.8 mM. The product is classified as hazardous, and users should consult the Safety Data Sheet before handling.