Formulation: A solid
Formal Name: 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-benzamide, monohydrochloride, monohydrate
Purity: ≥98%
Formula Markup: C28H22F3N7O • HCl [H2O]
Formula Weight: 584
Shelf life (days): 1460
CAS Number: 923288-90-8
Notes: Nilotinib is an inhibitor of wild-type and mutant Bcr-Abl (IC50s = 15 and 9-400 nM, respectively).{17481} It is selective for wild-type and mutant Bcr-Abl over Src and LYN (IC50s = >5,000 nM for both). Nilotinib inhibits Bcr-Abl autophosphorylation and cell proliferation in Ba/F3 cells expressing wild-type or mutant Bcr-Abl (IC50s = 7-155 and 13-51 nM, respectively). In vivo, nilotinib (1 mg/kg) reduces midbrain Bcr-Abl autophosphorylation, amyloid-β levels, and neuronal loss, as well as improves autophagosome clearance and reverses cognitive deficits in the Tg2576 transgenic mouse model of Alzheimer’s disease.{65243} It also reduces serum creatine levels, renal profibrotic gene expression, and tubulointerstitial damage, as well as increases survival in a rat model of 5/6 nephrectomy-induced chronic kidney disease.{65244} Formulations containing nilotinib have been used in the treatment of leukemia.
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