Tyrosine kinase inhibitor; Inhibits BCR/ABL and ABL
CAS
641571-10-0
Synonyme
AMN107; Tasigna
Quantité
50 mg
Formule moléculaire
C28H22F3N7O
Pureté
≥95%
Marque
STEMCELL Technologies
Caractéristiques principales
Nilotinib is a second-generation inhibitor of the oncogenic tyrosine kinase BCR-ABL with IC50 values of 19, 140, and 9,200 nM for wild-type, E255K, and T315I mutant forms of BCR-ABL, respectively (Kitagawa et al.; Verstovsek et al.; O'Hare)
It binds to the ATP-binding pocket of ABL, with higher affinity than imatinib (Manley et al. 2006; Verstovsek et al.) 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 (KIT), and colony-stimulating factor 1 receptor (CSF-1R; Manley et al. 2010)