Cat No.
CEI-0267
Description
Nilotinib (AMN-107) can inhibit Bcr-Abl with IC50 of 30 nM.
Alias
Tasigna
Synonyms
Tasigna
CAS No.
641571-10-0
Targets
Bcr-Abl
Chemical Name
4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)benzamide
M.Wt
529.52
Purity
>99%
Solubility
DMSO 36 mg/mL Water
Storage
2 years at -20centigrade Powder
In vitro
Nilotinib(AMN-107) is a novel tyrosine kinase inhibitor targeting KIT (CD117), PDGFR and BCR-ABL and inhibiting the proliferation of both imatinib-sensitive and imatinib-resistant cells in vitro. AMN-107, which is more potent than imatinib, can inhibit the proliferation of haematopoietic cells expressing the mutants in Ph+ CML and acute lymphoblastic leukaemia with IC50 of 12 nM, approximately. For several imatinib-resistant Bcr-Abl mutants expect T3151, AMN-107 can effective against them.
In vivo
In mice transduced with Bcr-Abl, AMN-107 reduced mortality and tumour burden. In mice transduced with the E255V imatinib-resistant mutant of Bcr-Abl, AMN-107 delayed the onset of leukaemia.
