Description
Nilotinib (AMN-107) can inhibit Bcr-Abl with IC50 of 30 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C28H22F3N7O
Chemical Name
4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)benzamide
Solubility
DMSO 36 mg/mL Water
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.
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