Nilotinib-d3 is a labeled analogue of Nilotinib which functions as a Bcr-Abl tyrosine kinase antagonist. Studies suggest that Nilotinib-d3 inhibits proliferation, migration and actin filament formation in HSCs. In addition, Nilotinib-d3 can cause apoptosis in HSCs via reducing the expression of bcl-2 and increasing the expression p53, cleavage of PARP, along with an increased expression of PPARγ and TRAIL-R. Nilotinib-d3 strongly inhibits the phosphorylation of ERK and Akt1 via suppressing PDGF and TGFβ. Alternatively, Nilotinib-d3 shows significant efficacy towards chronic myeloid leukemia in chronic, accelerated, and blastic phases. Nilotinib-d3 is far more effective than imatinib (sc-267106) and dasatinib (sc-358114) at inhibiting rhodamine 123 and Hoechst 33342 efflux in human hematopoietic stem cells.
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