尼洛替尼-d3是尼洛替尼的标记类似物，起Bcr-Abl酪氨酸激酶拮抗剂的作用。研究表明，尼洛替尼-d3抑制HSCs的增殖，迁移和肌动蛋白丝形成。此外，尼洛替尼-d3可以通过减少bcl-2的表达和增加p53的表达，PARP的裂解以及PPARγ和TRAIL-R的表达增加，导致HSCs凋亡。尼洛替尼-d3通过抑制PDGF和TGFβ强烈抑制ERK和Akt1的磷酸化。或者，尼洛替尼-d3在慢性，加速和破伤期对慢性粒细胞白血病表现出显着的疗效。尼洛替尼-d3在抑制人类造血干细胞中的罗丹明123和赫斯特33342外排方面远比伊马替尼和达沙替尼有效。 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 and dasatinib at inhibiting rhodamine 123 and Hoechst 33342 efflux in human hematopoietic stem cells.
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Nilotinib-d3
CAS number：1215678-43-5 molecular formula：C28H19D3F3N7O
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| Chinese alias | - | ||
| English alias | 4-Methyl-N-{3-[4-(~2~H_3_)methyl-1H-imidazol-1-yl]-5-(trifluoromethyl)phenyl}-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}benzamide | 4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]-N-[3-[4-(trideuteriomethyl)imidazol-1-yl]-5-(trifluoromethyl)phenyl]benzami | ||
| CAS number | 1215678-43-5 | molecular formula | C28H19D3F3N7O |
| molecular weight | 532.53 g/mol | Exact mass | ≥95 atom% D,≥95% |
| PSA | - | logp | - |
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RTECS：
CV5581770
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