| 包装: | 1mg |
| 规格: | 98% |
| 市场价: | 7779元 |
| 分子量: | 536.5 |
Background:
Radotinib-d6is intended for use as an internal standard for the quantification of radotinib by GC- or LC-MS. Radotinib is a second generation tyrosine kinase inhibitor that targets both the wild-type and mutant forms of Bcr-Abl (IC50= 30.6 nM in Ba/F3 human chronic myeloid leukemia cells expressing the wild-type enzyme).1Radotinib also inhibits platelet-derived growth factor receptors (PDGFRs) α and β with IC50values of 75.5 and 130 nM, respectively.2,3Binding of radotinib to Bcr-Ablin vitroinhibits the phosphorylation of the downstream signaling mediator CrkL.3In acute myeloid leukemia cells,in vitrotreatment with radotinib at doses of 10 to 100 µM reduces viability, activates the mitochondrial apoptosis pathway, and promotes expression of the differentiation marker CD11b.2
1.Zabriskie, M.S., Vellore, N.A., Gantz, K.C., et al.Radotinib is an effective inhibitor of native and kinase domain-mutant BCR-ABL1Leukemia29(9)1939-1942(2015) 2.Heo, S.-K., Noh, E.-K., Yoon, D.-J., et al.Radotinib induces apoptosis of CD11b+ cells differentiated from acute myeloid leukemia cellsPLoS One10(6)e0129853(2015) 3.Kim, S.-H., Menon, H., Jootar, S., et al.Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitorsHaematologica99(7)1191-1196(2014)
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