Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 4-(methyl-d3)-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(2-pyrazinyl)-2-pyrimidinyl]amino]-benzamide-2,5,6-d3
Purity: ≥99% deuterated forms (d1-d6)
Formula Markup: C27H15D6F3N8O
Formula Weight: 536.540529
CAS Number: 2754051-83-5
Notes: Radotinib-d6 is intended for use as an internal standard for the quantification of radotinib (Item No. 19923) 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).{38002} Radotinib also inhibits platelet-derived growth factor receptors (PDGFRs) α and β with IC50 values of 75.5 and 130 nM, respectively.{38000,38001} Binding of radotinib to Bcr-Abl in vitro inhibits the phosphorylation of the downstream signaling mediator CrkL.{38001} In acute myeloid leukemia cells, in vitro treatment with radotinib at doses of 10 to 100 µM reduces viability, activates the mitochondrial apoptosis pathway, and promotes expression of the differentiation marker CD11b.{38000}