Radotinib

Radotinib

CAT N°: 19923
Price:

From 48.00 40.80

Radotinib is a selective second generation tyrosine kinase inhibitor that targets both the wild-type and mutant forms of Bcr-Abl, with an IC50 value of 30.6 nM in Ba/F3 human chronic myeloid leukemia cells expressing the wild-type form.{38002} Radotinib also inhibits platelet-derived growth factor receptors (PDGFRs) ? and ? 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 10-100 µM reduces viability, activates the mitochondrial apoptosis pathway, and promotes expression of the differentiation marker CD11b.{38000}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(2-pyrazinyl)-2-pyrimidinyl]amino]-benzamide
  • Correlated keywords
    • IY5511 PDGFRa PDGFRb supect BcrAbl cd-11b baf3 CML
  • Product Overview:
    Radotinib is a selective second generation tyrosine kinase inhibitor that targets both the wild-type and mutant forms of Bcr-Abl, with an IC50 value of 30.6 nM in Ba/F3 human chronic myeloid leukemia cells expressing the wild-type form.{38002} Radotinib also inhibits platelet-derived growth factor receptors (PDGFRs) ? and ? 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 10-100 µM reduces viability, activates the mitochondrial apoptosis pathway, and promotes expression of the differentiation marker CD11b.{38000}

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