Radotinib

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. Radotinib also inhibits platelet-derived growth factor receptors (PDGFRs) alpha and beta with IC50 values of 75.5 and 130 nM, respectively. Binding of radotinib to Bcr-Abl in vitro inhibits the phosphorylation of the downstream signaling mediator CrkL. 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.Formal Name: 4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[[4-(2-pyrazinyl)-2-pyrimidinyl]amino]-benzamide. CAS Number: 926037-48-1. Synonyms: IY-5511. Molecular Formula: C27H21F3N8O. Formula Weight: 530.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 3 mg/mL, DMSO: 10 mg/mL. lambdamax: 215, 270 nm. SMILES: CC(C=CC(C(NC1=CC(N2C=NC(C)=C2)=CC(C(F)(F)F)=C1)=O)=C3)=C3NC4=NC(C5=NC=CN=C5)=CC=N4. InChi Code: InChI=1S/C27H21F3N8O/c1-16-3-4-18(9-23(16)37-26-33-6-5-22(36-26)24-13-31-7-8-32-24)25(39)35-20-10-19(27(28,29)30)11-21(12-20)38-14-17(2)34-15-38/h3-15H,1-2H3,(H,35,39)(H,33,36,37). InChi Key: DUPWHXBITIZIKZ-UHFFFAOYSA-N.