Radotinib

Radotinib (IY-5511) is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC₅₀ of 34 nM. Radotinib has anti-prion and anti-tumor activities. Radotinib can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases^[1][2][3]. In Vitro:Radotinib (0-100 μM; 72 h) can inhibit the proliferation, induce apoptosis and cell cycle arrest of multiple myeloma cell lines. The mechanism involves the inhibition of the STAT3 and JAK2 signaling pathways^[1].
Radotinib (0-40 μM; 24 h) reduces the levels of PrP^Sc in ZW13-2 neuronal cells infected with 22L or 139A scrapie strains^[2]. In Vivo:Radotinib (100 mg/kg; intraperitoneal injection; once a day except on weekends; 21 days) has anti-tumor activity in a nude mouse model implanted with IM-9 cells^[1].
Radotinib (100 mg/kg; oral gavage; 4-8 weeks) can prolong the survival time of hamsters and reduce the deposition of PrP^Sc in hamsters infected with the 263K scrapie strain^[2].