Radotinib dihydrochloride  (Synonyms: IY-5511 dihydrochloride)

Radotinib (IY-5511) dihydrochloride is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC₅₀ of 34 nM. Radotinib dihydrochloride has anti-prion and anti-tumor activities. Radotinib dihydrochloride can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib dihydrochloride 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].

Radotinib (0-100 μM; 72 h) dihydrochloride 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) dihydrochloride reduces the levels of PrPSc in ZW13-2 neuronal cells infected with 22L or 139A scrapie strains^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Radotinib (100 mg/kg; intraperitoneal injection; once a day except on weekends; 21 days) dihydrochloride has anti-tumor activity in a nude mouse model implanted with IM-9 cells^[1].
Radotinib (100 mg/kg; oral gavage; 4-8 weeks) dihydrochloride can prolong the survival time of hamsters and reduce the deposition of PrPSc in hamsters infected with the 263K scrapie strain^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

603.43

C₂₇H₂₃Cl₂F₃N₈O

926037-85-6

O=C(C1=CC=C(C)C(NC2=NC(C3=NC=CN=C3)=CC=N2)=C1)NC4=CC(C(F)(F)F)=CC(N5C=NC(C)=C5)=C4.Cl.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Heo SK, et al. Radotinib inhibits multiple myeloma cell proliferation via suppression of STAT3 signaling. PLoS One. 2022 May 3;17(5):e0265958.  [Content Brief]

  [2]. Choi YG, et al. Radotinib Decreases Prion Propagation and Prolongs Survival Times in Models of Prion Disease. Int J Mol Sci. 2023 Jul 31;24(15):12241.  [Content Brief]

  [3]. Kim SH, et al. Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors. Haematologica. 2014 Jul;99(7):1191-6.  [Content Brief]