Radotinib dihydrochloride
Based on 1 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 926037-85-6
- Formula: C27H23Cl2F3N8O
- Molecular Weight:603.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Radotinib dihydrochloride
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Biological Activity
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.
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Cell Line:RPMI-8226, MM.1S, U266B1, and IM-9 cells
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Concentration:0, 10, 50 and 100 μM
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Incubation Time:72 h
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Result:Inhibited the cell viability in a dose-dependent manner.
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.
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Animal Model:Athymic nude male mice aged five weeks old treated IM-9 cells[1].
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Dosage:100 mg/kg
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Administration:Intraperitoneal injection; once a day except on weekends; 21 days
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Result:Inhibited the growth of xenografted IM-9 cells in nude mice.
Repressed the expression of the activity and expression of STAT3, and its downstream proteins including Bcl-xL, Mcl-1, c-Myc, cyclin D1, and cyclin D3 in IM-9 cells isolated from the tumor tissue.
Dramatically reduced the expression of phospho-STAT3-positive cells in the tumor tissue.
Significantly increased the number of TUNEL-positive cells in the tumor tissue.
Chemical Information
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CAS No. 926037-85-6
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Molecular Weight 603.43
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Formula C27H23Cl2F3N8O
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SMILES
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
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Synonyms
IY-5511 dihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Pharmacol Res
Ceritinib inhibits growth and ACTH production of PitNETs: Insights from patient-derived organoids. [Abstract]2025 Nov:221:107993. PMID: 41083089
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)