Radotinib

Catalog No.S8134 Synonyms: IY-5511

Radotinib Chemical Structure

Molecular Weight(MW): 530.50

Radotinib is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia.

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Biological Activity

Description Radotinib is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia.
Targets
BCR-ABL1 [1]
34 nM
In vitro

In vitro, Radotinib binds BCR-ABL1 and reduces phosphorylation of CrkL, a BCR-ABL1 target protein. Radotinib also effectively inhibits the proliferation of common mutant clones of BCR-ABL1, with the exception of T315I. [1] In AML cells, radotinib significantly decreases the cell viability, promotes differentiation, and induces CD11b expression and apoptosis. In NB4, THP-1, and Kasumi-1 cells, radotinib also induces CD11b expression, and decreases the viability. [2]

Protocol

Cell Research:[2]
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  • Cell lines: BMCs of AML and CML patients, NB4, HL60, KASUMI-1, and THP-1 cells
  • Concentrations: ~100 μM
  • Incubation Time: 72 h
  • Method: Cells are seeded in 96-well plates at a density of 2×104 cells/ml with 100 μL of medium per well and then incubated with various concentrations of radotinib (0, 1, 10, and 100 μM) for 72 h at 37°C. The CellTiter 96 solution (20 μL) is added directly to each well and plates are incubated for 4 h in a humidified 5% CO2 atmosphere at 37°C. Absorbance is measured with a PowerWave XS2 Microplate Spectrophotometer at 490 nm and the results are expressed as percentage changes from the basal condition using four to five culture wells for each experimental treatment. In some experiments, HL60 cells are cultured with 100 nM ATRA and 1 μM dasatinib for 4 days, and 10 μM radotinib is added to each group according to the planned schedule
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (188.5 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 530.50
Formula

C27H21F3N8O

CAS No. 926037-48-1
Storage powder
Synonyms IY-5511

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02422719 Recruiting Chronic Myeloid Leukemia Ulsan University Hospital April 2015 Phase 2
NCT02421926 Withdrawn Leukemia, Myelogenous, Chronic, BCR-ABL Positive Asan Medical Center October 2014 --
NCT01511289 Completed Leukemia|Leukemia, Myeloid|Leukemia, Myelogenous, Chronic, BCR-ABL Positive|Philadelphia Chromosome|Bone Marrow Diseases|Hematologic Diseases Il-Yang Pharm. Co., Ltd. August 2011 Phase 3
NCT01602952 Active, not recruiting Leukemia|Leukemia, Myeloid|Leukemia, Myelogenous, Chronic, BCR-ABL Positive|Philadelphia Chromosome|Hematologic Diseases Il-Yang Pharm. Co., Ltd. July 2008 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID