Radotinib

Catalog No.S8134 Batch:S813401

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Technical Data

Formula

C27H21F3N8O

Molecular Weight 530.50 CAS No. 926037-48-1
Solubility (25°C)* In vitro DMSO 100 mg/mL (188.5 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Radotinib (IY-5511) 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 (from reference)

Cell Assay:[2]
  • 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

Selleck's Radotinib has been cited by 1 publication

Multikinase Abl/DDR/Src Inhibition Produces Optimal Effects for Tyrosine Kinase Inhibition in Neurodegeneration. [ Drugs R D, 2019, 19(2):149-166] PubMed: 30919310

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.