Home Angiogenesis Bcr-Abl inhibitor Radotinib For research use only.

Radotinib

Synonyms: IY-5511

Radotinib (IY-5511) is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia.

Radotinib Chemical Structure

Radotinib Chemical Structure

CAS: 926037-48-1

Selleck's Radotinib has been cited by 1 publication

Purity & Quality Control

Batch: S813401 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.42%
99.42

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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 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]
Cell Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04691661 Recruiting Parkinson Disease Il-Yang Pharm. Co. Ltd. September 9 2021 Phase 2

Chemical lnformation & Solubility

Molecular Weight 530.50 Formula

C27H21F3N8O
CAS No. 926037-48-1 SDF Download Radotinib SDF
Smiles CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=NC=CN=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (188.5 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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