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Radotinib Bcr-Abl inhibitor

Cat.No.S8134

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

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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (188.5 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 530.50 Formula

C27H21F3N8O

Storage (From the date of receipt)
CAS No. 926037-48-1 Download SDF Storage of Stock Solutions

Synonyms IY-5511 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

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Mechanism of Action

Targets/IC50/Ki
BCR-ABL1
34 nM
In vitro
In vitro, Radotinib binds BCR-ABL1 and reduces phosphorylation of CrkL, a BCR-ABL1 target protein. This compound also effectively inhibits the proliferation of common mutant clones of BCR-ABL1, with the exception of T315I. In AML cells, it significantly decreases the cell viability, promotes differentiation, and induces CD11b expression and apoptosis. In NB4, THP-1, and Kasumi-1 cells, this chemical also induces CD11b expression, and decreases the viability.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-09-03)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03459534 RECRUITING
Chronic Myeloid Leukemia, Chronic Phase; CML, Chronic Phase; CML, Refractory; CML - Philadelphia Chromosome
Il-Yang Pharm. Co., Ltd.
2018-06-25 PHASE3
NCT04691661 ACTIVE_NOT_RECRUITING
Parkinson Disease
Il-Yang Pharm. Co., Ltd.
2021-09-09 PHASE2
NCT06461078 COMPLETED
Drug Kinetics
Il-Yang Pharm. Co., Ltd.
2024-07-22 PHASE1
NCT03722420 ACTIVE_NOT_RECRUITING
Chronic Myeloid Leukemia, Chronic Phase
Il-Yang Pharm. Co., Ltd.
2018-12-28 PHASE3
NCT04691661 Recruiting
Parkinson Disease
Il-Yang Pharm. Co. Ltd.
2021-09-09 Phase 2
NCT02422719 UNKNOWN
Chronic Myeloid Leukemia
Ulsan University Hospital
2015-04 PHASE2

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