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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.
Radotinib Bcr-Abl inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 530.50

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

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

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

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.

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Mechanism of Action

Targets/IC50/Ki
BCR-ABL1 [1]
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. [1] 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. [2]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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