Art. -Nr.: HY-15728

Radotinib

(Synonyms: IY-5511)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Radotinib (IY-5511) is an orally active and BBB-permeable selective tyrosine kinase Bcr-Abl1 inhibitor with an IC₅₀ of 34 nM. Radotinib has anti-prion and anti-tumor activities. Radotinib can inhibit the proliferation, induce cell cycle arrest and apoptosis of tumor cells . Radotinib can be used in the research of cancer such as chronic myeloid leukemia and multiple myeloma, as well as neurodegenerative diseases such as prion diseases.

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Reinheit: 99.19%
CAS. Nr.: 926037-48-1
Formel: C₂₇H₂₁F₃N₈O
Molecular Weight:530.50

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Radotinib Chemical Structure

CAS. Nr.: 926037-48-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

JAK2

STAT3

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen :

Abl
Bcr-Abl

Alle STAT Isoform-spezifische Produkte anzeigen :

Alle JAK Isoform-spezifische Produkte anzeigen :

In Vitro

Radotinib (0-100 μM; 72 h) can inhibit the proliferation, induce apoptosis and cell cycle arrest of multiple myeloma cell lines. The mechanism involves the inhibition of the STAT3 and JAK2 signaling pathways^[1].
Radotinib (0-40 μM; 24 h) reduces the levels of PrP^Sc in ZW13-2 neuronal cells infected with 22L or 139A scrapie strains^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

RPMI-8226, MM.1S, U266B1, and IM-9 cells
Concentration:

0, 10, 50 and 100 μM
Incubation Time:

72 h
Result:

Inhibited the cell viability in a dose-dependent manner.

In Vivo

Radotinib (100 mg/kg; intraperitoneal injection; once a day except on weekends; 21 days) has anti-tumor activity in a nude mouse model implanted with IM-9 cells^[1].
Radotinib (100 mg/kg; oral gavage; 4-8 weeks) can prolong the survival time of hamsters and reduce the deposition of PrP^Sc in hamsters infected with the 263K scrapie strain^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Athymic nude male mice aged five weeks old treated IM-9 cells^[1]
Dosage:

100 mg/kg
Administration:

Intraperitoneal injection; once a day except on weekends; 21 days
Result:

Inhibited the growth of xenografted IM-9 cells in nude mice.
Repressed the expression of the activity and expression of STAT3, and its downstream proteins including Bcl-xL, Mcl-1, c-Myc, cyclin D1, and cyclin D3 in IM-9 cells isolated from the tumor tissue.
Dramatically reduced the expression of phospho-STAT3-positive cells in the tumor tissue. Significantly increased the number of TUNEL-positive cells in the tumor tissue.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 926037-48-1
Appearance Solid
Molecular Weight 530.50
Formel C₂₇H₂₁F₃N₈O
Color Light yellow to yellow
SMILES

O=C(NC1=CC(C(F)(F)F)=CC(N2C=C(C)N=C2)=C1)C3=CC=C(C)C(NC4=NC=CC(C5=NC=CN=C5)=N4)=C3
Synonyms

IY-5511
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Journal Impact Factor

Pharmacol Res

Ceritinib inhibits growth and ACTH production of PitNETs: Insights from patient-derived organoids. [Abstract]

2025 Nov:221:107993. PMID: 41083089

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 5 mg/mL (9.43 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8850 mL

9.4251 mL

18.8501 mL

5 mM

0.3770 mL

1.8850 mL

3.7700 mL

10 mM

---

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.5 mg/mL (0.94 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Heo SK, et al. Radotinib inhibits multiple myeloma cell proliferation via suppression of STAT3 signaling. PLoS One. 2022 May 3;17(5):e0265958. [Content Brief]

[2]. Choi YG, et al. Radotinib Decreases Prion Propagation and Prolongs Survival Times in Models of Prion Disease. Int J Mol Sci. 2023 Jul 31;24(15):12241. [Content Brief]

[3]. Kim SH, et al. Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors. Haematologica. 2014 Jul;99(7):1191-6. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8850 mL	9.4251 mL	18.8501 mL	47.1254 mL
DMSO	5 mM	0.3770 mL	1.8850 mL	3.7700 mL	9.4251 mL

Keywords

Radotinib

1 Cited Publications

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Radotinib

Anti-Infection Compound Library

Apoptosis Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Protein Tyrosine Kinase Compound Library

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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

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Publications Citing Use of MedChemExpress (MCE) Radotinib

Alle Bcr-Abl Isoform-spezifische Produkte anzeigen

Alle STAT Isoform-spezifische Produkte anzeigen

Alle JAK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Radotinib Related Classifications

HY-15728 Related Classifications