Radotinib
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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- Purity: 99.19%
- CAS No.: 926037-48-1
- 화학식: C27H21F3N8O
- 분자량:530.50
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Radotinib
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Biological Activity
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JAK2 |
STAT3 |
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 PrPSc 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.
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Cell Line:RPMI-8226, MM.1S, U266B1, and IM-9 cells
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Concentration:0, 10, 50 and 100 μM
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Incubation Time:72 h
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Result:Inhibited the cell viability in a dose-dependent manner.
Radotinib (100 mg/kg; oral gavage; 4-8 weeks) can prolong the survival time of hamsters and reduce the deposition of PrPSc 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.
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Animal Model:Athymic nude male mice aged five weeks old treated IM-9 cells[1]
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Dosage:100 mg/kg
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Administration:Intraperitoneal injection; once a day except on weekends; 21 days
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 926037-48-1
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Appearance Solid
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분자량 530.50
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화학식 C27H21F3N8O
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Color Light yellow to yellow
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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
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Synonyms
IY-5511
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선적
Room temperature in continental US; may vary elsewhere.
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보관
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
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Most Recent
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Pharmacol Res
Ceritinib inhibits growth and ACTH production of PitNETs: Insights from patient-derived organoids. [Abstract]2025 Nov:221:107993. PMID: 41083089
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (274 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.8850 mL | 9.4251 mL | 18.8501 mL | 47.1254 mL |
| 5 mM | 0.3770 mL | 1.8850 mL | 3.7700 mL | 9.4251 mL |
Radotinib Related Classifications
HY-15728 Related Classifications
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