Radotinib(IY-5511) (Synonyms: IY-5511) |
| رقم الكتالوجGC11140 |
Bcr-Abl tyrosine kinase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 926037-48-1
Sample solution is provided at 25 µL, 10mM.
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Radotinib(IY-5511) is a novel and selective Bcl-Abl tyrosine kinase inhibitor. [1]
Bcl-Abl is a constitutively activated chimeric tyrosine kinase which is the genetic abnormality expressed in patient with CML (chronic myeloid leukemia).
In vitro, radotinib couples to Bcr-Abl and reduce the phosphorylation of Bcr-Abl target protein CrkL. The pre-clinical studies shows superiority of radotinib to imatinib in both wild-type and mutant BCR-ABL1 positive CML cell lines. [1]
In a phase I clinical trial, dose up to 1000 mg/day of radotinib exhibits no dose-limiting toxicities. Phase II study proves radotinib to be an effective and well tolerated in chronic phase-chronic myeloid leukemia patients with resistance and/or intolerance to Bcr-Abl1 tyrosine kinase inhibitors. [1]
Reference:
1. Kim SH, Menon H, Jootar S 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.
| Cell experiment [1]: | |
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Cell lines |
Bone marrow cells (BMCs) from patients with AML |
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Preparation method |
The solubility of this compound in DMSO is > 26.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
1, 10, and 100 µM, 72 h, 37 ℃ |
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Applications |
Radotinib is an inhibitor of BCR-ABL1 tyrosine kinase and has been approved for the second-line treatment of chronic myeloid leukemia. In BMCs from patients with AML, radotinib increased cleaved caspase-3, caspase-7, and caspase-9 levels, resulting in increasing apoptosis. Radotinib also induced G0/G1 phase arrest and inhibited proliferating of BMCs from patients with AML. |
| Clinical experiment [2]: | |
|
Clinical samples |
Patients at least 18 years of age with Philadelphia chromosome-positive chronic phase-CML with resistance and/or intolerance to imatinib. |
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Dosage form |
400 mg, twice daily |
|
Application |
Patients’ response to radotinib is comparable to other 2nd-generation tyrosine kinase inhibitors. Radotinib is well tolerated and effective in chronic phase-chronic myeloid leukemia patients with resistance and/or intolerance to imatinib. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Heo S K, Noh E K, Gwon G D, et al. Radotinib inhibits acute myeloid leukemia cell proliferation via induction of mitochondrial-dependent apoptosis and CDK inhibitors[J]. European journal of pharmacology, 2016, 789: 280-290. [2]. Kim S H, Menon H, Jootar S, et al. Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors[J]. Haematologica, 2014: haematol. 2013.096776. | |
| Cas No. | 926037-48-1 | SDF | |
| المرادفات | IY-5511 | ||
| Chemical Name | (Z)-4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-((4-(pyrazin-2-yl)pyrimidin-2-yl)amino)benzimidic acid | ||
| Canonical SMILES | CC1=C(NC2=NC=CC(C3=CN=CC=N3)=N2)C=C(/C(O)=N/C4=CC(N(C=N5)C=C5C)=CC(C(F)(F)F)=C4)C=C1 | ||
| Formula | C27H21F3N8O | M.Wt | 530.5 |
| الذوبان | ≥ 26.55mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.885 mL | 9.4251 mL | 18.8501 mL |
| 5 mM | 0.377 mL | 1.885 mL | 3.77 mL |
| 10 mM | 0.1885 mL | 0.9425 mL | 1.885 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
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