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Purity: ≥98%
Radotinib (formerly IY-5511; IY5511; trade name Supect) is a novel, potent, selective, orally bioavailable, and 2nd generation BCR-ABL1 tyrosine kinase inhibitor with potential antineoplastic activity. It inhibits BCR-ABL1 with an IC50 of 34 nM. It was developed by Ilyang Pharmaceutical in S. Korea and has the potential for the treatment of Chronic Myeloid Leukemia.
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| Additional Infomation |
Radotinib is under investigation for the treatment of Leukemia, Myelogenous, Chronic, BCR-ABL Positive.
Radotinib is a second-generation tyrosine kinase inhibitor of Bcr-Abl fusion protein and the platelet-derived growth factor receptor (PDGFR), with potential antineoplastic activity. Upon administration, radotinib specifically inhibits the Bcr-Abl fusion protein, an abnormal enzyme expressed in Philadelphia chromosome positive chronic myeloid leukemia (CML) cells. In addition, this agent also inhibits PDGFR thereby blocking PDGFR-mediated signal transduction pathways. The inhibitory effect of radotinib on these specific tyrosine kinases may decrease cellular proliferation and inhibit angiogenesis. PDGFR, upregulated in many tumor cell types, is a receptor tyrosine kinase essential to cell migration and the development of the microvasculature. Drug Indication Radotinib is indicated for the treatment of different types of cancer, most notably Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) with resistance or intolerance of other Bcr-Abl tyrosine-kinase inhibitors, such as patients resistant or intolerant to imatinib. Mechanism of Action Philadelphia chromosome positive (Ph+) leukemia is driven by the constitutive enzymatic activity of the BCR-ABL1 fusion kinase. Tyrosine kinase inhibitors (TKIs) that block the activity of BCR-ABL1 are successfully used clinically to treat chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). |
| Molecular Formula |
C27H21F3N8O
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|---|---|
| Molecular Weight |
530.50
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| Exact Mass |
530.179
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| CAS # |
926037-48-1
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| Related CAS # |
Radotinib-d6;2754051-83-5
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| PubChem CID |
16063245
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.665
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| LogP |
4.29
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
39
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| Complexity |
818
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DUPWHXBITIZIKZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H21F3N8O/c1-16-3-4-18(9-23(16)37-26-33-6-5-22(36-26)24-13-31-7-8-32-24)25(39)35-20-10-19(27(28,29)30)11-21(12-20)38-14-17(2)34-15-38/h3-15H,1-2H3,(H,35,39)(H,33,36,37)
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| Chemical Name |
4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-((4-(pyrazin-2-yl)pyrimidin-2-yl)amino)benzamide
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| Synonyms |
IY-5511; IY5511; Radotinib; IY-5511 HCl; IY 5511; IY5511 HCl; trade name Supect.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.62 mg/mL (1.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.2 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.62 mg/mL (1.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.2 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8850 mL | 9.4251 mL | 18.8501 mL | |
| 5 mM | 0.3770 mL | 1.8850 mL | 3.7700 mL | |
| 10 mM | 0.1885 mL | 0.9425 mL | 1.8850 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03459534 | Recruiting | Drug: Radotinib HCl | Chronic Myeloid Leukemia, Chronic Phase |
Il-Yang Pharm. Co., Ltd. | June 25, 2018 | Phase 3 |
| NCT04691661 | Recruiting | Drug: Radotinib HCl 50 mg Drug: Placebo |
Parkinson Disease | Il-Yang Pharm. Co., Ltd. | September 9, 2021 | Phase 2 |
| NCT03722420 | Active, not recruiting | Drug: Radotinib Drug: Imatinib |
Chronic Myeloid Leukemia, Chronic Phase |
Il-Yang Pharm. Co., Ltd. | December 28, 2018 | Phase 3 |
| NCT01511289 | Completed | Drug: Imatinib Drug: Radotinib |
Leukemia Leukemia, Myeloid |
Il-Yang Pharm. Co., Ltd. | August 2011 | Phase 3 |
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