| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Radorinib (0-100 μM; 72 hours) dihydrochloride inhibits the proliferation of multiple myeloma cell lines and induces apoptosis and cell cycle arrest. Its mechanism involves the inhibition of the STAT3 and JAK2 signaling pathways [1]. Radorinib (0-40 μM; 24 hours) dihydrochloride reduces the level of PrPSc in ZW13-2 neurons infected with 22L or 139A scrapie strains [2].
|
|---|---|
| ln Vivo |
Radotinib (100 mg/kg; intraperitoneal injection; once daily except weekends; 21 days) dihydrochloride exhibits antitumor activity in nude mouse models implanted with IM-9 cells[1]. Radotinib (100 mg/kg; gavage; 4–8 weeks) dihydrochloride prolongs the survival time of hamsters and reduces the deposition of PrPSc in hamsters infected with the 263K sheep scrapie strain[2].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: RPMI-8226, MM.1S, U266B1 and IM-9 cells Tested Concentrations: 0, 10, 50 and 100 μM Incubation Duration: 72 hours Experimental Results: Cell viability was inhibited in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models:Five-week-old male athymic nude mice were treated with IM-9 cells [1].
Doses: 100 mg/kg Route of Administration: Intraperitoneal injection; once daily except weekends; for 21 days. Experimental Results: Inhibited the growth of xenografted IM-9 cells in nude mice. Inhibited 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 tumor tissues. Significantly reduced the expression of phosphorylated STAT3-positive cells in tumor tissues. Significantly increased the number of TUNEL-positive cells in tumor tissues. |
| References |
|
| Molecular Formula |
C27H23CL2F3N8O
|
|---|---|
| Molecular Weight |
603.43
|
| CAS # |
926037-85-6
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(C1=CC=C(C)C(NC2=NC(C3=NC=CN=C3)=CC=N2)=C1)NC4=CC(C(F)(F)F)=CC(N5C=NC(C)=C5)=C4.Cl.Cl
|
| Synonyms |
IY-5511 dihydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6572 mL | 8.2860 mL | 16.5719 mL | |
| 5 mM | 0.3314 mL | 1.6572 mL | 3.3144 mL | |
| 10 mM | 0.1657 mL | 0.8286 mL | 1.6572 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.
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