Ceranib-2
Based on 1 Customer Validation
Ceranib-2 is a potent and nonlipid ceramidase inhibitor that inhibits cellular ceramidase activity with an IC50 of 28 μM in SKOV3 cells. Ceranib-2 induces the accumulation of multiple ceramide species, decreases levels of sphingosine and sphingosine-1-phosphate (S1P), and induces cell apoptosis. Anticancer activity.
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- Pureza: 98.92%
- No. CAS: 1402830-75-4
- Fòrmula: C25H19NO3
- Peso molecular:381.42
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Apoptosis Compound Library
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Actividad biológica
IC50: 28 μM (Ceramidase)[1]
Ceranib-2 (10 nM-10 μM; 72 hours; SKOV3 cells) treatment inhibits cell proliferation and/or survival with an IC50 value of 0.73 μM[1].
Ceranib-2 (0.75-1.5 μM; 48 hours; SKOV3 cells) treatment causes accumulation of cells in the sub-G1 (apoptosis), G2 and S (0.75 μM only) phases of the cell cycle, concomitant with reductions in the number of cells in G1 phase[1].
Ceranib-2 produces a dose-dependent decrease in ceramidase activity, with 50% inhibition at 28 μM, induces the accumulation of multiple ceramide species, and decreases levels of sphingosine and S1P[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SKOV3 cells
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Concentration:10 nM-10 µM
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Incubation Time:72 hours
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Result:Cell proliferation and/or survival were inhibited with an IC50 value of 0.73 μM for Ceranib-2.
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Cell Line:SKOV3 cells
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Concentration:0.75 μM, or 1.5 μM
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Incubation Time:48 hours
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Result:Induced cell-cycle arrest and cell death.
Intraperitoneal administration of 50 mg/kg Ceranib-2 results in progressive increases in its circulating levels, reaching a peak plasma concentration of approximately 40 μM at the 2 hr time point. Ceranib-2 appears to be cleared with a half-life of less than 2 hr[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Balb/c mice injected with JC murine mammary adenocarcinoma cells[1]
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Dosage:20 mg/kg or 50 mg/kg
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Administration:Intraperitoneal injection; daily for 5 days per week; for 3 weeks
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Result:Delayed tumor growth in a syngeneic tumor model.
Chemical Information
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No. CAS 1402830-75-4
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Appearance Solid
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Peso molecular 381.42
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Fòrmula C25H19NO3
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Color White to yellow
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SMILES
O=C1NC(C=CC=C2)=C2C(C3=CC=CC=C3)=C1C(/C=C/C4=CC=C(C=C4)OC)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
DMSO : 50 mg/mL (131.09 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.55 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Draper JM, et al. Discovery and evaluation of inhibitors of human ceramidase. Mol Cancer Ther. 2011 Nov;10(11):2052-61. [Content Brief]
[2]. Kus G, et al. Induction of apoptosis in prostate cancer cells by the novel ceramidase inhibitor ceranib-2. In Vitro Cell Dev Biol Anim. 2015 Nov;51(10):1056-63. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6218 mL | 13.1089 mL | 26.2178 mL | 65.5445 mL |
| 5 mM | 0.5244 mL | 2.6218 mL | 5.2436 mL | 13.1089 mL | |
| 10 mM | 0.2622 mL | 1.3109 mL | 2.6218 mL | 6.5545 mL | |
| 15 mM | 0.1748 mL | 0.8739 mL | 1.7479 mL | 4.3696 mL | |
| 20 mM | 0.1311 mL | 0.6554 mL | 1.3109 mL | 3.2772 mL | |
| 25 mM | 0.1049 mL | 0.5244 mL | 1.0487 mL | 2.6218 mL | |
| 30 mM | 0.0874 mL | 0.4370 mL | 0.8739 mL | 2.1848 mL | |
| 40 mM | 0.0655 mL | 0.3277 mL | 0.6554 mL | 1.6386 mL | |
| 50 mM | 0.0524 mL | 0.2622 mL | 0.5244 mL | 1.3109 mL | |
| 60 mM | 0.0437 mL | 0.2185 mL | 0.4370 mL | 1.0924 mL | |
| 80 mM | 0.0328 mL | 0.1639 mL | 0.3277 mL | 0.8193 mL | |
| 100 mM | 0.0262 mL | 0.1311 mL | 0.2622 mL | 0.6554 mL |
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