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| Targets |
Ceranib-2 targets ceramidase enzymes, which are key regulators of sphingolipid metabolism. Ceramidases catalyze the conversion of ceramide to sphingosine, which is subsequently phosphorylated to sphingosine-1-phosphate (S1P). By inhibiting ceramidase, Ceranib-2 blocks this conversion, leading to the accumulation of ceramide species and decreased levels of sphingosine and S1P. This shift in the ceramide/S1P balance (the “ceramide/S1P rheostat”) has significant effects on cell proliferation, apoptosis, and survival. Ceranib-2 is a non-lipid inhibitor that avoids the off-target effects often associated with lipid-based ceramidase inhibitors.
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| ln Vitro |
Ceranib-2 treatment (10 nM-10 µM; 72 hours; SKOV3 cells) reduces the growth and/or survival of cells, with an IC50 value of 0.73 µM [1]. After 48 hours of treatment with ceretib-2 (0.75-1.5 µM; SKOV3 cells), cells accumulate in the sub-G1 (apoptotic), G2, and S (0.75 µM only) phases of the cell cycle, resulting in a drop in total cell quantity. G1 phase cells [1]. Ceranib-2 inhibits ceramidase activity in a dose-dependent manner, causing a 50% drop at 28 μM. It also induces the buildup of various ceramide species and lowers levels of sphingosine and S1P [1].
Ceranib-2 exhibits potent in vitro activity as a ceramidase inhibitor. It inhibits cellular ceramidase activity with an IC50 of 28 μM in SKOV3 cells. The compound increases intracellular accumulation of various ceramides, including C14 ceramide, and decreases levels of sphingosine and sphingosine-1-phosphate (S1P). These effects on sphingolipid metabolism confirm its mechanism of action as a ceramidase inhibitor. The compound is used in cancer biology to study the role of ceramide accumulation in apoptosis and tumor suppression. |
| ln Vivo |
Treatment with Ceranib-2 (20–50 mg/kg; i.p.; once daily, five days a week; for three weeks; female Balb/c mice) in syngeneic tumor models slows the growth of tumors without hematologic suppression or overt toxicity [1]. After administering 50 mg/kg of Ceranib-2 intraperitoneally, the levels gradually increased and at the 2-hour mark, the peak plasma concentration was approximately 40 μM. Ceranib-2's half-life of less than two hours suggests that it is removed [1].
In vivo activity of Ceranib-2 has been studied in animal models of cancer and other diseases. By inhibiting ceramidase and increasing ceramide levels, the compound promotes apoptosis and inhibits tumor growth. It has also been studied in models of inflammation and metabolic disease, where sphingolipid signaling plays a critical role. However, detailed in vivo efficacy data are less extensively documented compared to in vitro findings. The compound serves as a valuable pharmacological tool for understanding the role of ceramidase in various disease states. |
| Enzyme Assay |
In vitro enzyme assays for Ceranib-2 involve measuring its inhibition of ceramidase activity. These assays typically use cell lysates or recombinant ceramidase enzymes and a fluorogenic or radiolabeled ceramide substrate. The enzyme is incubated with the substrate and varying concentrations of Ceranib-2. The production of sphingosine or the decrease in ceramide is measured. The IC50 value (28 μM in SKOV3 cells) is determined from dose-response curves. These assays confirm that Ceranib-2 directly inhibits ceramidase activity.
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: SKOV3 Cell Tested Concentrations: 10 nM-10 µM Incubation Duration: 72 hrs (hours) Experimental Results: Ceranib-2 inhibits cell proliferation and/or survival with an IC50 value of 0.73 µM. Cell cycle analysis[1] Cell Types: SKOV3 Cell Tested Concentrations: 0.75 μM or 1.5 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induction of cell cycle arrest and cell death. In vitro cellular assays for Ceranib-2 are typically performed in cancer cell lines, particularly SKOV3 ovarian carcinoma cells. Cells are treated with Ceranib-2 at various concentrations for specified durations. Sphingolipid profiling is performed by LC-MS/MS to measure ceramide species, sphingosine, and S1P levels. Apoptosis is assessed using Annexin V staining or caspase activity assays. Cell proliferation is measured using MTT or CellTiter-Glo assays. These experiments confirm the compound’s mechanism of action and its effects on cell viability and sphingolipid metabolism. |
| Animal Protocol |
Animal/Disease Models: Female balb/c (Bagg ALBino) mouse were injected with JC mouse breast cancer cells [1]
Doses: 20 mg/kg or 50 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day, 5 days a week; for 3 weeks. Experimental Results: Same Delayed tumor growth in genetic tumor models. In vivo animal experiments with Ceranib-2 have been conducted in mouse models of cancer and other diseases. Tumor xenograft models are commonly used to evaluate the compound’s antitumor efficacy. Ceranib-2 is administered via intraperitoneal injection or oral gavage at varying doses. Tumor size is measured over time, and tumor tissues are harvested for sphingolipid profiling and histological analysis. Biomarkers such as ceramide, sphingosine, and S1P levels are measured in plasma and tissues to confirm target engagement. The compound’s effects on survival, tumor growth inhibition, and modulation of sphingolipid metabolism are evaluated. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for Ceranib-2 are limited. The compound has a molecular weight of 367.40 and is soluble in DMSO (40 mg/mL). It is typically stored as a powder at -20°C (3 years) or 4°C (2 years), and in solution at -80°C (6 months) or -20°C (1 month). Its bioavailability, half-life, and tissue distribution have not been extensively characterized. As a research compound, Ceranib-2 is primarily used in vitro and in cell-based assays. Further PK studies would be needed to support advanced preclinical development.
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| Toxicity/Toxicokinetics |
Toxicological data for Ceranib-2 are limited. The compound is intended for research use only and is not approved for human therapeutic use. In cell-based assays, Ceranib-2 has been used at concentrations up to 28 μM without significant cytotoxicity reported in some contexts. However, comprehensive toxicological evaluations have not been extensively published. The compound’s effects on sphingolipid metabolism suggest that it could have significant biological effects, and appropriate safety precautions should be taken when handling it in the laboratory.
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| References | |
| Additional Infomation |
Ceranib-2 is a potent and non-lipid ceramidase inhibitor used in sphingolipid research. It inhibits ceramidase activity with an IC50 of 28 μM in SKOV3 cells, increases ceramide accumulation, and decreases sphingosine and S1P levels. The compound is also known as 3-[(E)-3-(4-hydroxyphenyl)prop-2-enoyl]-4-phenyl-1H-quinolin-2-one. Ceranib-2 is used in cancer biology to study the role of ceramide accumulation in apoptosis and tumor suppression. It is also employed in inflammation and metabolic disease research to probe the ceramide/S1P rheostat. Ceranib-2’s non-lipid structure makes it a preferred tool over lipid-based inhibitors for many applications.
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| Molecular Formula |
C₂₅H₁₉NO₃
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|---|---|
| Molecular Weight |
381.42
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| Exact Mass |
381.136
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| CAS # |
1402830-75-4
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| Appearance |
White to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
629.2±55.0 °C at 760 mmHg
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| Flash Point |
334.4±31.5 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.657
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| LogP |
4.9
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| Synonyms |
Ceranib2; Ceranib 2
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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) |
DMSO : ~50 mg/mL (~131.09 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.55 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: 2.5 mg/mL (6.55 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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 | 2.6218 mL | 13.1089 mL | 26.2178 mL | |
| 5 mM | 0.5244 mL | 2.6218 mL | 5.2436 mL | |
| 10 mM | 0.2622 mL | 1.3109 mL | 2.6218 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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