| Ceranib-2inhibitor of cellular ceramidase activity |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 1402830-75-4 | SDF | Download SDF |
| Chemical Name | 3-[3-(4-methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-2(1H)-quinolinone | ||
| Canonical SMILES | O=C(N1)C(C(/C=C/C2=CC=C(OC)C=C2)=O)=C(C3=CC=CC=C3)C4=C1C=CC=C4 | ||
| Formula | C25H19NO3 | M.Wt | 381.4 |
| Solubility | ≤20mg/ml in DMSO;25mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 28 μM
Ceranib-2 is an inhibitor of cellular ceramidase activity.
Ceramidase catalyzes the hydrolysis of the N-acyl linkage between the fatty acid and sphingosine base in ceramide to produce sphingosine and a free fatty acid. Ceramidase plays a key role in regulating cell fate and its inhibition in both malignant and non-cancerous cells results in apoptosis.
In vitro: In a previous study, a more potent analogue (Ceranib-2) of novel ceramidase inhibitor (Ceranib-1) was identified by screening a small molecule library. In a cell-based assay, both Ceranib-1 and Ceranib-2 were able to inhibit cellular ceramidase activity, decrease levels of sphingosine and S1P, inhibit the proliferation of cells alone and, induce the accumulation of multiple ceramide species, and induce cell-cycle arrest and death in combination with paclitaxel [1].
In vivo: In a previous study, Ceranib-2 was given by i.p. injection on 5 days per week. Resutls showed that the average normalized size of tumors in each treatment group increased over time. However, by day 11 Ceranib-2-treated groups had significantly lower tumor volumes. By day 21, the average normalized tumor volumes for the control, 20 mg/kg and 50 mg/kg Ceranib-2 groups were 1,400, 940, and 710, respectively. In addition, the administration of Ceranib-2 did not alter the total body weight of the mice [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:[1] Draper, J.M.,Xia, Z.,Smith, R.A., et al. Discovery and evaluation of inhibitors of human ceramidase. Molecular Cancer Therapeutics 1-27 (2011).
