CAS NO: | 1402830-75-4 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 381.4 |
Cas No. | 1402830-75-4 |
Formula | C25H19NO3 |
Solubility | ≤20mg/ml in DMSO;25mg/ml in dimethyl formamide |
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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
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).