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Ceranib-2 Sale

目录号 : GC15981

A ceramidase inhibitor

Ceranib-2 Chemical Structure

Cas No.:1402830-75-4

规格 价格 库存 购买数量
5mg
¥594.00
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10mg
¥1,089.00
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25mg
¥2,277.00
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50mg
¥3,762.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

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).

Chemical Properties

Cas No. 1402830-75-4 SDF
化学名 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
分子式 C25H19NO3 分子量 381.4
溶解度 ≤20mg/ml in DMSO;25mg/ml in dimethyl formamide 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.6219 mL 13.1096 mL 26.2192 mL
5 mM 0.5244 mL 2.6219 mL 5.2438 mL
10 mM 0.2622 mL 1.311 mL 2.6219 mL
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