Ceranib-2|1402830-75-4|-陌孚医药/Medlife

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Ceranib-2

目录号: PC15330 纯度: ≥98%

CAS No. :1402830-75-4

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中文名称

Ceranib-2

英文名称

Ceranib-2

英文别名

3-[3-(4-Methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-2(1H)-quinolinone;3-[3-(4-Methoxyphenyl)-1-oxo-2-propenyl]-4-phenyl-2(1H)-quinolinone

Cas No.

1402830-75-4

分子式

C₂₅H₁₉NO₃

分子量

381.42

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

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.

性状

Solid

IC50 & Target[1][2]

IC50: 28 μM (Ceramidase)

体外研究(In Vitro)

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.
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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	SKOV3 cells
Concentration:	10 nM-10 μM
Incubation Time:	72 hours
Result:	Cell proliferation and/or survival were inhibited with an IC₅₀ value of 0.73 μM for Ceranib-2.

Cell Cycle Analysis

Cell Line:	SKOV3 cells
Concentration:	0.75 μM, or 1.5 μM
Incubation Time:	48 hours
Result:	Induced cell-cycle arrest and cell death.

体内研究(In Vivo)

Ceranib-2 (20-50 mg/kg; intraperitoneal injection; daily for 5 days per week; for 3 weeks; female Balb/c mice) treatment delays tumor growth in a syngeneic tumor model without hematologic suppression or overt signs of toxicity.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female Balb/c mice injected with JC murine mammary adenocarcinoma cells
Dosage:	20 mg/kg or 50 mg/kg
Administration:	Intraperitoneal injection; daily for 5 days per week; for 3 weeks
Result:	Delayed tumor growth in a syngeneic tumor model.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Draper JM, et al. Discovery and evaluation of inhibitors of human ceramidase. Mol Cancer Ther. 2011 Nov;10(11):2052-61. [Information]

[2]. Kus G, et al. Induction of apoptosis in prostate cancer cells by the novel ceramidase inhibitor ceranib-2. 体外研究 Cell Dev Biol Anim. 2015 Nov;51(10):1056-63. [Information]

溶解度数据

体外研究:

DMSO : 50 mg/mL (131.09 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.5 mg/mL (6.55 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.55 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: 2.5 mg/mL (6.55 mM); Clear solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.55 mM) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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