Ceranib-2 是一种有效的非脂质神经酰胺酶 (ceramidase) 抑制剂，可在 SKOV3 细胞中抑制细胞神经酰胺酶活性，IC50为 28 μM。Ceranib-2 可诱导多种神经酰胺物质的积累，降低鞘氨醇和鞘氨醇1-磷酸 (S1P) 的水平，并诱导细胞凋亡 (apoptosis)。抗癌活性。
| 生物活性 | Ceranib-2 is a potent and nonlipidceramidaseinhibitor that inhibits cellularceramidaseactivity with anIC50of 28 μM in SKOV3 cells. Ceranib-2 induces the accumulation of multiple ceramide species, decreases levels of sphingosine andsphingosine-1-phosphate (S1P), and induces cellapoptosis. Anticancer activity[1][2]. |
| IC50& Target | IC50: 28 μM (Ceramidase)[1] |
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 IC50value of 0.73 μM[1].
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[1].
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[1].
Cell Proliferation Assay[1] | Cell Line: | SKOV3 cells | | Concentration: | 10 nM-10 μM | | Incubation Time: | 72 hours | | Result: | Cell proliferation and/or survival were inhibited with an IC50value of 0.73 μM for Ceranib-2. |
Cell Cycle Analysis[1] | Cell Line: | SKOV3 cells | | Concentration: | 0.75 μM, or 1.5 μM | | Incubation Time: | 48 hours | | Result: | Induced cell-cycle arrest and cell death. |
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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[1].
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[1].
| Animal Model: | Female Balb/c mice injected with JC murine mammary adenocarcinoma cells[1] | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(131.09 mM;Need ultrasonic) 配制储备液 | 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 |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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. 请依序添加每种溶剂： 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。 2. 请依序添加每种溶剂： 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。 *以上所有助溶剂都可在本网站选购。
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