1402830-75-4
1402830-75-4 結構式
基本信息
化合物CERANIB-2
3-[3-(4-Methoxyphenyl)-1-oxo-2-propenyl]-4-phenyl-2(1H)-quinolinone
3-[3-(4-Methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-2(1H)-quinolinone
2(1H)-Quinolinone, 3-[3-(4-methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-
常見問題列表
IC50: 28 μM (Ceramidase)
Ceranib-2 (10 nM-10 μM; 72 hours; SKOV3 cells) treatment inhibits cell proliferation and/or survival with an IC
50
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.
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 IC 50 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. |
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.
| 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. |