网站主页 >> CAS数据库列表 >> 3-[3-(4-Methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-2(1H)-quinolinone
3-[3-(4-Methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-2(1H)-quinolinone
|
|
|
- CAS号:
- 1402830-75-4
- 英文名:
- 3-[3-(4-Methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-2(1H)-quinolinone
- 英文别名:
- Ceranib-2 >=98% (HPLC);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-
- 中文名:
- 3-[3-(4-Methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-2(1H)-quinolinone
- 中文别名:
- 化合物 T10761;化合物CERANIB-2
- CBNumber:
- CB22715575
- 分子式:
- C25H19NO3
- 分子量:
- 381.42326
- MOL File:
- 1402830-75-4.mol
|
|
|
3-[3-(4-Methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-2(1H)-quinolinone化学性质
-
储存条件:
-
-20°C
-
|
-
溶解度:
-
DMSO: soluble20mg/mL, clear
-
|
-
形态:
-
powder
-
|
-
颜色:
-
white to beige
-
|
3-[3-(4-Methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-2(1H)-quinolinone性质、用途与生产工艺
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。
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.
|
3-[3-(4-Methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-2(1H)-quinolinone
上下游产品信息
上游原料
下游产品
3-[3-(4-Methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-2(1H)-quinolinone
生产厂家
1402830-75-4, 3-[3-(4-Methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-2(1H)-quinolinone 相关搜索:
- 化合物CERANIB-2
- 化合物 T10761
- 1402830-75-4
- Ceranib-2 >=98% (HPLC)
- 2(1H)-Quinolinone, 3-[3-(4-methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-
- 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