Ceranib-2 是一种神经酰胺酶抑制剂,在 SKOV3 细胞中的 IC50 为 28 μM。 Ceranib-2 降低鞘氨醇和 S1P 的水平,诱导细胞凋亡并表现出抗癌活性。
产品描述
Ceranib-2 is an inhibitor of ceramidase with an IC50 of 28 μM in SKOV3 cells. Ceranib-2 decreases levels of sphingosine and S1P, induces cell apoptosis and exhibits anticancer activity.
体外活性
In SKOV3 cells, Ceranib-2 (28 μM) decreases with 50% inhibition and induces the accumulation of multiple ceramide species. Ceranib-2 (10 nM-10 μM) inhibits cell proliferation and survival with an IC50 value of 0.73 μM. Ceranib-2 (0.75-1.5 μM) accumulates cells in the sub-G1. G2 and S phases of the cell cycle are concomitantly reduced in the number of cells in the G1 phase at the dose of 0.75 μM[1].
体内活性
In female Balb/c mice, Ceranib-2 (20-50 mg/kg; i.p.) delays tumor growth without hematologic suppression in a syngeneic tumor model. Ceranib-2 (50 mg/kg; i.p.) increases the circulating levels, reaching a peak plasma concentration of approximately 40 μM at 2 hr[1].
Cas No.
1402830-75-4
分子式
C25H19NO3
分子量
381.42
别名
3-[(E)-3-(4-hydroxyphenyl)prop-2-enoyl]-4-phenyl-1H-quinolin-2-one
储存和溶解度
DMSO:40 mg/mL (104.9 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years