Ceranib-2

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. (In Vitro) :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. (In Vivo) :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.