Ceranib-2

Research use only, not for human use.

Ceranib-2 is an inhibitor of ceramidase with an IC50 of 28 μM in SKOV3 cells.

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.

Ceranib-2 (10 nM-10 μM; 72 hours; SKOV3 cells) treatment inhibits cell proliferation and/or survival with an IC50 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 IC50 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-[(E)-3-(4-hydroxyphenyl)prop-2-enoyl]-4-phenyl-1H-quinolin-2-one

Apoptosis

Apoptosis

PEGs

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1402830-75-4

381.431

C25H19NO3

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (131.09 mM)

COc1ccc(\C=C\C(=O)c2c(-c3ccccc3)c3ccccc3[nH]c2=O)cc1

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(-20℃)

With Ice Pack

≥ 2 years