| Identification | Back Directory | [Name]
3-[3-(4-Methoxyphenyl)-1-oxo-2-propen-1-yl]-4-phenyl-2(1H)-quinolinone | [CAS]
1402830-75-4 | [Synonyms]
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- | [EINECS(EC#)]
802-692-7 | [Molecular Formula]
C25H19NO3 | [MDL Number]
MFCD25977826 | [MOL File]
1402830-75-4.mol | [Molecular Weight]
381.42 |
| Hazard Information | Back Directory | [Description]
Ceranib-2 is a ceramidase inhibitor that inhibits ceramidase activity (IC50 = 28 μM in SKOV3 cells). It also increases intracellular accumulation of various ceramides, including C14 ceramide , C24 ceramide , C26 ceramide, and C26:1 ceramide, and total ceramide levels and decreases levels of dihydrosphingosine, sphingosine, and sphingosine-1-phosphate in SKOV3 cells. In vivo, ceranib-2 (20 and 50 mg/kg, i.p.) reduces tumor volume in a JC mammary adenocarcinoma mouse syngeneic tumor model. | [Uses]
Ceranib-2 is a potent and nonlipid ceramidase inhibitor that inhibits cellular ceramidase activity with an IC50 of 28 μM in SKOV3 cells. Ceranib-2 induces the accumulation of multiple ceramide species, decreases levels of sphingosine and sphingosine-1-phosphate (S1P), and induces cell apoptosis. Anticancer activity[1][2]. | [in vivo]
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[1].
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[1]. | Animal Model: | Female Balb/c mice injected with JC murine mammary adenocarcinoma cells[1] | | 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.
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| [References]
[1] Draper JM, et al. Discovery and evaluation of inhibitors of human ceramidase. Mol Cancer Ther. 2011 Nov;10(11):2052-61. DOI:10.1158/1535-7163.MCT-11-0365
[2] Kus G, et al. Induction of apoptosis in prostate cancer cells by the novel ceramidase inhibitor ceranib-2. In Vitro Cell Dev Biol Anim. 2015 Nov;51(10):1056-63. DOI:10.1007/s11626-015-9932-9 |
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