Description
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.
Product information
CAS Number: 1402830-75-4
Molecular Weight: 381.42
Formula: C25H19NO3
Chemical Name: 3-[(2E)-3-(4-methoxyphenyl)prop-2-enoyl]-4-phenyl-1, 2-dihydroquinolin-2-one
Smiles: COC1C=CC(/C=C/C(=O)C2=C(C3=CC=CC=C3NC2=O)C2C=CC=CC=2)=CC=1
InChiKey: YIJGNIIQDRGGFT-DTQAZKPQSA-N
InChi: InChI=1S/C25H19NO3/c1-29-19-14-11-17(12-15-19)13-16-22(27)24-23(18-7-3-2-4-8-18)20-9-5-6-10-21(20)26-25(24)28/h2-16H,1H3,(H,26,28)/b16-13+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 50 mg/mL (131.09 mM; Need ultrasonic)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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.
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.
References:
- Draper JM, et al. Discovery and evaluation of inhibitors of human ceramidase. Mol Cancer Ther. 2011 Nov;10(11):2052-61.
- 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.
Products are for research use only. Not for human use.
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