1. GPCR/G Protein
    Apoptosis
  2. LPL Receptor
    Apoptosis
  3. Ceranib-2

Ceranib-2 

Cat. No.: HY-116147
Handling Instructions

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.

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Ceranib-2 Chemical Structure

Ceranib-2 Chemical Structure

CAS No. : 1402830-75-4

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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[1][2].

IC50 & Target

IC50: 28 μM (Ceramidase)[1]

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[1].
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[1].
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[1].

Cell Proliferation Assay[1]

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[1]

Cell Line: SKOV3 cells
Concentration: 0.75 μM, or 1.5 μM
Incubation Time: 48 hours
Result: Induced cell-cycle arrest and cell death.
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.
Molecular Weight

381.42

Formula

C₂₅H₁₉NO₃

CAS No.

1402830-75-4

SMILES

O=C1NC(C=CC=C2)=C2C(C3=CC=CC=C3)=C1C(/C=C/C4=CC=C(C=C4)OC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

Ceranib-2Ceranib2Ceranib 2LPL ReceptorApoptosisLysophospholipid ReceptorCeramideS1Pnonlipidanticancersphingosineanti-proliferationcellularpromoteapoptosisInhibitorinhibitorinhibit

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