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

Ceranib-2 

Cat. No.: HY-116147 Purity: 99.25%
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.

For research use only. We do not sell to patients.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (131.09 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6218 mL 13.1089 mL 26.2178 mL
5 mM 0.5244 mL 2.6218 mL 5.2436 mL
10 mM 0.2622 mL 1.3109 mL 2.6218 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (6.55 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: 2.5 mg/mL (6.55 mM); Clear solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Keywords:

Ceranib-2Ceranib2Ceranib 2LPL ReceptorApoptosisLysophospholipid ReceptorCeramideS1Pnonlipidanticancersphingosineanti-proliferationcellularpromoteapoptosisInhibitorinhibitorinhibit

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Ceranib-2
Cat. No.:
HY-116147
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