Ceranib-2

SKU: orb1940808

Description

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.

Key Properties

• CAS Number: 1402830-75-4
• MW: 381.431
• Purity: >98% (HPLC)
• Formula: C₂₅H₁₉NO₃
• SMILES: COc1ccc(\C=C\C(=O)c2c(-c3ccccc3)c3ccccc3[nH]c2=O)cc1
• Target: Apoptosis
• Solubility: In Vitro: DMSO : 50 mg/mL (131.09 mM)

Bioactivity

• 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. 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.
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• 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. 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

3-[(E)-3-(4-hydroxyphenyl)prop-2-enoyl]-4-phenyl-1H-quinolin-2-one

Quick Database Links

Gene Symbol

Apoptosis