Celecoxib (SC-58635)

N.º de catálogoS1261 Lote:S126107

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Datos técnicos

Fórmula

C17H14F3N3O2S
Peso molecular 381.37 Número CAS 169590-42-5
Solubilidad (25°C)* In vitro DMSO 76 mg/mL (199.28 mM)
Ethanol 38 mg/mL (99.64 mM)
Water Insoluble
In vivo (Agregue los solventes al producto individualmente y en orden.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
10% DMSO 40% PEG 300 5%Tween80 45% water

Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, póngase en contacto con nuestro equipo de ventas para pruebas personalizadas.

 5.000mg/ml (13.11mM) Taking the 1 mL working solution as an example, add 100 μL of 50 mg/ml clear DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue adding Dilute 450 μL ddH2O to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
10% DMSO 90% corn oil

Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, póngase en contacto con nuestro equipo de ventas para pruebas personalizadas.

 0.400mg/ml (1.05mM) Taking the 1 mL working solution as an example, add 100 μL of 4 mg/ml clear DMSO stock solution to 900 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml significa ligeramente soluble o insoluble.
* Tenga en cuenta que Selleck prueba la solubilidad de todos los compuestos internamente, y la solubilidad real puede diferir ligeramente de los valores publicados. Esto es normal y se debe a ligeras variaciones entre lotes.
* Envío a temperatura ambiente (Las pruebas de estabilidad demuestran que este producto se puede enviar sin medidas de refrigeración.)

Preparación de soluciones madre

Actividad biológica

Descripción Celecoxib es un inhibidor selectivo de la COX-2 con una IC50 de 40 nM en células Sf9.
Objetivos
COX-2
(Sf9 cells)
40 nM
In vitro

Celecoxib muestra baja sensibilidad contra COX-1 con una IC50 de 15 μM. Este compuesto muestra un efecto antiproliferativo en líneas celulares de carcinoma nasofaríngeo (NPC) incluyendo HNE1 y CNE1-LMP1 con una IC50 de 32,86 μM y 61,31 μM, respectivamente.

In vivo

Celecoxib exhibe una potente actividad antiinflamatoria oral. Este compuesto reduce la inflamación aguda en el ensayo de edema por carragenina y la inflamación crónica en el modelo de artritis adyuvante con una ED50 de 7,1 mg/kg y 0,37 mg/kg/día, respectivamente. Además, también exhibe actividad analgésica en el modelo de hiperalgesia de Hargreaves con una ED50 de 34,5 mg/kg. Asimismo, este producto químico no produce toxicidad gastrointestinal aguda en ratas a dosis de hasta 200 mg/kg y no produce toxicidad gastrointestinal crónica en ratas a dosis de hasta 600 mg/kg/día durante 10 días. En un modelo de ratón hembra C3Hf/KamLaw, aumenta el tiempo de supervivencia medio de 105 días (rango, 79-145 días) después de 13,5 Gy de irradiación torácica local (LTI) sola a 142 días (rango, 94-155 días).

Protocolo (de referencia)

Ensayo de quinasa:

[1]
  • Ensayo enzimático de COX in vitro

    La expresión de la proteína COX en células de insecto se determina evaluando la capacidad de síntesis de PG en homogeneizados de células incubadas durante 3 días con baculovirus COX-1 o COX-2. Las células que expresan COX-1 o COX-2 se homogeneizan y se incuban con ácido araquidónico (10 μM). La actividad de la COX se determina monitorizando la producción de PG. No se detecta actividad de la COX en células Sf9 infectadas de forma simulada. Este compuesto se preincuba con homogeneizados brutos de CHAPS al 1 % (2-10 μg de proteína) durante 10 minutos antes de la adición de ácido araquidónico. El PGE2 formado se detecta mediante ELISA después de 10 minutos de incubación.
Ensayo celular:

[2]
  • Líneas celulares

    HNE1 and CNE1-LMP1

  • Concentraciones

    0-75 μM

  • Tiempo de incubación

    48 hours

  • Método

    The antiproliferative effect of Celecoxib on NPC cells is assessed using an MTT assay. Cells are seeded into 96-well plates and allowed to attach for 24 hours. The cells are then treated with increasing concentrations of this compound (0 to 75 μM) dissolved in DMSO (final concentration ≤0.1%) and incubated for up to 48 hours. After the incubation, 20 μL of MTT dye (5 mg/mL) are added to each well and cells are incubated at 37 °C for 4 hours. After removing the supernatants, the crystals are dissolved in DMSO and the absorbance is measured at 490 nm. The half-maximal inhibitory concentration (IC50) values and the 95% confidence intervals are calculated using probit regression using SPSS 15.0 software. The experiment is performed in triplicate and repeated at least three times.
Estudio en animales:

[1]
  • Modelos animales

    A 0.1 mL aliquot of a 1% solution of carrageenan in 0.9% sterile saline or 1 mg of Mycobacterium butyricum in 50 μL of mineral oil is administered to the right hind foot pad of male Sprague−Dawley rats.

  • Dosificaciones

    ≤200 mg/kg

  • Administración

    Administered via p.o.

Referencias

  • https://pubmed.ncbi.nlm.nih.gov/9135032/
  • https://pubmed.ncbi.nlm.nih.gov/22504904/
  • https://pubmed.ncbi.nlm.nih.gov/22672748/

Validación de productos por parte del cliente

<p>Reduced hepatic lipid contents and alleviated liver injury in EC-AMPK mice treated with selective COX-2 inhibitors. Wild-type and EC-AMPK mice given a high fat diet were treated with vehicle, celecoxib or nimesulide for a period of 4 weeks. At the end of treatment, parameters including body weight and circulating glucose (A), serum triglyceride and cholesterol levels (B were measured and presented as percentage comparisons against those from vehicle-treated wild-type mice. *<em>P</em> < 0.05 versus wild-type mice treated with vehicle; #<em>P</em> < 0.05 versus EC-AMPK mice treated with vehicle, <em>n</em> = 3-5.</p>

Datos de [ Br J Pharmacol , 2014 , 171(2), 498-508 ]

Breast cancer cells, wild type (WT) or anoikis resistant (AR) variants, were treated with celecoxib (CEL 5.0 uM) and/or sildenafil (SIL, 2.0 uM). Cells were isolated after 24h and viability determined by trypan blue exclusion (n = 3, +/- SEM) * p < 0.05 greater than corresponding value in vehicle control. Upper inset pictures: HCC38 cells in 96 well plates were treated with celecoxib (CEL 5.0 uM) and/or sildenafil (SIL, 2.0 uM). Cells were isolated after 24h and viability determined using a live-dead assay (red cells = dead; green cells = alive) (n = 3, +/- SEM) * p < 0.05 greater than corresponding value in vehicle control.

Datos de [ J Cell Physiol , 2014 , 10.1002/jcp.24843 ]

Tumors were resected from mice 10 days after orthotopic inoculation of 4T1-Luc2 cells, and hydrogels loaded with the following payloads were evaluated: anti–PD-1, anti-CTLA-4, IL-15sa, lenalidomide, celecoxib, STING-RR, or R848. Mice that did not receive a hydrogel were examined as a negative control. (A) IVIS imaging of 4T1-Luc2 cells is shown for all groups described and illustrates tumor burden.

Datos de [ , , Science, 2018, 10(433), doi: 10.1126/scitranslmed.aar1916 ]

Effect of celecoxib on the in vitro proliferation of BRAFV600E and NRASQ61R melanoma cell lines. a BRAFV600E A375 and NRASQ61R SK-MEL-2 melanoma cells were seeded at the density of 3 × 10<sup>3</sup> per well in a 96-well plate and incubated with the indicated concentrations of celecoxib. Untreated cells were used as a control. DMSO (vehicle of celecoxib) concentration was maintained at 0.02% in all wells. Following a 24 h incubation at 37℃ in a 5% CO2 atmosphere, growth inhibition was determined by MTT assay. Data are expressed as mean percent of proliferation ± SD of treated cells as compared to untreated control cells. Mean percent of proliferation and SD were calculated from three independent experiments performed in triplicate. Difference between doses of celecoxib was calculated using unpaired t-test. *** indicate P < 0.001. b BRAFV600E A375 and NRASQ61R SK-MEL-2 melanoma cells were seeded at the density of 4 × 10<sup>5</sup> per well in a 75 cm<sup>2</sup> tissue culture flask and incubated with celecoxib (60 μM). Untreated cells were used as a control. DMSO (vehicle of celecoxib) concentration was maintained at 0.02% in all wells. Following a 24 h incubation at 37℃ in a 5% CO2 atmosphere, viability of cells was determined by trypan blue assay. Data are expressed as mean percentage of viable (negative) and death cells (positive) of treated cells as compared to untreated control cells. *** indicate P < 0.001

Datos de [ , , J Transl Med, 2017, 15(1):46 ]

Sellecks Celecoxib (SC-58635) Ha sido citado por 115 Publicaciones

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Missense Mutant p53 Transactivates Wnt/β-Catenin Signaling in Neighboring p53-Destabilized Cells through the COX-2/PGE2 Pathway [ Cancer Res Commun, 2025, 5(1):13-23] PubMed: 39641656
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Celecoxib Combined with Tocilizumab Has Anti-Inflammatory Effects and Promotes the Recovery of Damaged Cartilage via the Nrf2/HO-1 Pathway In Vitro [ Biomolecules, 2024, 14(12)1636] PubMed: 39766343

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