Celecoxib

Catalog No.S1261 Batch:S126104

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Technical Data

Formula

C17H14F3N3O2S

Molecular Weight 381.37 CAS No. 169590-42-5
Solubility (25°C)* In vitro DMSO 76 mg/mL (199.28 mM)
Ethanol 76 mg/mL (199.28 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Celecoxib is a selective COX-2 inhibitor with IC50 of 40 nM in Sf9 cells.
Targets
COX-2 [1]
(Sf9 cells)
40 nM
In vitro

Celecoxib shows low sensitivity against COX-1 with IC50 of 15 μM. [1] Celecoxib shows an anti-proliferative effect on nasopharyngeal carcinoma (NPC) cell lines including HNE1 and CNE1-LMP1 with IC50 of 32.86 μM and 61.31 μM, respectively. [2]

In vivo

Celecoxib exhibits a potent, oral anti-inflammatory activity. Celecoxib reduces acute inflammation in the carrageenan edema assay and chronic inflammation in the adjuvant arthritis model with ED50 of 7.1 mg/kg and 0.37 mg/kg/day, respectively. In addition, Celecoxib also exhibits analgesic activity in the Hargreaves hyperalgesia model with ED50 of 34.5 mg/kg. Besides, Celecoxib produces no acute GI toxicity in rats at doses up to 200 mg/kg and no chronic GI toxicity in rats at doses up to 600 mg/kg/day over 10 days. [1] In a C3Hf/KamLaw female mouse model, Celecoxib increases median survival time of 105 days (range, 79-145 days) after 13.5 Gy local thoracic irradiation (LTI) alone to 142 days (range, 94-155 days). [3]

Protocol (from reference)

Kinase Assay:

[1]

  • COX enzyme assay in vitro

    Expression of COX protein in insect cells is determined by assessing PG-synthetic capability in homogenates from cells incubated for 3 days with COX-1 or COX-2 baculovirus. Cells expressing COX-1 or COX-2 are homogenized and incubated with arachidonic acid (10 μM). COX activity is determined by monitoring PG production. No COX activity is detected in mock-infected Sf9 cells. Celecoxib are preincubated with crude 1% CHAPS homogenates (2-10 μg of protein) for 10 minutes before addition of arachidonic acid. PGE2 formed is detected by ELISA after 10 minute incubation.

Cell Assay:

[2]

  • Cell lines

    HNE1 and CNE1-LMP1

  • Concentrations

    0-75 μM

  • Incubation Time

    48 hours

  • Method

    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 Celecoxib (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.

Animal Study:

[1]

  • Animal Models

    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.

  • Dosages

    ≤200 mg/kg

  • Administration

    Administered via p.o.

Customer Product Validation

Data from [Br J Pharmacol, 2014, 171(2), 498-508]

Data from [Data independently produced by J Cell Physiol, 2014, 10.1002/jcp.24843]

Data from [Data independently produced by , , Science, 2018, 10(433), doi: 10.1126/scitranslmed.aar1916]

Data from [Data independently produced by , , J Transl Med, 2017, 15(1):46]

Selleck's Celecoxib has been cited by 107 publications

Leptin-mediated suppression of lipoprotein lipase cleavage enhances lipid uptake and facilitates lymph node metastasis in gastric cancer [ Cancer Commun (Lond), 2024, 10.1002/cac2.12583] PubMed: 38958445
Therapeutic Anti-Tumor Efficacy of DC-Based Vaccines Targeting TME-Associated Antigens Is Improved When Combined with a Chemokine-Modulating Regimen and/or Anti-PD-L1 [ Vaccines (Basel), 2024, 12(7)777] PubMed: 39066414
Modulation of autophagy and apoptosis can contribute to the anticancer effect of Abemaciclib/Celecoxib combination in colon cancer cells [ Med Oncol, 2024, 41(2):43] PubMed: 38170401
A reversible SRC-relayed COX2 inflammatory program drives resistance to BRAF and EGFR inhibition in BRAFV600E colorectal tumors [ Nat Cancer, 2023, 4(2):240-256] PubMed: 36759733
MFSD2A potentiates gastric cancer response to anti-PD-1 immunotherapy by reprogramming the tumor microenvironment to activate T cell response [ Cancer Commun (Lond), 2023, 10.1002/cac2.12476] PubMed: 37539769
Upregulation of β-catenin signaling represents a single common pathway leading to the various phenotypes of spinal degeneration and pain [ Bone Res, 2023, 11(1):18] PubMed: 37059724
25-hydroxyvitamin D3 generates immunomodulatory plasticity in human periodontal ligament-derived mesenchymal stromal cells that is inflammatory context-dependent [ Front Immunol, 2023, 14:1100041] PubMed: 36761739
COX-2/PGE2 upregulation contributes to the chromosome 17p-deleted lymphoma [ Oncogenesis, 2023, 12(1):5] PubMed: 36750552
Phospholipid metabolic adaptation promotes survival of IDH2 mutant acute myeloid leukemia cells [ Cancer Sci, 2023, 10.1111/cas.15994] PubMed: 37882467
Aristolochic acid induces an inflammatory response with prostaglandin E2 production and apoptosis in NRK-52E proximal tubular cells [ Toxicol Lett, 2023, 378:39-50] PubMed: 36863539

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