Celecoxib

製品コードS1261 バッチS126105

印刷

化学情報

Chemical Structure Synonyms SC 58635 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C17H14F3N3O2S
分子量 381.37 CAS No. 169590-42-5
Solubility (25°C)* 体外 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 セレコキシブは、40nMのIC50による選択的なCOX-2阻害剤です。
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]

プロトコル(参考用のみ)

キナーゼアッセイ 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.
細胞アッセイ 細胞株 HNE1 and CNE1-LMP1
濃度 0-75 μM
反応時間 48 hours
実験の流れ

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.
動物実験 動物モデル 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.
投薬量 ≤200 mg/kg
投与方法 Administered via p.o.

カスタマーフィードバック

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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
Stress granules affect the sensitivity of renal cancer cells to sorafenib by sequestering and stabilizing COX‑2 mRNA [ Oncol Lett, 2023, 25(6):274] PubMed: 37216166
Cyclooxygenase‑2 contributes to the hypoxia‑induced aggravation of the neuroinflammation response stimulated by lipopolysaccharide in microglia [ Exp Ther Med, 2023, 25(3):123] PubMed: 36845947

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