Celecoxib
(Synonyms: 塞来昔布; SC 58635) 目录号 : GC14475Celecoxib是一种高度选择性的环氧合酶-2(COX-2)抑制剂,IC50值为40nM。
Cas No.:169590-42-5
Sample solution is provided at 25 µL, 10mM.
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- Purity: >99.50%
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- SDS (Safety Data Sheet)
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Cell experiment [1]: | |
Cell lines | Tendon cells |
Preparation Method | Cells were first seeded into 24-well flat-bottomed culture plates. Celecoxib was then added to the culture dish at dosages of 0, 0.8, 2.0, 4.0, and 8.0µg/mL. Then 24h after Celecoxib was added to cells, cells were observed under microscope and then MTT assay was performed. |
Reaction Conditions | 0.8, 2.0, 4.0, 8.0µg/mL; 24h |
Applications | Celecoxib dose-dependently inhibited tendon cell viability and migration, but no cell necrosis or changes in cell morphology were observed. |
Animal experiment [2]: | |
Animal models | Female BALB/c nude mice |
Preparation Method | Mice were randomly divided into the following five treatment groups: control; mice were injected with PGE2 (1mg/kg); mice were injected with PGE2 (1mg/kg) and Celecoxib (100mg/kg); mice received pneumonectomy; mice received pneumonectomy and Celecoxib (100mg/kg). A549 cells were prepared as a suspension of 106 cells in 150µL saline and injected using a 29-gauge needle into the lateral tail vein under sterile conditions. Celecoxib (100mg/kg) was administered orally starting from the day before tumor cell injection until the mice were sacrificed. After the mice were sacrificed, the lungs were flushed with 5% picric acid solution. Lung metastasis was determined by counting the total number of metastatic nodules in each lung. |
Dosage form | 100mg/kg; p.o. |
Applications | The metastasis of A549 cells in mice receiving unilateral pneumonec tomy was more than that in control mice, and treatment with Celecoxib inhibited this increase in metastases. The mean level of plasma PGE2 in mice receive ing unilateral pneumonectomy increased, and treatment with Celecoxib significantly inhibited the increase in PGE2 plasma level. |
References: |
Celecoxib is a highly selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 value of 40nM[1]. Celecoxib is a selective nonsteroidal anti-inflammatory drug (NSAID) commonly used to treat acute pain, osteoarthritis (OA), rheumatoid arthritis (RA), juvenile rheumatoid arthritis and ankylosing spondylitis (AS)[2]. Celecoxib has strong anti-tumor activity and can prevent and treat a variety of cancers such as pancreatic cancer, breast cancer, ovarian cancer, and non-small cell lung cancer[3]. Celecoxib can prevent the occurrence of colorectal adenomatous polyps[4].
In vitro, Celecoxib (0.8, 2.0, 4.0, 8.0µg/mL) treated tenocytes for 24h dose-dependently inhibited cell viability and migration, but did not change cell morphology or cause cell necrosis[5]. Celecoxib (1-100μM) treated human osteoblasts for 24h, inhibited cell proliferation in a dose-dependent manner and caused an increase in intracellular Ca2+ concentration[6].
In vivo, Celecoxib (100mg/kg) was orally administered to mice with lung cancer model and unilateral lung resection, inhibiting lung cancer metastasis and the increase in plasma PGE2 levels[7]. Celecoxib (10, 20mg/kg) was orally administered to rats with gastric cancer model, significantly reducing the incidence and growth of gastric cancer in rats[8].
References:
[1] Cao H, Yu R, Choi Y, et al. Discovery of cyclooxygenase inhibitors from medicinal plants used to treat inflammation[J]. Pharmacological research, 2010, 61(6): 519-524.
[2] Frampton J E, Keating G M. Celecoxib: a review of its use in the management of arthritis and acute pain[J]. Drugs, 2007, 67: 2433-2474.
[3] Jendrossek V. Targeting apoptosis pathways by Celecoxib in cancer[J]. Cancer letters, 2013, 332(2): 313-324.
[4] Arber N, Eagle C J, Spicak J, et al. Celecoxib for the prevention of colorectal adenomatous polyps[J]. New England Journal of Medicine, 2006, 355(9): 885-895.
[5] Tsai W C, Hsu C C, Chou S W, et al. Effects of celecoxib on migration, proliferation and collagen expression of tendon cells[J]. Connective tissue research, 2007, 48(1): 46-51.
[6] Wang J L, Lin K L, Chen J S, et al. Effect of celecoxib on Ca2+ movement and cell proliferation in human osteoblasts[J]. Biochemical pharmacology, 2004, 67(6): 1123-1130.
[7] Zhang S, Da L, Yang X, et al. Celecoxib potentially inhibits metastasis of lung cancer promoted by surgery in mice, via suppression of the PGE2-modulated β-catenin pathway[J]. Toxicology letters, 2014, 225(2): 201-207.
[8] Hu P J, Yu J, Zeng Z R, et al. Chemoprevention of gastric cancer by celecoxib in rats[J]. Gut, 2004, 53(2): 195-200.
Celecoxib是一种高度选择性的环氧合酶-2(COX-2)抑制剂,IC50值为40nM[1]。Celecoxib是一种选择性非甾体抗炎药(NSAID),常用于治疗急性疼痛、骨关节炎(OA)、类风湿性关节炎(RA)、幼年类风湿性关节炎和强直性脊柱炎(AS)等[2]。Celecoxib 具有强大的抗肿瘤活性,能够预防和治疗胰腺癌、乳腺癌、卵巢癌、非小细胞肺癌等多种癌症[3]。Celecoxib能够预防结直肠腺瘤性息肉的发生[4]。
在体外,Celecoxib(0.8, 2.0, 4.0, 8.0µg/mL)处理肌腱细胞24h,剂量依赖性地抑制了细胞活力和迁移,但不改变细胞形态或造成细胞坏死[5]。Celecoxib(1-100μM)处理人成骨细胞24h,剂量依赖性地抑制了细胞增殖,引起了细胞内Ca2+浓度的增加[6]。
在体内,Celecoxib(100mg/kg)通过口服治疗肺癌模型并做了单侧肺切除手术的小鼠,抑制了肺癌转移,抑制了血浆PGE2水平的升高[7]。Celecoxib(10、20mg/kg)通过口服治疗胃癌模型大鼠,显著降低了大鼠胃癌的发病率和生长[8]。
Cas No. | 169590-42-5 | SDF | |
别名 | 塞来昔布; SC 58635 | ||
化学名 | 4-[5-(4-methylphenyl)-3-(trifluoromethyl)pyrazol-1-yl]benzenesulfonamide | ||
Canonical SMILES | CC1=CC=C(C=C1)C2=CC(=NN2C3=CC=C(C=C3)S(=O)(=O)N)C(F)(F)F | ||
分子式 | C17H14F3N3O2S | 分子量 | 381.37 |
溶解度 | ≥ 19.1mg/mL in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.6221 mL | 13.1106 mL | 26.2213 mL |
5 mM | 0.5244 mL | 2.6221 mL | 5.2443 mL |
10 mM | 0.2622 mL | 1.3111 mL | 2.6221 mL |
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