Rofecoxib
Based on 5 publication(s) in Google Scholar
Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC50s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC50 > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells).
For research use only. We do not sell to patients.
- Purity: 99.89%
- CAS No.: 162011-90-7
- Formula: C17H14O4S
- Molecular Weight:314.36
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Rofecoxib
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Biological Activity
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Human COX-2 18 nM (IC50, in Chinese hamster ovary cells) |
Human COX-2 26 nM (IC50, in human osteosarcoma cells) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.02 μM
Compound: 1 (MK-966)
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In vitro potency against human Prostaglandin G/H synthase 2 in transfected CHO cells.
In vitro potency against human Prostaglandin G/H synthase 2 in transfected CHO cells.
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[PMID: 10197970] |
| CHO | IC50 |
0.02 μM
Compound: 1 (Rofecoxib)
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Inhibitory of human Prostaglandin G/H synthase 2 expressed in CHO cells.
Inhibitory of human Prostaglandin G/H synthase 2 expressed in CHO cells.
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[PMID: 12643942] |
| CHO | IC50 |
0.02 μM
Compound: Rofecoxib
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In vitro inhibitory potency against human COX-2 in stably transfected chinese hamster ovary (CHO) cells
In vitro inhibitory potency against human COX-2 in stably transfected chinese hamster ovary (CHO) cells
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[PMID: 10576684] |
| CHO | IC50 |
0.02 μM
Compound: Rofecoxib
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Inhibition of PGE-2 production in CHO cells expressing human COX-2.
Inhibition of PGE-2 production in CHO cells expressing human COX-2.
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[PMID: 10576685] |
| CHO | IC50 |
18 μM
Compound: MK 966; Vioxx(R)
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Inhibition of human COX2 expressed in CHO cells cells assessed as reduction in PGE2 release
Inhibition of human COX2 expressed in CHO cells cells assessed as reduction in PGE2 release
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[PMID: 30909021] |
| DU-145 | IC50 |
200 μM
Compound: 2, Rofecoxib, MK 966, VIOXX
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Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay
Antiproliferative activity against human DU145 cells after 72 hrs by MTT assay
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[PMID: 23735281] |
| J774 | IC50 |
>10 μM
Compound: rofecoxib
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In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells
In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells
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[PMID: 15857149] |
| J774 | IC50 |
0.012 μM
Compound: rofecoxib
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In vitro inhibitory activity against Prostaglandin G/H synthase 2 in murine J774 cells
In vitro inhibitory activity against Prostaglandin G/H synthase 2 in murine J774 cells
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[PMID: 15857149] |
| PC-3 | IC50 |
>50 μM
Compound: 2, Rofecoxib, MK 966, VIOXX
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Antiproliferative activity against human PC3 cells expressing PCDNA after 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells expressing PCDNA after 72 hrs by MTT assay
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[PMID: 23735281] |
| PC-3 | IC50 |
>50 μM
Compound: 2, Rofecoxib, MK 966, VIOXX
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Antiproliferative activity against human PC3 cells expressing SKP2 after 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells expressing SKP2 after 72 hrs by MTT assay
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[PMID: 23735281] |
| PC-3 | IC50 |
200 μM
Compound: 2, Rofecoxib, MK 966, VIOXX
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Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
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[PMID: 23735281] |
| Sf21 | IC50 |
0.12 μM
Compound: rofecoxib
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Inhibition of human recombinant COX2 expressed in insect Sf21 cells by EIA assay
Inhibition of human recombinant COX2 expressed in insect Sf21 cells by EIA assay
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[PMID: 17378609] |
| Sf21 | IC50 |
0.156 μM
Compound: 1,A, Vivoxx
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Inhibition of human recombinant COX2 expressed in Sf21 cells assessed as PGE2 production using arachidonic acid as substrate preincubated for 15 mins measured after 5 mins by EIA
Inhibition of human recombinant COX2 expressed in Sf21 cells assessed as PGE2 production using arachidonic acid as substrate preincubated for 15 mins measured after 5 mins by EIA
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[PMID: 21752640] |
| Sf21 | IC50 |
0.17 μM
Compound: 2
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Inhibition of human recombinant COX2 expressed in Sf21 cells assessed as conversion of arachidonic acid to PGE2 preincubated for 15 mins measured after 5 mins by enzyme immunoassay
Inhibition of human recombinant COX2 expressed in Sf21 cells assessed as conversion of arachidonic acid to PGE2 preincubated for 15 mins measured after 5 mins by enzyme immunoassay
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[PMID: 21958737] |
| Sf21 | IC50 |
0.17 μM
Compound: Rofecoxib
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Inhibition of human recombinant COX2 expressed in Sf21 cells using arachidonic acid as substrate preincubated for 15 mins before arachidonic acid addition measured after 5 mins
Inhibition of human recombinant COX2 expressed in Sf21 cells using arachidonic acid as substrate preincubated for 15 mins before arachidonic acid addition measured after 5 mins
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[PMID: 22652053] |
| Sf21 | IC50 |
74.5 nM
Compound: Rofecoxib
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Inhibition of human recombinant COX2 expressed in Sf21 cells assessed as effect on prostaglandin E2 production by ELISA
Inhibition of human recombinant COX2 expressed in Sf21 cells assessed as effect on prostaglandin E2 production by ELISA
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[PMID: 19056264] |
| Sf9 | IC50 |
107 nM
Compound: Rofecoxib
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Inhibition of human COX2 expressed in baculovirus-infected SF9 cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay
Inhibition of human COX2 expressed in baculovirus-infected SF9 cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay
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[PMID: 19520573] |
| U-937 | IC50 |
>10 μM
Compound: 3 (rofecoxib)
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In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells
In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells
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[PMID: 12877584] |
| U-937 | IC50 |
2 μM
Compound: Rofecoxib
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Inhibition of COX-1 in U-937 (human lymphoma) cell microsomes.
Inhibition of COX-1 in U-937 (human lymphoma) cell microsomes.
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[PMID: 10576685] |
Rofecoxib (MK-0966) is a potent and orally active inhibitor of COX-2, with IC50s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over COX-1 (IC50 >50 μM in U937 cells and >15 μM in Chinese hamster ovary cells). Rofecoxib time dependently inhibits purified human recombinant COX-2 (IC50=0.34 μM) but suppresses purified human COX-1 in a non-time-dependent manner that can only be observed at a very low substrate concentration (IC50=26 μM at 0.1 μM arachidonic acid concentration). Rofecoxib selectively inhibits lipopolysaccharide-induced, COX-2-derived PGE(2) synthesis with an IC50 value of 0.53 ± 0.02 μM compared with an IC50 value of 18.8 ± 0.9 μM for the inhibition of COX-1-derived thromboxane B(2) synthesis after blood coagulation[1]. Rofecoxib (36 μM) causes a cell proliferation of 68% in MPP89, of 58% in Ist-Mes-1 and 40% in Ist-Mes-2. MSTO-211H and NCI-H2452 treated with 36 μM of Rofecoxib have a survival of 97% and 90% respectively. Rofecoxib (36 μM) decreases COX-2 and mRNA levels in Ist-Mes-1, Ist-Mes-2 and MPP89 cell lines[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 162011-90-7
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Appearance Solid
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Molecular Weight 314.36
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Formula C17H14O4S
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Color White to yellow
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SMILES
O=C1OCC(C2=CC=C(S(=O)(C)=O)C=C2)=C1C3=CC=CC=C3
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Synonyms
MK 966
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Br J Pharmacol
Assessment of the molecular mechanisms of drug-induced hidden cardiotoxicity by a multi-omics approach: The example of rofecoxib. [Abstract]2025 Jun 18. PMID: 40532721 -
Biochem Pharmacol
Chronic treatment with rofecoxib but not ischemic preconditioning of the myocardium ameliorates early intestinal damage following cardiac ischemia/reperfusion injury in rats. [Abstract]2020 Aug;178:114099. PMID: 32540483 -
Cells
Lack of Small Intestinal Dysbiosis Following Long-Term Selective Inhibition of Cyclooxygenase-2 by Rofecoxib in the Rat. [Abstract]2019 Mar 15;8(3). pii: E251. PMID: 30884758 -
J Pharmacol Exp Ther
Disulfiram activation of prostaglandin E2 synthesis: a novel antifibrotic mechanism in pulmonary fibrosis. [Abstract]2025 Jun;392(6):103588. PMID: 40359874 -
Asian Pac J Cancer Prev
Antitumour Activities of Selected Pure Compounds Identified from the Serum of Crocodylus porosus, Malayopython reticulatus, Varanus salvator and Cuora kamaroma amboinensis. [Abstract]2021 Feb 12;22(S1):97-106. PMID: 33576218
Solvent & Solubility
DMSO : 33.33 mg/mL (106.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
The anti-proliferative activity of single drug treatments is assessed in a monolayer culture condition by plating Ist-Mes-1, Ist-Mes-2 and MPP89 cells in T25 flask. After 24 h, DMSO (at the same final concentration of that present in medium with drugs), 50 μM gefitinib or 36 μM Rofecoxib are added. The cells are then harvested at 48 h after treatment and analyzed by western blot and RT-PCR to evaluate the effect of the drugs on expression and mRNA levels of EGFR and COX-2. The expression of the cell cycle arrest genes and p-AKT, AKT, p-ERK and ERK is detected by Western blot to assess the antiproliferative activity of the two drugs in isolation (25 μM gefitinib or 4 μM Rofecoxib) and in combination 25 μM gefitinib+4 μM Rofecoxib[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Retinopathy of prematurity (ROP) is induced in C57BL/6J mice. The mice are randomly allocated into three experimental groups with 16 mice in each group: normal group-age-matched mice are maintained in room air from birth to P17 and are served as negative control; untreated ROP group-ROP is induced as described above without treatment and served as positive control; Rofecoxib-treated ROP group-ROP mice are treated daily with Rofecoxib (15 mg/kg body weight, intraperitoneally) from P12 to P17. Rofecoxib is dissolved in a 0.5% aqueous methylcellulose solution before administration[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (289 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Rofecoxib, et al. Rofecoxib [Vioxx, MK-0966; 4-(4'-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles. J Pharmacol Exp Ther. 1999 Aug;290(2):551-60. [Content Brief]
[2]. Liu NN, et al. Rofecoxib inhibits retinal neovascularization via down regulation of cyclooxygenase-2 and vascular endothelial growth factor expression. Clin Exp Ophthalmol. 2015 Jul;43(5):458-65. [Content Brief]
[3]. Stoppoloni D, et al. Synergistic effect of gefitinib and rofecoxib in mesothelioma cells. Mol Cancer. 2010 Feb 2;9:27. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.1811 mL | 15.9053 mL | 31.8107 mL | 79.5267 mL |
| 5 mM | 0.6362 mL | 3.1811 mL | 6.3621 mL | 15.9053 mL | |
| 10 mM | 0.3181 mL | 1.5905 mL | 3.1811 mL | 7.9527 mL | |
| 15 mM | 0.2121 mL | 1.0604 mL | 2.1207 mL | 5.3018 mL | |
| 20 mM | 0.1591 mL | 0.7953 mL | 1.5905 mL | 3.9763 mL | |
| 25 mM | 0.1272 mL | 0.6362 mL | 1.2724 mL | 3.1811 mL | |
| 30 mM | 0.1060 mL | 0.5302 mL | 1.0604 mL | 2.6509 mL | |
| 40 mM | 0.0795 mL | 0.3976 mL | 0.7953 mL | 1.9882 mL | |
| 50 mM | 0.0636 mL | 0.3181 mL | 0.6362 mL | 1.5905 mL | |
| 60 mM | 0.0530 mL | 0.2651 mL | 0.5302 mL | 1.3254 mL | |
| 80 mM | 0.0398 mL | 0.1988 mL | 0.3976 mL | 0.9941 mL | |
| 100 mM | 0.0318 mL | 0.1591 mL | 0.3181 mL | 0.7953 mL |
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