301692-76-2
301692-76-2 structure
- Name: Polmacoxib
- Chemical Name: 5-{4-(aminosulfonyl)phenyl}-2,2-dimethyl-4-(3-fluorophenyl)-3(2H)-furanone
- CAS Number: 301692-76-2
- Molecular Formula: C18H16FNO4S
- Molecular Weight: 361.38700
- Catalog: Signaling Pathways Immunology/Inflammation COX
- Create Date: 2017-09-09 20:17:21
- Modify Date: 2025-08-24 20:21:18
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Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory drug (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase[1]. Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models[2].
| Name | 5-{4-(aminosulfonyl)phenyl}-2,2-dimethyl-4-(3-fluorophenyl)-3(2H)-furanone |
|---|---|
| Synonyms | 4-(3-(3-fluorophenyl)-5,5-dimethyl-4-oxo-4,5-dihydrofuran-2-yl)benzenesulfonamide |
| Description | Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory drug (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase[1]. Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models[2]. |
|---|---|
| Related Catalog | |
| Target |
COX-2:0.1 μg/mL (IC50) carbonic anhydrase |
| In Vitro | Polmacoxib (CG100649) (0-1 μg/ml; 24 hours; HCA-7 and HT-29 cells) can inhibit COX-2 activity and PGE2 production in human colon cancer cells, at lower concentrations compared to Celecoxib[2]. |
| In Vivo | Polmacoxib (7 mg/kg; p.o.; daily for 8 weeks) suppresses intestinal polyp formation in ApcMin/+ mice[2]. Polmacoxib (7-15 mg/kg; p.o.; daily from day 27 post-injection to day 111; athymic nude mice; subcutaneous xenograft mouse model) reduces tumor volume and tumor weight by 58% and 48%, respectively, compared to a 48% and 36% reduction following treatment with Celecoxib[2]. Polmacoxib (7-15 mg/kg; p.o.; began on day 14 and continued for 8 weeks; athymic nu/nu mice; orthotopic xenograft mouse model) inhibits CRC growth in an orthotopic xenograft mouse model, reducing tumor weight by 70% using 7 mg/kg or by 83% using 15 mg/kg, compared to a similar 70% reduction following treatment with 500 mg/kg of Celecoxib[2]. |
| References |
| Molecular Formula | C18H16FNO4S |
|---|---|
| Molecular Weight | 361.38700 |
| Exact Mass | 361.07800 |
| PSA | 94.84000 |
| LogP | 4.50040 |
| Hazard Codes | Xi |
|---|