Polmacoxib  (Synonyms: CG100649)

Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Polmacoxib (7 mg/kg; p.o.; daily for 8 weeks) suppresses intestinal polyp formation in Apc^Min/+ 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

361.39

Solid

C₁₈H₁₆FNO₄S

301692-76-2

O=S(C1=CC=C(C(OC2(C)C)=C(C3=CC=CC(F)=C3)C2=O)C=C1)(N)=O

Room temperature in continental US; may vary elsewhere.

• [1]. Kim SH, et al. CG100649, a novel COX-2 inhibitor, inhibits colorectal adenoma and carcinoma growth in mouse models. Invest New Drugs. 2014;32(6):1105-1112.  [Content Brief]

  [2]. Flick AC, et al. Synthetic Approaches to the New Drugs Approved During 2015 [published correction appears in J Med Chem. 2017 Oct 26;60(20):8680]. J Med Chem. 2017;60(15):6480-6515.  [Content Brief]