Polmacoxib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Polmacoxib (CG-100649) 是一种新型 NSAID，可抑制 COX-2 和碳酸酐酶 (CA)-I/-II。

Polmacoxib (CG-100649) is a novel NSAID proposed to inhibit both COX-2 and carbonic anhydrase (CA)-I/-II; inhibits premalignant and malignant colorectal lesions in mouse models, partly through inhibiting tumor cell proliferation; induces the G2/M cell cycle arrest in colon cancer cells, and inhibits the tumor growth in colon cancer xenograft in nude mice. Rheumatoid Arthritis Approved(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. (In Vivo):Polmacoxib (7 mg/kg; p.o.; daily for 8 weeks) suppresses intestinal polyp formation in ApcMin/+ mice.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.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.

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.

Polmacoxib (7 mg/kg; p.o.; daily for 8 weeks) suppresses intestinal polyp formation in ApcMin/+ mice.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.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.

CG-100649

Chromatin/Epigenetic

COX

COX

Inflammation/Immunology

Rheumatoid Arthritis

301692-76-2

361.39

C12H16FNO4S

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (691.77 mM)

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

4-(3-(3-fluorophenyl)-5,5-dimethyl-4-oxo-4,5-dihydrofuran-2-yl)benzenesulfonamide

(-20℃)

With Ice Pack

≥ 2 years