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Polmacoxib
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Polmacoxib
CAS No. : 301692-76-2
MCE 站:Polmacoxib
产品活性:Polmacoxib (CG100649) 是一种首创的,具有口服活性的非甾体抗炎药 (NSAID),它是一种双重抑制剂,可以抑制 COX-2 (IC50 ~ 0.1 μg/ml)和碳酸酐酶 (carbonic anhydrase)。Polmacoxib 在小鼠模型中抑制大肠腺瘤和肿瘤生长。
研究领域:Immunology/Inflammation | Metabolic Enzyme/Protease
作用靶点:COX | 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.
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.
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