tcsc2377 Tolfenamic Acid

Tolfenamic Acid is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC₅₀ of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.

IC50 & Target: IC50: 13.49 μM (COX-2, in cells)^[1]

In Vitro: Tolfenamic Acid is a nonsteroidal antiinflammatory agent, selectively inhibits COX-2, with an IC₅₀ of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1^[1]. Tolfenamic Acid (100 μM) inhibits >70% of cell viability of BE3, OE33, and SKGT5. Tolfenamic Acid also acts as a potent Sp protein inhibitor, decreases Sp1 and Sp4 and suppresses c-Met expression in esophageal cancer cells BE3 and SKGT5^[2]. Tolfenamic Acid (50 μM) significantly affects gene expression in L3.6pl cells, and downregulates CENPF, KIF20A, LMNB1, MYB, SKP2, CCNE2, and DDIT3^[3].

In Vivo: Tolfenamic Acid (50 mg/kg 3 times/wk, p.o.) inhibits tumor formation and tumor incidence in N-nitrosomethylbenzylamine (NMBA)-induced esophageal tumor model. Tolfenamic Acid also causes decreases in tumor multiplicity and tumor volume in rats treated with NMBA^[2].