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Tolfenamic acid-d₄ is intended for use as an internal standard for the quantification of tolfenamic acid by GC- or LC-MS. Tolfenamic acid is a non-steroidal anti-inflammatory drug (NSAID) with anticancer activity. It is selective for COX-2 over COX-1 in canine DH82 monocyte/macrophage cells (IC₅₀s = 3.53 and >51.2 μg/ml, respectively). Tolfenamic acid inhibits calcium influx in human polymorphonuclear leukocytes (PMNLs) induced by N-formyl-L-methionyl-L-leucyl-L-phenylalanine (fMLP; ) or the calcium ionophore A23187 (Item Nos. 11016 | 22030) in a concentration-dependent manner. It decreases protein levels of the transcription factors Sp1, Sp3, and Sp4 in PANC-1 and L3.6pl cells when used at a concentration of 50 μM and inhibits proliferation of PANC-1, L3.6pl, and PANC-28 cells in a concentration-dependent manner. Tolfenamic acid (50 and 100 μM) decreases the viability of and induces apoptosis in MDA-MB-231 cells. It reduces tumor growth in an MDA-MB-231 mouse xenograft model when administered at doses of 25 and 50 mg/kg. Tolfenamic acid (150 μmol/kg) reduces carrageenan-induced paw edema in mice by 24%.

Labelled Tolfenamic Acid. Non-steroidal anti-inflammatory drugs (NSAIDs). A derivative of anthranilic acid, related structurally to Mefenamic and Flufenamic acids. Anti-inflammatory, analgesic.

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