DuP-697 

DuP-697 is a member of the vicinal diaryl heterocycles and a potent, irreversible, selective and orally active COX-2 inhibitor (IC₅₀ of 10 nM and 800 nM for human COX-2 and COX-1, respectively). DuP-697 exerts antiproliferative (IC₅₀ of 42.8 nM), antiangiogenic and apoptotic effects on HT29 colorectal cancer cells. DuP-697 inhibits prostaglandin synthesis and has anti-inflammatory, anticancer and antipyretic effects^[1][2][3].

DuP-697 (0-100 nM; 24 hours; HT29 cells) treatment shows antiproliferative with an IC₅₀ value of 42.8 nM^[1].
DuP-697 (25-100 nM; 72 hours; HT29 cells) treatment causes concentration dependent apoptosis in HT29 cells. The percentage of UR (apoptosis portion) area increases gradually according to the concentration of DuP-697 from 7% in control group to 52% in 100 nM DuP-697^[1].
DuP-697 in 100, 10 and 1 nM concentrations cause antiangiogenic effect. Antiangiogenic scores of DuP-697 are 1.2, 0.8 and 0.5, respectively^[1].

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

DuP-697 is a potent inhibitor of paw swelling in nonestablished and established adjuvant arthritis in rats (ED₅₀ = 0.03 and 0.18 mg/kg/day, respectively). DuP-697 has no effect on phenylquinone writhing in rats (ED₅₀ greater than 100 mg/kg), but is analgetic against inflammation-related pain in the Randall-Selitto assay (ED₅₀ = 3.5 mg/kg) and is a very potent antipyretic agent (ED₅₀ = 0.05 mg/kg). DuP-697 (5 mg/kg i.v.) does not alter renal blood flow or the renal vascular response to angiotensin II in furosemide-pretreated, volume-depleted rats^[2].
DuP-697 is a moderate inhibitor of bull seminal vesicle prostaglandin (PG) synthesis (IC₅₀ of 24 μM) and a potent inhibitor of rat brain PG synthesis (IC₅₀ of 4.5 μM) but was ineffective against rat kidney PG synthesis (IC₅₀ of 75 μM)^[2].

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

411.31

C₁₇H₁₂BrFO₂S₂

88149-94-4

O=S(C1=CC=C(C2=C(C3=CC=C(F)C=C3)SC(Br)=C2)C=C1)(C)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Altun A, et al. Anticancer effect of COX-2 inhibitor DuP-697 alone and in combination with tyrosine kinase inhibitor (E7080) on colon cancer cell lines. Asian Pac J Cancer Prev. 2014;15(7):3113-21.  [Content Brief]

  [2]. Gans KR, et al. Anti-inflammatory and safety profile of DuP 697, a novel orally effective prostaglandin synthesis inhibitor. J Pharmacol Exp Ther. 1990 Jul;254(1):180-7.  [Content Brief]

  [3]. Gierse JK, et al. Expression and selective inhibition of the constitutive and inducible forms of human cyclo-oxygenase. Biochem J. 1995 Jan 15;305 ( Pt 2):479-84.  [Content Brief]