1. Immunology/Inflammation
    Apoptosis
  2. COX
    Apoptosis
  3. DuP-697

DuP-697 

Cat. No.: HY-103387
Handling Instructions

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.

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DuP-697 Chemical Structure

DuP-697 Chemical Structure

CAS No. : 88149-94-4

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Description

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].

IC50 & Target[3]

hCOX-2

10 nM (IC50)

hCOX-1

800 nM (IC50)

In Vitro

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].

Cell Proliferation Assay[1]

Cell Line: HT29 cells
Concentration: 0 nM, 12.5 nM, 25 nM, 50 nM, 100 nM
Incubation Time: 24 hours
Result: Exhibited decreasing CI values in a concentration dependent manner. Showed statistically significant cytotoxic effect.

Apoptosis Analysis[1]

Cell Line: HT29 cells
Concentration: 25 nM, 50 nM, 100 nM
Incubation Time: 72 hours
Result: Caused concentration dependent apoptosis in HT29 cells.
In Vivo

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].

Molecular Weight

411.31

Formula

C₁₇H₁₂BrFO₂S₂

CAS No.

88149-94-4

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

DuP-697DuP697DuP 697COXApoptosisCyclooxygenaseCOX- 2annexin-Vapoptosisantiproliferativeantiangiogeniccolorectalcanceranti-inflammatoryprostaglandinantipyreticInhibitorinhibitorinhibit

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DuP-697
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