2. Immunology/Inflammation Apoptosis
  3. COX Apoptosis
  4. 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.

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DuP-697 Chemical Structure

DuP-697 Chemical Structure

CAS No. : 88149-94-4

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Based on 1 publication(s) in Google Scholar

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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].

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

DuP-697 Related Antibodies

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

411.31

Formula

C17H12BrFO2S2
CAS No.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMF : ≥ 54 mg/mL (131.29 mM)

DMSO : ≥ 15 mg/mL (36.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : ≥ 7 mg/mL (17.02 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4313 mL 12.1563 mL 24.3126 mL
5 mM 0.4863 mL 2.4313 mL 4.8625 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: ≥99.0%

COA (257 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO / DMF 1 mM 2.4313 mL 12.1563 mL 24.3126 mL 60.7814 mL
5 mM 0.4863 mL 2.4313 mL 4.8625 mL 12.1563 mL
10 mM 0.2431 mL 1.2156 mL 2.4313 mL 6.0781 mL
15 mM 0.1621 mL 0.8104 mL 1.6208 mL 4.0521 mL
DMSO / DMF 20 mM 0.1216 mL 0.6078 mL 1.2156 mL 3.0391 mL
25 mM 0.0973 mL 0.4863 mL 0.9725 mL 2.4313 mL
30 mM 0.0810 mL 0.4052 mL 0.8104 mL 2.0260 mL
DMF 40 mM 0.0608 mL 0.3039 mL 0.6078 mL 1.5195 mL
50 mM 0.0486 mL 0.2431 mL 0.4863 mL 1.2156 mL
60 mM 0.0405 mL 0.2026 mL 0.4052 mL 1.0130 mL
80 mM 0.0304 mL 0.1520 mL 0.3039 mL 0.7598 mL
100 mM 0.0243 mL 0.1216 mL 0.2431 mL 0.6078 mL
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DuP-697 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DuP-69788149-94-4DuP697DuP 697COXApoptosisCyclooxygenaseCOX- 2annexin-Vapoptosisantiproliferativeantiangiogeniccolorectalcanceranti-inflammatoryprostaglandinantipyreticInhibitorinhibitorinhibit

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