2. Cell Cycle/DNA Damage Immunology/Inflammation Apoptosis Metabolic Enzyme/Protease NF-κB
  3. Topoisomerase COX Apoptosis Reactive Oxygen Species
  4. Topo I/COX-2-IN-2

Topo I/COX-2-IN-2 (Compound W10) is a potent dual-target inhibitor of Topo I and COX-2 with IC50 values of 0.90 μM and 2.31 μM, respectively. Topo I/COX-2-IN-2 induces cancer cell apoptosis through the mitochondrial pathway.

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Topo I/COX-2-IN-2 Chemical Structure

Topo I/COX-2-IN-2 Chemical Structure

CAS No. : 2841455-91-0

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Topo I/COX-2-IN-2 Related Antibodies

Top Publications Citing Use of Products

View All Topoisomerase Isoform Specific Products:

View All Isoforms
Topoisomerase Topo I Topo II

View All COX Isoform Specific Products:

View All Isoforms
COX COX-1 COX-2 COX-3

  • Biological Activity

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Description

Topo I/COX-2-IN-2 (Compound W10) is a potent dual-target inhibitor of Topo I and COX-2 with IC50 values of 0.90 μM and 2.31 μM, respectively. Topo I/COX-2-IN-2 induces cancer cell apoptosis through the mitochondrial pathway[1].

IC50 & Target

Topoisomerase I

0.90 μM (IC50)

COX-2

2.31 μM (IC50)

In Vitro

Topo I/COX-2-IN-2 (Compound W10) (0-30 μM) shows good toxicity against cancer cells[1].
Topo I/COX-2-IN-2 forms an ionic bonding interaction with DA13 of DNA to improve Topo I inhibition[1].
Topo I/COX-2-IN-2 (0-9 μM, 24 h) arrests cell cycle of HT29 and RKO at G1/G0 phase, induces apoptosis in HT29 and RKO cells through the mitochondrial pathway, and inhibits abnormal activation of the NF-κB/IκB pathway. [1].

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

Topo I/COX-2-IN-2 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HT29, RKO, HCT116, LoVo and SW480
Concentration: 0-30 μM
Incubation Time: 72 h
Result: Showed good toxicity with IC50 values of 1.48 ± 0.08 μM, 2.06 ± 0.01 μM, 4.89 ± 0.36 μM, 8.42 ± 0.22 μM and 7.36 ± 0.64 μM for HT29, RKO, HCT116, LoVo and SW480 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: HT29 and RKO
Concentration: 2, 4 and 8 μM for HT29; 3, 6 and 9 μM for RKO
Incubation Time: 24 h
Result: Blocked the cell cycle in G1/G0 phase in both HT29 and RKO. In HT29 cells, the arresting activity was not obvious for the ratio of G1/G0 phase in high-concentration treatment group increased from 55.20% to 65.17% slightly, while in RKO cells, the ratio of G1/G0 phase obviously increased from 37.57% to 76.99%.

Apoptosis Analysis[1]

Cell Line: HT29 and RKO
Concentration: 2, 4 and 8 μM for HT29; 3, 6 and 9 μM for RKO
Incubation Time: 24 h
Result: Mainly induced the late apoptosis in HT29 cells and exhibited dual induction of late and early apoptosis in RKO cells.
Induced the production of reactive oxygen species (ROS) burst and significantly reduce the mitochondrial membrane potential.

Western Blot Analysis[1]

Cell Line: HT29 and RKO
Concentration: 2, 4 and 8 μM for HT29; 3, 6 and 9 μM for RKO
Incubation Time: 24 h
Result: Induced increased expression of the pro-apoptotic proteins Bax, cytochrome c and apoptotic effector cleaved caspase 3/9, reduced the expression of the inhibitory factor Bcl-2.
The expressions of phosphorylated NF-κB and IκB were significantly decreased.
In Vivo

Topo I/COX-2-IN-2 (Compound W10) (15 and 30 mg/kg; i.p.; b.i.d for 2 weeks) inhibits tumor growth and shows obvious necrosis on tumor tissue[1].
Topo I/COX-2-IN-2 has acceptable pharmacokinetic properties for intraperitoneal injection and oral administration[1].

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

Animal Model: Male BALB/c nude mice weighing 20–25 g, HT29 xenograft model[1]
Dosage: 15 and 30 mg/kg
Administration: Intraperitoneal injection, twice daily for 2 weeks
Result: 30 mg/kg group immediately slowed down the tumor growth rate after administration, and almost completely prevented tumor growth in the later stage, and its tumor growth inhibition (TGI) was 57.86%. 15 mg/kg group showed 40.67% TGI.
Showed obvious necrosis on tumor tissue.
Animal Model: 250–280 g male SD rats[1]
Dosage: 100 mg/kg and 30 mg/kg
Administration: Intragastric administration (100 mg/kg) or intraperitoneal injection (30 mg/kg) (Pharmacokinetics Study)
Result: Pharmacokinetic data of Topo I/COX-2-IN-2 (W10) in vivoa[1]
Comp. Dose
(mg/kg)		 Route T1/2(h) Tmax(h) Cmax
(μg/mL)		 AUC0-t
(μg⋅h/mL)
Topo I/COX-2-IN-2 100 p.o. 8.87 ± 1.92 3.67 ± 0.58 2.00 ± 0.41 24.81 ± 5.76
30 i.p. 4.27 ± 0.22 0.28 ± 0.05 1.60 ± 0.34 5.41 ± 0.20

a Topo I/COX-2-IN-2 was administered to 6 SD rats with different administration methods and doses, and the serum concentration was analyzed. The analysis method is the linear trapezoidal PKsolver 2.0 computer program of the non-compartmental model. All the data are from the above 6 rats, and the data are represented by the mean and standard deviation.
Molecular Weight

420.93

Formula

C24H25ClN4O
CAS No.
SMILES

ClC1=C(C(NC2=CC=CC=C2C(NC3=CC=C(C=C3)N4CCNCC4)=O)=CC=C1)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Topo I/COX-2-IN-2 Related Classifications

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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:

Topo I/COX-2-IN-22841455-91-0TopoisomeraseCOXApoptosisReactive Oxygen SpeciesCyclooxygenasecolon cancerHT29RKOBALB/c nude miceInhibitorinhibitorinhibit

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