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Anticancer agent 337

Anticancer agent 337 (compound 5n) is a topoisomerase I inhibitor. Anticancer agent 337 inhibits topoisomerase I activity in a concentration-dependent manner, suppresses cancer cell migration, induces apoptosis, and arrests the cell cycle at the G1 phase. Anticancer agent 337 can be used in the research of lung cancer, hepatocellular carcinoma, and cervical adenocarcinoma.

Para uso exclusivo en investigación. No vendemos a pacientes.

Fòrmula: C₃₃H₄₂N₄O₂Se
Peso molecular:605.67

Almacenamiento:

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

Anticancer agent 337 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

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- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
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Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

Topoisomerase I

Ver todos los productos específicos de isoformas Topoisomerase :

In Vitro

Anticancer agent 337 (compound 5n) (48 h) potently inhibits the proliferation of A549, HepG2, and HeLa cancer cells with IC₅₀ values of 5.22 μM, 6.28 μM, and 3.62 μM, respectively, while exhibiting minimal toxicity to normal LO-2 hepatocytes^[1].
Anticancer agent 337 (10-100 μM; 30 min) inhibits human Topo I activity in a concentration-dependent manner, blocking supercoiled DNA relaxation at concentrations ranging from 10.0 μM to 100.0 μM^[1].
Anticancer agent 337 (100 μM; 30 min) acts as a Topo I poison at 100.0 μM, stabilizing the Topo I-DNA cleavage complex to induce DNA strand breaks, consistent with the mechanism of CPT (HY-16560)^[1].
Anticancer agent 337 (1.25-5 μM; 48 h treatment followed by 14-day culture) suppresses the long-term proliferation of A549 cells in a concentration-dependent manner, with stronger inhibition at 5.0 μM than the positive control CPT^[1].
Anticancer agent 337 (1.25-5 μM; 24 h, 48 h) inhibits the migration of A549 cells in a concentration-dependent manner over 24 h and 48 h, demonstrating anti-metastatic potential^[1].
Anticancer agent 337 (1.25-5 μM; 24 h) potently induces apoptosis in A549 cells in vitro in a concentration-dependent manner, with an 84.0% total apoptosis rate at 5.0 μM, which is significantly higher than that of the positive control CPT^[1].
Anticancer agent 337 (1.25-5 μM; 24 h) induces dose-dependent G1/G0 phase cell cycle arrest in A549 cells, with 74.36% of cells accumulating in G1 phase at a concentration of 5.0 μM^[1].
Anticancer agent 337 (1.25-5 μM; 48 h) induces concentration-dependent DNA double-strand breaks in A549 cells, with γ-H2AX foci levels at 5.0 μM comparable to those induced by the positive control CPT^[1].
Anticancer agent 337 (1.25-5 μM; 24 h) induces concentration-dependent mitochondrial dysfunction in A549 cells, reducing mitochondrial membrane potential at concentrations of 1.25 μM, 2.5 μM, and 5.0 μM^[1].
Anticancer agent 337 (1.25-5 μM; 12 h) induces concentration-dependent oxidative stress in A549 cells, significantly increasing intracellular ROS levels at concentrations of 1.25 μM, 2.5 μM, and 5.0 μM^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

human A549 lung carcinoma cells
Concentration:

1.25, 2.5, 5 μM
Incubation Time:

48 h (treatment followed by 14-day culture)
Result:

Induced a concentration-dependent reduction in colony formation.
Showed stronger inhibitory effects on cell proliferation than the positive control CPT at 5 μM.

Apoptosis Analysis^[1]

Cell Line:

human A549 lung carcinoma cells
Concentration:

1.25-5 μM
Incubation Time:

24 h
Result:

Induced total apoptosis (early + late) in a concentration-dependent manner, with rates of 10.5%, 25.7%, and 84.0% at 1.25 μM, 2.5 μM, and 5 μM, respectively.
Induced significantly higher apoptosis than the positive control CPT (15.3% apoptosis rate) at 5 μM.

Cell Cycle Analysis^[1]

Cell Line:

human A549 lung carcinoma cells
Concentration:

1.25, 2.5, 5 μM
Incubation Time:

24 h
Result:

Induced dose-dependent G1/G0 phase cell cycle arrest.
Increased the proportion of G1-phase cells from 41.83% (control) to 74.36% at 5 μM.
Decreased the combined S and G2/M phase proportion from 58.17% to 25.82% at 5 μM.

Immunofluorescence^[1]

Cell Line:

human A549 lung carcinoma cells
Concentration:

1.25, 2.5, 5 μM
Incubation Time:

48 h
Result:

Induced a concentration-dependent accumulation of γ-H2AX foci, a marker of DNA double-strand breaks.
Induced DSB levels similar to the positive control CPT at 5 μM.

In Vivo

Anticancer agent 337 (compound 5n) (50-100 mg/kg; i.p.; single dose) exhibits an acceptable in vivo safety profile at a single intraperitoneal dose of 50.0 mg/kg in healthy KM mice, but causes acute toxicity and mortality at 100.0 mg/kg^[1].

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

Animal Model:

KM mice (female, 18-24 g)^[1]
Dosage:

50 mg/kg; 100 mg/kg
Administration:

i.p.; single dose
Result:

Exhibited normal growth with gradual weight gain over 14 days, no behavioral abnormalities, and histopathological examination of heart, liver, spleen, lungs, and kidneys showed no signs of necrosis, inflammation, or morphological abnormalities at 50 mg/kg.
Caused acute toxic reactions, resulting in mortality in 4 out of 8 treated mice at 100 mg/kg.

Chemical Information

Peso molecular 605.67
Fòrmula C₃₃H₄₂N₄O₂Se
SMILES

O=C(NCCC[Se]C#N)CCC[C@]1([H])[C@@]2([H])[C@@]3([H])[C@@](CCCN3CCC2)([H])CN1CC4=CC=C(C(C5=CC=CC=C5)=O)C=C4
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Xiao J, et al. Design, synthesis, and biological evaluation of novel selenium-matrine hybrid compounds as topo I -targeted anticancer agents. Bioorganic chemistry. 2026 Jun 27;180:110173. [Content Brief]

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Anticancer agent 337

Ver todos los productos específicos de isoformas Topoisomerase