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.
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- 分子式: C33H42N4O2Se
- 分子量:605.67
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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生物活性
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Topoisomerase I |
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.
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Cell Line:human A549 lung carcinoma cells
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Concentration:1.25, 2.5, 5 μM
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Incubation Time:48 h (treatment followed by 14-day culture)
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Result:Induced a concentration-dependent reduction in colony formation.
Showed stronger inhibitory effects on cell proliferation than the positive control CPT at 5 μM.
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Cell Line:human A549 lung carcinoma cells
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Concentration:1.25-5 μM
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Incubation Time:24 h
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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.
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Cell Line:human A549 lung carcinoma cells
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Concentration:1.25, 2.5, 5 μM
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Incubation Time:24 h
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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.
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Cell Line:human A549 lung carcinoma cells
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Concentration:1.25, 2.5, 5 μM
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Incubation Time:48 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KM mice (female, 18-24 g)[1]
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Dosage:50 mg/kg; 100 mg/kg
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Administration:i.p.; single dose
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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.
化学情報
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分子量 605.67
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分子式 C33H42N4O2Se
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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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Anticancer agent 337 関連分類
HY-184750 関連分類
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