Anticancer agent 358
Anticancer agent 358 is a PARP inhibitor with antiproliferative activity against lung cancer cells and low toxicity to normal hepatocytes. Anticancer agent 358 binds to the active site of PARP via hydrogen bonds and π-π interactions with key residues, thereby promoting the accumulation of DNA damage. Anticancer agent 358 induces DNA damage, apoptosis, and autophagy in lung cancer cells. Anticancer agent 358 can be used for the research of non-small cell lung cancer.
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- CAS 番号: 3087062-38-9
- 分子式: C31H27FN6O2S
- 分子量:566.65
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
13.87 μM
|
Antiproliferative activity against human A549 lung cancer cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
Antiproliferative activity against human A549 lung cancer cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
|
42481535 |
| PC-9 | IC50 |
3.81 μM
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Antiproliferative activity against human PC-9 lung cancer cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
Antiproliferative activity against human PC-9 lung cancer cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
|
42481535 |
| NCI-H460 | IC50 |
10.01 μM
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Antiproliferative activity against human H460 lung cancer cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
Antiproliferative activity against human H460 lung cancer cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay.
|
42481535 |
Anticancer agent 358 (compound 14 h) (10-80 μM; 72 h) potently inhibits the proliferation of A549, PC-9, H460, and H1299 human lung cancer cells with IC50 values of 13.87 μM, 3.81 μM, 10.01 μM, and minimal cytotoxicity against normal L02 liver cells[1].
Anticancer agent 358 (5-20 μM; 24 h) induces dose-dependent cell death in A549, PC-9, and H460 human lung cancer cells, with a particularly pronounced effect in PC-9 cells[1].
Anticancer agent 358 (5-20 μM; 24 h) induces significant DNA damage in A549, PC-9, and H460 human lung cancer cells[1].
Anticancer agent 358 effectively binds to the active site of the PARP protein through key hydrogen bonding and π-π stacking interactions, suggesting potential PARP inhibition activity[1].
Anticancer agent 358 (5-20 μM; 72 h) promotes apoptosis in A549 and H460 human lung cancer cells but does not significantly induce apoptosis in PC-9 human lung cancer cells[1].
Anticancer agent 358 (5-20 μM; 72 h) upregulates the expression of key proteins involved in DNA damage and apoptosis, including caspase-9, γH2AX, and PARP, in A549, PC-9, and H460 human lung cancer cells[1].
Anticancer agent 358 (5-20 μM; 24 h) induces dose-dependent autophagy in A549, PC-9, and H460 human lung cancer cells[1].
Anticancer agent 358 (5-20 μM; 72 h) modulates the expression of key genes involved in DNA damage response, oxidative stress, apoptosis, and autophagy in a cell line-specific manner, with significant upregulation of p21, Bcl-2, caspase-6, Keap1, and ATG7 in H460 human lung cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, PC-9, H460, H1299, L02
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Concentration:10 μM; 20; 40 μM; 80 μM
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Incubation Time:72 h
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Result:Reduced relative cell viability to 42.71% for A549, 43.14% for PC-9, 17.54% for H460, 71.74% for H1299, and above 70% for L02 at 20 μM.
Achieved IC50 values of 13.87 μM (A549), 3.81 μM (PC-9), and 10.01 μM (H460).
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Cell Line:A549, PC-9, H460
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Concentration:10-20 μM (A549); 5-10 μM (PC-9, H460)
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Incubation Time:72 h
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Result:Elevated apoptotic rate to 5.80% in A549 cells and 28.43% in H460 cells, compared to 3.19% and 15.81% in respective control groups.
Showed no significant change in apoptotic rate in PC-9 cells relative to controls.
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Cell Line:A549, PC-9, H460
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Concentration:10-20 μM (A549); 5-10 μM (PC-9, H460)
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Incubation Time:24 h
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Result:Increased the number of MDC-positive puncta (autophagosomes) in a dose-dependent manner across all tested cell lines.
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Cell Line:A549, PC-9, H460
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Concentration:10-20 μM (A549); 5-10 μM (PC-9, H460)
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Incubation Time:72 h
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Result:Differentially modulated gene expression in a cell line-specific manner.
Significantly upregulated the expression of p21, Bcl-2, caspase-6, Keap1, and ATG7 genes in H460 cells.
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Cell Line:A549, PC-9, H460
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Concentration:10-20 μM (A549); 5-10 μM (PC-9, H460)
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Incubation Time:72 h
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Result:Increased the expression of caspase-9, γH2AX, and PARP proteins in A549, PC-9, and H460 cells.
化学情報
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CAS 番号 3087062-38-9
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分子量 566.65
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分子式 C31H27FN6O2S
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SMILES
O=C(C1=C(C)N=C(C2=CC=C(OCC(C)C)C(C#N)=C2)S1)NC3=CC=C(C4=CN(CC5=CC=C(F)C=C5)N=N4)C=C3
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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)