DEHYDROALTENUSIN
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- CAS号:
- 31186-13-7
- 英文名:
- dehydroaltenusin
- 英文别名:
- dehydroaltenusin;6H-Dibenzo[b,d]pyran-2,6(4aH)-dione, 3,7-dihydroxy-9-methoxy-4a-methyl-, (4aS)-
- 中文名:
- DEHYDROALTENUSIN
- 中文别名:
- 脱氢阿霉素;化合物 T15094
- CBNumber:
- CB81362873
- 分子式:
- C15H12O6
- 分子量:
- 288.25
- MOL File:
- 31186-13-7.mol
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DEHYDROALTENUSIN化学性质
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沸点:
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654.0±55.0 °C(Predicted)
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密度:
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1.54±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系数(pKa):
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6.76±0.40(Predicted)
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DEHYDROALTENUSIN性质、用途与生产工艺
Dehydroaltenusin 脱氢阿霉素是真核DNA 聚合酶 α (DNA polymerase α) 的小分子选择性抑制剂，一种由真菌产生的抗生素，其 IC50值为 0.68 μM。 Dehydroaltenusin 对哺乳动物 polα 活性的抑制作用模式对 DNA 模板引物 (Ki=0.23 μM) 是竞争性的，对 2'-脱氧核糖核苷 5'-三磷酸底物是非竞争性的 (Ki=0.18 μM)。
Dehydroaltenusin 在 S 期阻止癌细胞周期并触发凋亡 apoptosis。
Dehydroaltenusin 在体内具有抗人类腺癌肿瘤的抗肿瘤活性。
IC50: 0.68 μM (DNA polymerase α)
Dehydroaltenusin (38.0-44.4 μM; 24 hours) inhibits cell growth in a dose-dependent manner and the LD
50
values varies from 38.0 to 44.4 μM.
Dehydroaltenusin (38.0 μM; 6 hours) inhibits cell growth by blocking the S-phase of DNA replication.
Dehydroaltenusin (75.0 μM; 24 hours) has a strong apoptotic effect on human cancer cells, DNA ladders can be detected after 12 h of incubation with dehydroaltenusin.
Cell Proliferation Assay
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Cell Line:
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Human cancer cell line: A549, BALL-1, HeLa and NUGC-3 cells
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Concentration:
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38.0-44.4 μM
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Incubation Time:
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24 hours
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Result:
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Inhibited cell growth of human cancer cell lines.
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Cell Cycle Analysis
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Cell Line:
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HeLa cells
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Concentration:
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38.0 μM
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Incubation Time:
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6 hours
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Result:
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Decreased to 45% of the control value after 6 h of incubation [
3
H]-thymidine.
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Apoptosis Analysis
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Cell Line:
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HeLa cells
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Concentration:
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75.0 μM
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Incubation Time:
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12-24 hours
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Result:
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Detected DNA ladders after 12 hours of incubation.
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Dehydroaltenusin (injection; 20 mg/kg; 2-day intervals; 12-39 days) shows suppressed tumor growth from 21 days.
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Animal Model:
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Nude mice bearing HeLa solid tumors
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Dosage:
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20 mg/kg
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Administration:
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Injection; 20 mg/kg; 2-day intervals; 12-39 days
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Result:
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Suppressed tumor growth.
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DEHYDROALTENUSIN
上下游产品信息
上游原料
下游产品
31186-13-7, DEHYDROALTENUSIN 相关搜索:
- 抑制剂
- 标准品
- 化合物 T15094
- 脱氢阿霉素
- 31186-13-7
- 6H-Dibenzo[b,d]pyran-2,6(4aH)-dione, 3,7-dihydroxy-9-methoxy-4a-methyl-, (4aS)-
- dehydroaltenusin