174402-32-5
- CAS号:174402-32-5
- 英文名:Edotecarin
- 中文名:174402-32-5
- CBNumber:CB42583033
- 分子式:C29H28N4O11
- 分子量:608.56
- MOL File:174402-32-5.mol
- 熔点 :330° (dec)
- 比旋光度 :D23 +117° (c = 0.8 in 1:1 acetonitrile/water)
- 沸点 :1047.5±75.0 °C(Predicted)
- 密度 :1.96±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 形态 :Solid
- 酸度系数(pKa) :9.61±0.20(Predicted)
- 颜色 :Yellow to orange
174402-32-5性质、用途与生产工艺
- 生物活性 Edotecarin 是一种有效的 topoisomerase I 抑制剂,可诱导单链 DNA 断裂,IC50 值为 50 nM。
-
靶点
Topoisomerase I
50 nM (IC 50 )
Protein Kinase C
160 μM (IC 50 )
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体外研究
In the presence of human colon cancer cells labeled with 3 Hthymidine, edotecarin (0.6 μmol/L) increases the formation of DNA-protein complexes in a time-dependent manner.
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体内研究
Edotecarin produces an 83% increase in survival in mice bearing intracranial D-456MG glioma and shows a strong antimetastatic effect. Edotecarin results in tumor growth delays ranging from 10.45 days at the lowest dose (3 mg/kg) to 24.83 days at the highest (100 mg/kg). Combination treatment of edotecarin plus irinotecan improves antitumor activity in vivo compared with either agent alone.
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