174402-32-5
基本信息
PF 804950
Edotecarin
Edotecarin (J 107088)
5H-Indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione, 12-β-D-glucopyranosyl-12,13-dihydro-2,10-dihydroxy-6-[[2-hydroxy-1-(hydroxymethyl)ethyl]amino]-
物理化学性质
| 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 | -20°C储存 |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 9.61±0.20(Predicted) |
| 形态 | Solid |
| 颜色 | Yellow to orange |
常见问题列表
|
Topoisomerase I 50 nM (IC 50 ) |
Protein Kinase C 160 μM (IC 50 ) |
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.
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.