10-HydroxycAMPothecin 是具有抗癌活性的喜树碱衍生物,摘自专利文献 WO1999001456A1 中的化合物 23c。
产品描述
10-Hydroxycamptothecin is a DNA topoisomerase I inhibitor, utilized as a clinical therapy agent against hepatoma.
体外活性
In vitro, the 10-hydroxycamptothecin nanosuspensions released the encapsulated drug with nearly zero-order kinetics, and the accumulative release reached 90% within 72 hours. In vitro cytotoxicity assay showed that the 10-hydroxycamptothecin nanosuspensions had significantly enhanced cytotoxicity against HepG2 cells compared to the commercially available 10-hydroxycamptothecin injections [1].
体内活性
The in vivo study with H22 tumor-bearing mice and intravenous injection of the drug showed that in contrast to the 10-hydroxycamptothecin injections, the 10-hydroxycamptothecin nanosuspensions exhibited significantly enhanced biodistribution, particularly in the lung (393.40-fold AUC0–24 h, liver (192.35-fold AUC0–24 h, spleen (141.67-fold AUC0–24 h and tumor (64.21-fold AUC0–24 h. The 10-hydroxycamptothecin nanosuspensions also showed improved antitumor therapeutic efficacy over the injections (89.83% vs. 30.56%) [1].
Cas No.
67656-30-8
分子式
C20H16N2O5
分子量
364.35
别名
9-羟基喜树碱
储存和溶解度
H2O:Insoluble
DMSO:8 mg/mL (21.95 mM),warmed
Ethanol:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years