Belotecan hydrochloride 是一种合成的水溶性喜树碱衍生物和拓扑异构酶 I 抑制剂，具有潜在的抗肿瘤活性。

Belotecan hydrochloride is a synthetic water-soluble camptothecin derivative and topoisomerase I inhibitor with potential antitumor activity

Belotecan hydrochloride(CKD-602) was revealed to exert a significant cytotoxic effect on all cell lines in a time- and dose-dependent manner.?The cell viability IC50 values were 2.4 μg/ml for YD-8, 0.18 μg/ml for YD-9 and 0.05 μg/ml for YD-38 cells at 72 h following treatment[1].

Cells at a density of 2×10^4 cells/well in 100 μl RPMI with 10% FBS were added to the wells of a 96-well plate.?The cells were treated with different concentrations (0.01, 0.1, 0.5, 1, 5 and 10 μg/ml) of CKD-602 for 24, 48 and 72 h. Control samples of each cell line were treated with medium only.?For the viability assay, 20 μl/well CellTiter 96AQueous One Solution Reagent (MTS) was added.?After 1 h incubation at 37°C in a humidified atmosphere of 5% CO2, the absorbance at 490 nm was recorded using an ELISA plate reader ?The assay was performed in triplicate with three independent experiments for each condition.?The data from the treatment groups were normalized to those of the control samples and are presented as the mean ±standard error of the mean.?The half maximal (50%) inhibitory concentration (IC50) values were calculated from the dose-response curve[1].

213819-48-8

C25H28ClN3O4

469.97

CKD-602

DMSO:50 mg/mL (106.39 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years