产品
编 号:F744162
分子式:C23H32N4O7S2
分子量:540.65
产品类型
结构图
CAS No: 133711-99-6
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产品详情
生物活性:
Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 105 /M) and thereby increases the length of linear DNA.
体内研究:
At the highest non-toxic dose (HNTD) (6 mg/kg/injection, total dose, 36 mg/kg), intoplicine dimesylate shows highly active with a T/C of 0% and a corresponding total log cell kill of 3.
体外研究:
With 1-hour exposure to Intoplicine dimesylate at final concentrations of 2.5 micrograms/mL and 10.0 micrograms/mL, 26% and 54% of the assessable specimens shows positive in vitro responses, respectively. With continuous exposure to Intoplicine dimesylate at concentrations of 0.25 micrograms/mL and 2.5 micrograms/mL, 16% and 71% of the assessable specimens showed positive responses, respectively. Activity is seen against breast (71%), non-small-cell lung (69%), and ovarian (45%) cancer colony-forming units at a Intoplicine dimesylate concentration of 10.0 micrograms/mL after 1-hour exposure.