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Intoplicine dimesylate

CAS No. : 133711-99-6

MCE 站：Intoplicine dimesylate

产品活性：Intoplicine (RP 60475) dimesylate，一种 7H 苯并 [e] 吡啶并 [4,3-b] 吲哚系列的抗肿瘤衍生物，是一种 DNA 拓扑异构酶 I 和 II 抑制剂。Intoplicine dimesylate 与 DNA (K_A = 2 x 10⁵ /M) 强烈结合，从而增加线性 DNA 的长度。

研究领域：Cell Cycle/DNA Damage

作用靶点：Topoisomerase

In Vitro: 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.

In Vivo: 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.

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