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Intoplicine dimesylate
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Intoplicine dimesylate图片
CAS NO: 133711-99-6
包装与价格：
包装 价格(元)
5mg 电议
10mg 电议

半岛bd体育手机客户端 介绍
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 (KA = 2 x 105 /M) 强烈结合，从而增加线性 DNA 的长度。
Cas No. 133711-99-6
别名 RP 60475 dimesylate
分子式 C23H32N4O7S2
分子量 540.65
溶解度 DMSO : 115 mg/mL (212.71 mM; Need ultrasonic)
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
半岛bd体育手机客户端 描述

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[1][2].

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[2]. 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[2]. 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[2].

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[3].

[1]. Riou JF, et al. Intoplicine (RP 60475) and its derivatives, a new class of antitumor agents inhibiting both topoisomerase I and II activities. Cancer Res. 1993;53(24):5987-5993.
[2]. Eckardt JR, et al. Activity of intoplicine (RP60475), a new DNA topoisomerase I and II inhibitor, against human tumor colony-forming units in vitro. J Natl Cancer Inst. 1994;86(1):30-33.
[3]. Bissery MC, et al. Antitumor activity of intoplicine (RP 60475, NSC 645008), a new benzo-pyrido-indole: evaluation against solid tumors and leukemias in mice. Invest New Drugs. 1993;11(4):263-277.
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