Intoplicine (RP 60475)，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 与 DNA (K_A = 2 x 10⁵ /M) 强烈结合，从而增加线性 DNA 的长度。

Intoplicine (RP 60475), an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine strongly binds DNA (K A = 2 x 10 /M) and thereby increases the length of linear DNA.

Solid

Topoisomerase I Topoisomerase II

With 1-hour exposure to Intoplicine 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 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 concentration of 10.0 micrograms/mL after 1-hour exposure. has not independently confirmed the accuracy of these methods. They are for reference only.

At the highest non-toxic dose (HNTD) (6 mg/kg/injection, total dose, 36 mg/kg), Intoplicine shows highly active with a T/C of 0% and a corresponding total log cell kill of 3. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

[1]. 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 Jan 5;86(1):30-3.
[2]. Morjani H, et al. Molecular and cellular interactions between Intoplicine, DNA, and topoisomerase II studied by surface-enhanced Raman scattering spectroscopy. Cancer Res. 1993 Oct 15;53(20):4784-90.

In Vitro: DMSO : 80 mg/mL (229.59 mM; Need ultrasonic)配制储备液