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Intoplicine dimesylate

Catalog No. T38731 CAS 133711-99-6

Synonyms: RP 60475 dimesylate

Intoplicine (RP 60475) dimesylate is a DNA topoisomerase I and II inhibitor belonging to the 7H-benzo[e]pyrido[4,3-b]indole series. It exhibits a strong affinity for DNA (K A = 2 x 10^5 /M), resulting in increased linear DNA length.

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Intoplicine dimesylate Chemical Structure

Intoplicine dimesylate, CAS 133711-99-6

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Description	Intoplicine (RP 60475) dimesylate is a DNA topoisomerase I and II inhibitor belonging to the 7H-benzo[e]pyrido[4,3-b]indole series. It exhibits a strong affinity for DNA (K A = 2 x 10^5 /M), resulting in increased linear DNA length.
In vitro	Following exposure to Intoplicine dimesylate for one hour at concentrations of 2.5 and 10.0 micrograms/mL, in vitro assays demonstrated positive responses in 26% and 54% of the evaluated specimens, respectively[2]. Continuous exposure to the compound at lower concentrations of 0.25 and 2.5 micrograms/mL resulted in 16% and 71% of specimens showing positive responses, accordingly[2]. Notably, Intoplicine dimesylate exhibited activity against various cancer types, with efficacy observed in 71% of breast, 69% of non-small cell lung, and 45% of ovarian cancer colony-forming units at a concentration of 10.0 micrograms/mL following a one-hour exposure period[2].
In vivo	At the highest non-toxic dose (HNTD) of 6 mg/kg per injection (total dose of 36 mg/kg), intoplicine dimesylate demonstrated a significant activity level, evidenced by a tumor control (T/C) rate of 0% and an associated total log cell kill value of 3[3].

Synonyms	RP 60475 dimesylate
Molecular Weight	540.65
Formula	C23H32N4O7S2
CAS No.	133711-99-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Intoplicine dimesylate 133711-99-6 Intoplicine RP-60475 Dimesylate RP60475 Dimesylate RP60475 RP 60475 RP 60475 dimesylate Intoplicine Dimesylate RP-60475 RP 60475 Dimesylate inhibitor inhibit

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