Intoplicine Chemical Properties

Melting point:

216-218 °C

Boiling point:

635.5±55.0 °C(Predicted)

Density 

1.286±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

Soluble in DMSO

form 

Solid

pka

8.26±0.30(Predicted)

color 

White to off-white

Intoplicine Usage And Synthesis

Uses

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 (KA = 2 x 105 /M) and thereby increases the length of linear DNA[1][2].

Definition

ChEBI: Intoplicine is a pyridoindole.

in vivo

IC 50

Topoisomerase I; Topoisomerase II

References

[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. DOI:10.1093/jnci/86.1.30
[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. PMID:8402662
[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. DOI:10.1007/BF00874425

Intoplicine(125974-72-3)Related Product Information

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