| Identification | Back Directory | [Name]
Intoplicine | [CAS]
125974-72-3 | [Synonyms]
Intoplicine
11-(3-Dimethylaminopropylamino)-3-hydroxy-8-methyl-7H-benzo[e]pyrido[4,3-b]indole
7H-Benzo[e]pyrido[4,3-b]indol-3-ol, 11-[[3-(dimethylamino)propyl]amino]-8-methyl- | [Molecular Formula]
C21H24N4O | [MDL Number]
MFCD00866361 | [MOL File]
125974-72-3.mol | [Molecular Weight]
348.44 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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]
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[3]. | [IC 50]
Topoisomerase I; Topoisomerase II | [storage]
Store at -20°C | [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 |
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LGM Pharma
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www.lgmpharma.com |
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MedChemExpress
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