1. Cell Cycle/DNA Damage
  2. Topoisomerase
  3. Intoplicine

Intoplicine 

Cat. No.: HY-101647
Handling Instructions

Intoplicine is a DNA topoisomerase I and II inhibitor.

For research use only. We do not sell to patients.

Intoplicine Chemical Structure

Intoplicine Chemical Structure

CAS No. : 125974-72-3

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Description

Intoplicine is a DNA topoisomerase I and II inhibitor.

IC50 & Target[1]

Topoisomerase I

 

Topoisomerase II

 

In Vitro

Activity of Intoplicine (RP60475), a new DNA topoisomerase I and II inhibitor, against human tumor colony-forming units in vitro. Intoplicine (RP60475) is the most active analogue evaluated in the 7H-benzo[e]-pyrido-[4,3-b]-indole series of antineoplastic compounds. Intoplicine exerts its activity through inhibition of DNA topoisomerase I and II[1]. Intoplicine is found to unwind DNA and to inhibit purified calf thymus topoisomerase II via a stabilization of the ternary cleavable complex[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

348.44

Formula

C₂₁H₂₄N₄O

CAS No.

125974-72-3

SMILES

OC1=CC=C2C3=C(NC4=C3C(NCCCN(C)C)=NC=C4C)C=CC2=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Kinase Assay
[2]

The assay is performed with various concentrations of calf thymus Topo II (20 to 0.1 decatenation units) in a 20 μL final reaction volume containing 0.25 μg of supercoiled pBR322 DNA, 20 mM Tris HC1 (pH 7.5), 60 mM KCl, 10 mM MgCl2, 30 μg /mL bovine serum albumin, 0.5 mM EDTA, 0.5 mM Dithiothreitol, and 1 μM Intoplicine or water. The final nucleotide concentration is 20.8 μM.The reaction is assembled in ice and the reaction mixture is then incubated at 37°C for 5 min. Then sample is mixed at room temperature with 20 μL of preaggregated silver hydrosol and immediately analyzed by SERS. Control experiments consisting of measurement of the SERS spectra of buffer alone, Topo II alone, Intoplicine alone (1μM), DNA alone, Topo II+Intoplicine, and DNA+Intoplicine are performed under the same conditions, except that distilled water is used to adjust the reaction volume to 20μL[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

The K562 human erythroleukemia cell line is established from a patient with chronic myelogenous leukemia. Cells are in the exponential growth phase at 5-8×105 in RPMI 1640 (GIBCO) supplemented with 10% fetal calf serum (Seromed) and 2 mM L-glutamine. Cell growth and viability are determined by phase contrast microscopy and by using the trypan blue test. Cells (2×106) are incubated with 1 μM Intoplicine for 1 h at 37°C, washed twice with PBS by centrifugation (200× g at 4°C) and resuspended in 200 μL PBS[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

IntoplicineTopoisomeraseInhibitorinhibitorinhibit

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