125974-72-3
125974-72-3 structure
- Name: Intoplicine
- Chemical Name: Intoplicine
- CAS Number: 125974-72-3
- Molecular Formula: C21H24N4O
- Molecular Weight: 348.44100
- Catalog: Research Areas Cancer
- Create Date: 2018-03-15 08:00:00
- Modify Date: 2024-01-08 16:33:10
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Intoplicine is a DNA topoisomerase I and II inhibitor.
| Name | Intoplicine |
|---|---|
| Synonyms |
11-((3-(Dimethylamino)propyl)amino)-8-methyl-7H-benzo(e)pyrido(4,3-b)indol-3-ol
UNII-FB2CIN6HMI |
| Description | Intoplicine is a DNA topoisomerase I and II inhibitor. |
|---|---|
| Related Catalog | |
| Target |
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]. |
| Kinase Assay | 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]. |
| Cell Assay | 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]. |
| References |
| Density | 1.286g/cm3 |
|---|---|
| Boiling Point | 635.5ºC at 760mmHg |
| Molecular Formula | C21H24N4O |
| Molecular Weight | 348.44100 |
| Flash Point | 338.2ºC |
| Exact Mass | 348.19500 |
| PSA | 64.18000 |
| LogP | 4.31990 |
| Vapour Pressure | 9.55E-17mmHg at 25°C |
| Index of Refraction | 1.755 |
| Storage condition | 2-8℃ |
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125974-72-3 |
| Literature: Nguyen; Lhoste; Lavelle; Bissery; Bisagni Journal of Medicinal Chemistry, 1990 , vol. 33, # 5 p. 1519 - 1528 |
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125974-72-3 |
| Literature: Nguyen; Lhoste; Lavelle; Bissery; Bisagni Journal of Medicinal Chemistry, 1990 , vol. 33, # 5 p. 1519 - 1528 |
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125974-72-3 |
| Literature: Nguyen; Lhoste; Lavelle; Bissery; Bisagni Journal of Medicinal Chemistry, 1990 , vol. 33, # 5 p. 1519 - 1528 |
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125974-72-3 |
| Literature: Nguyen; Lhoste; Lavelle; Bissery; Bisagni Journal of Medicinal Chemistry, 1990 , vol. 33, # 5 p. 1519 - 1528 |
| Precursor 1 | |
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| DownStream 0 | |