Intoplicine
Based on 1 Customer Validation
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.
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- Purity: 98.36%
- CAS No.: 125974-72-3
- 화학식: C21H24N4O
- 분자량:348.44
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보관:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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All Topoisomerase Isoforms
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Biological Activity
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Topoisomerase I |
Topoisomerase II |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | IC50 |
0.56 μM
Compound: Intoplicine
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Antiproliferative activity against human DU145 prostate cell line
Antiproliferative activity against human DU145 prostate cell line
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[PMID: 10498216] |
| HT-29 | IC50 |
0.89 μM
Compound: Intoplicine
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Antiproliferative activity against human HT-29 colon cell line
Antiproliferative activity against human HT-29 colon cell line
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[PMID: 10498216] |
| MCF7 | IC50 |
1 μM
Compound: Intoplicine
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Antiproliferative activity against human MCF-7 breast cell line
Antiproliferative activity against human MCF-7 breast cell line
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[PMID: 10498216] |
| SK-OV-3 | IC50 |
0.45 μM
Compound: Intoplicine
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Antiproliferative activity against human SKOV-3 ovarian cell line
Antiproliferative activity against human SKOV-3 ovarian cell line
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[PMID: 10498216] |
With 1-hour exposure to Intoplicine at final concentrations of 2.5 micrograms/mL and 10.0 micrograms/mL, 26% and 54% of the assessable specimens shows positive in vitro responses, respectively[2].
With continuous exposure to Intoplicine at concentrations of 0.25 micrograms/mL and 2.5 micrograms/mL, 16% and 71% of the assessable specimens showed positive responses, respectively[2].
Activity is seen against breast (71%), non-small-cell lung (69%), and ovarian (45%) cancer colony-forming units at a Intoplicine concentration of 10.0 micrograms/mL after 1-hour exposure[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 125974-72-3
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Appearance Solid
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분자량 348.44
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화학식 C21H24N4O
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Color White to off-white
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SMILES
OC1=CC=C2C3=C(NC4=C3C(NCCCN(C)C)=NC=C4C)C=CC2=C1
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Synonyms
RP 60475
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
용액&용해도
DMSO : 80 mg/mL (229.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (5.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (5.74 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (285 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8699 mL | 14.3497 mL | 28.6993 mL | 71.7484 mL |
| 5 mM | 0.5740 mL | 2.8699 mL | 5.7399 mL | 14.3497 mL | |
| 10 mM | 0.2870 mL | 1.4350 mL | 2.8699 mL | 7.1748 mL | |
| 15 mM | 0.1913 mL | 0.9566 mL | 1.9133 mL | 4.7832 mL | |
| 20 mM | 0.1435 mL | 0.7175 mL | 1.4350 mL | 3.5874 mL | |
| 25 mM | 0.1148 mL | 0.5740 mL | 1.1480 mL | 2.8699 mL | |
| 30 mM | 0.0957 mL | 0.4783 mL | 0.9566 mL | 2.3916 mL | |
| 40 mM | 0.0717 mL | 0.3587 mL | 0.7175 mL | 1.7937 mL | |
| 50 mM | 0.0574 mL | 0.2870 mL | 0.5740 mL | 1.4350 mL | |
| 60 mM | 0.0478 mL | 0.2392 mL | 0.4783 mL | 1.1958 mL | |
| 80 mM | 0.0359 mL | 0.1794 mL | 0.3587 mL | 0.8969 mL | |
| 100 mM | 0.0287 mL | 0.1435 mL | 0.2870 mL | 0.7175 mL |
Intoplicine Related Classifications
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