Indotecan
Based on 1 Customer Validation
Indotecan (LMP-400), an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.0%
- No. CAS: 915303-09-2
- Fòrmula: C26H26N2O7
- Peso molecular:478.49
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Almacenamiento:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Ver todos los productos específicos de isoformas Topoisomerase
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Actividad biológica
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Topoisomerase I |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | GI50 |
0.155 μM
Compound: 6, indotecan
|
Antiproliferative activity against human DU145 cells by SRB assay
Antiproliferative activity against human DU145 cells by SRB assay
|
[PMID: 21710981] |
| DU-145 | GI50 |
0.155 μM
Compound: 6; MP400; NSC 724998
|
Antiproliferative activity in human DU145 cells assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity in human DU145 cells assessed as cell growth inhibition after 48 hrs by SRB assay
|
[PMID: 27097152] |
| DU-145 | GI50 |
0.155 μM
Compound: 11
|
Cytotoxicity against human DU145 cell line
Cytotoxicity against human DU145 cell line
|
[PMID: 17034134] |
| DU-145 | GI50 |
0.155 μM
Compound: 5
|
Cytotoxicity against human DU145 cells
Cytotoxicity against human DU145 cells
|
[PMID: 20630766] |
| HCT-116 | GI50 |
1.15 μM
Compound: 6, indotecan
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Antiproliferative activity against human HCT116 cells by SRB assay
Antiproliferative activity against human HCT116 cells by SRB assay
|
[PMID: 21710981] |
| HCT-116 | GI50 |
1.15 μM
Compound: 6; MP400; NSC 724998
|
Antiproliferative activity in human HCT116 cells assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity in human HCT116 cells assessed as cell growth inhibition after 48 hrs by SRB assay
|
[PMID: 27097152] |
| HCT-116 | GI50 |
1.15 μM
Compound: 11
|
Cytotoxicity against human HCT116 cell line
Cytotoxicity against human HCT116 cell line
|
[PMID: 17034134] |
| HCT-116 | GI50 |
1.15 μM
Compound: 5
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Cytotoxicity against human HCT116 cells
Cytotoxicity against human HCT116 cells
|
[PMID: 20630766] |
| HOP-62 | GI50 |
1.78 μM
Compound: 6, indotecan
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Antiproliferative activity against human HOP62 cells by SRB assay
Antiproliferative activity against human HOP62 cells by SRB assay
|
[PMID: 21710981] |
| HOP-62 | GI50 |
1.78 μM
Compound: 6; MP400; NSC 724998
|
Antiproliferative activity in human HOP62 cells assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity in human HOP62 cells assessed as cell growth inhibition after 48 hrs by SRB assay
|
[PMID: 27097152] |
| HOP-62 | GI50 |
1.78 μM
Compound: 11
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Cytotoxicity against human HOP62 cell line
Cytotoxicity against human HOP62 cell line
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[PMID: 17034134] |
| HOP-62 | GI50 |
1.78 μM
Compound: 5
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Cytotoxicity against human HOP62 cells
Cytotoxicity against human HOP62 cells
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[PMID: 20630766] |
| MCF7 | GI50 |
0.37 μM
Compound: 6, indotecan
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Antiproliferative activity against human MCF7 cells by SRB assay
Antiproliferative activity against human MCF7 cells by SRB assay
|
[PMID: 21710981] |
| MCF7 | GI50 |
0.37 μM
Compound: 5
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Cytotoxicity against human MCF7 cells
Cytotoxicity against human MCF7 cells
|
[PMID: 20630766] |
| MCF7 | GI50 |
0.374 μM
Compound: 6; MP400; NSC 724998
|
Antiproliferative activity in human MCF7 cells assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity in human MCF7 cells assessed as cell growth inhibition after 48 hrs by SRB assay
|
[PMID: 27097152] |
| MDA-MB-435 | GI50 |
67.6 μM
Compound: 11
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Cytotoxicity against human MDA-MB-435 cell line
Cytotoxicity against human MDA-MB-435 cell line
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[PMID: 17034134] |
| OVCAR-3 | GI50 |
74.1 μM
Compound: 6, indotecan
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Antiproliferative activity against human OVCAR3 cells by SRB assay
Antiproliferative activity against human OVCAR3 cells by SRB assay
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[PMID: 21710981] |
| OVCAR-3 | GI50 |
74.1 μM
Compound: 11
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Cytotoxicity against human OVCAR-3 cell line
Cytotoxicity against human OVCAR-3 cell line
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[PMID: 17034134] |
| OVCAR-3 | GI50 |
74.1 μM
Compound: 5
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Cytotoxicity against human OVCAR-3 cells
Cytotoxicity against human OVCAR-3 cells
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[PMID: 20630766] |
| SF-539 | GI50 |
0.04 μM
Compound: 6, indotecan
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Antiproliferative activity against human SF539 cells by SRB assay
Antiproliferative activity against human SF539 cells by SRB assay
|
[PMID: 21710981] |
| SF-539 | GI50 |
0.04 μM
Compound: 6; MP400; NSC 724998
|
Antiproliferative activity in human SF539 cells assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity in human SF539 cells assessed as cell growth inhibition after 48 hrs by SRB assay
|
[PMID: 27097152] |
| SF-539 | GI50 |
0.04 μM
Compound: 11
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Cytotoxicity against human SF539 cell line
Cytotoxicity against human SF539 cell line
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[PMID: 17034134] |
| SF-539 | GI50 |
0.04 μM
Compound: 5
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Cytotoxicity against human SF539 cells
Cytotoxicity against human SF539 cells
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[PMID: 20630766] |
| SN12C | GI50 |
0.813 μM
Compound: 6, indotecan
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Antiproliferative activity against human SN12C cells by SRB assay
Antiproliferative activity against human SN12C cells by SRB assay
|
[PMID: 21710981] |
| SN12C | GI50 |
0.813 μM
Compound: 6; MP400; NSC 724998
|
Antiproliferative activity in human SN12C cells assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity in human SN12C cells assessed as cell growth inhibition after 48 hrs by SRB assay
|
[PMID: 27097152] |
| SN12C | GI50 |
0.813 μM
Compound: 11
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Cytotoxicity against human SN12C cell line
Cytotoxicity against human SN12C cell line
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[PMID: 17034134] |
| SN12C | GI50 |
0.813 μM
Compound: 5
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Cytotoxicity against human SN12C cells
Cytotoxicity against human SN12C cells
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[PMID: 20630766] |
| UACC-62 | GI50 |
0.03 μM
Compound: 6, indotecan
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Antiproliferative activity against human UACC62 cells by SRB assay
Antiproliferative activity against human UACC62 cells by SRB assay
|
[PMID: 21710981] |
| UACC-62 | GI50 |
0.03 μM
Compound: 6; MP400; NSC 724998
|
Antiproliferative activity in human UACC62 cells assessed as cell growth inhibition after 48 hrs by SRB assay
Antiproliferative activity in human UACC62 cells assessed as cell growth inhibition after 48 hrs by SRB assay
|
[PMID: 27097152] |
| UACC-62 | GI50 |
0.03 μM
Compound: 11
|
Cytotoxicity against human UACC62 cell line
Cytotoxicity against human UACC62 cell line
|
[PMID: 17034134] |
| UACC-62 | GI50 |
0.03 μM
Compound: 5
|
Cytotoxicity against human UACC62 cells
Cytotoxicity against human UACC62 cells
|
[PMID: 20630766] |
Indotecan (48 h) inhibits the proliferation of L. infantum promastigotes, ex vivo-infected splenocytes, and uninfected splenocytes, with IC50s of 0.10 μM, 0.10 μM, and 57.16 μM, respectively[2].
Indotecan (1.1-90 μM; 30 min) induces TopI-DNA complexes and inhibits DNA synthesis in L. infantum cultures[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.
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Animal Model:Female BALB/c mice (4-6 weeks) were infected with metacyclic parasites intravenously through the tail vein[2]
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Dosage:2.5 mg/kg body weight per injection
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Administration:Intraperitoneally every 2 days for 15 days (total, eight doses)
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Result:A drastic reduction of the number of transforming amastigotes recovered from the target organs of drug-treated animals was observed.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 915303-09-2
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Appearance Solid
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Peso molecular 478.49
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Fòrmula C26H26N2O7
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Color White to gray
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SMILES
O=C1C2=CC(OC)=C(OC)C=C2C3=C(C(C=C(OCO4)C4=C5)=C5C3=O)N1CCCN6CCOCC6
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Synonyms
LMP-400; NSC-724998
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvente y solubilidad
DMSO : 1.23 mg/mL (2.57 mM; ultrasonic and adjust pH to 6 with 1 M HCl; 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 (stored under nitrogen). 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 (stored under nitrogen). 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: ≥ 0.12 mg/mL (0.25 mM); Clear solution
This protocol yields a clear solution of ≥ 0.12 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (1.2 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: ≥ 0.12 mg/mL (0.25 mM); Clear solution
This protocol yields a clear solution of ≥ 0.12 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (1.2 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 (stored under nitrogen)
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.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Balaña-Fouce R, et, al. Indotecan (LMP400) and AM13-55: two novel indenoisoquinolines show potential for treating visceral leishmaniasis. Antimicrob Agents Chemother. 2012 Oct;56(10):5264-70. [Content Brief]
[2]. Seol Y, et, al. Single-Molecule Supercoil Relaxation Assay as a Screening Tool to Determine the Mechanism and Efficacy of Human Topoisomerase IB Inhibitors. Mol Cancer Ther. 2015 Nov;14(11):2552-9. [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 (stored under nitrogen). 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 | 2.0899 mL | 10.4495 mL | 20.8991 mL | 52.2477 mL |
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