Indimitecan
Based on 1 Customer Validation
Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.30%
- No. CAS: 915360-05-3
- Fòrmula: C25H21N3O6
- Peso molecular:459.45
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
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Actividad biológica
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Top1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | GI50 |
<0.01 μM
Compound: 7, indimitecan
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Antiproliferative activity against human DU145 cells by SRB assay
Antiproliferative activity against human DU145 cells by SRB assay
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[PMID: 21710981] |
| DU-145 | GI50 |
<0.01 μM
Compound: 6
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Cytotoxicity against human DU145 cells
Cytotoxicity against human DU145 cells
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[PMID: 20630766] |
| HCT-116 | GI50 |
<0.01 μM
Compound: 7, indimitecan
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Antiproliferative activity against human HCT116 cells by SRB assay
Antiproliferative activity against human HCT116 cells by SRB assay
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[PMID: 21710981] |
| HCT-116 | GI50 |
<0.01 μM
Compound: 6
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Cytotoxicity against human HCT116 cells
Cytotoxicity against human HCT116 cells
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[PMID: 20630766] |
| HOP-62 | GI50 |
<0.01 μM
Compound: 7, indimitecan
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Antiproliferative activity against human HOP62 cells by SRB assay
Antiproliferative activity against human HOP62 cells by SRB assay
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[PMID: 21710981] |
| HOP-62 | GI50 |
<0.01 μM
Compound: 6
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Cytotoxicity against human HOP62 cells
Cytotoxicity against human HOP62 cells
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[PMID: 20630766] |
| L1210 | EC50 |
0.06 μM
Compound: 19
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Trypanocidal activity against Trypanosoma brucei brucei 427 bloodstream forms infected in mouse L1210 cells after 48 hrs
Trypanocidal activity against Trypanosoma brucei brucei 427 bloodstream forms infected in mouse L1210 cells after 48 hrs
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[PMID: 18824603] |
| MCF7 | GI50 |
0.01 μM
Compound: 7, indimitecan
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Antiproliferative activity against human MCF7 cells by SRB assay
Antiproliferative activity against human MCF7 cells by SRB assay
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[PMID: 21710981] |
| MCF7 | GI50 |
0.01 μM
Compound: 6
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Cytotoxicity against human MCF7 cells
Cytotoxicity against human MCF7 cells
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[PMID: 20630766] |
| OVCAR-3 | GI50 |
0.085 μM
Compound: 7, indimitecan
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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 |
0.085 μM
Compound: 6
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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 |
0.037 μM
Compound: 7, indimitecan
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Antiproliferative activity against human SF539 cells by SRB assay
Antiproliferative activity against human SF539 cells by SRB assay
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[PMID: 21710981] |
| SF-539 | GI50 |
0.037 μM
Compound: 6
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Cytotoxicity against human SF539 cells
Cytotoxicity against human SF539 cells
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[PMID: 20630766] |
| SN12C | GI50 |
<0.01 μM
Compound: 7, indimitecan
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Antiproliferative activity against human SN12C cells by SRB assay
Antiproliferative activity against human SN12C cells by SRB assay
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[PMID: 21710981] |
| SN12C | GI50 |
<0.01 μM
Compound: 6
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Cytotoxicity against human SN12C cells
Cytotoxicity against human SN12C cells
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[PMID: 20630766] |
| UACC-62 | GI50 |
<0.01 μM
Compound: 7, indimitecan
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Antiproliferative activity against human UACC62 cells by SRB assay
Antiproliferative activity against human UACC62 cells by SRB assay
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[PMID: 21710981] |
| UACC-62 | GI50 |
<0.01 μM
Compound: 6
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Cytotoxicity against human UACC62 cells
Cytotoxicity against human UACC62 cells
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[PMID: 20630766] |
Indimitecan (LMP776) (0-100 μM) shows antiproliferative potencies against various human cancer cell lines, with mean-graph midpoint (MGM) of 0.079 ± 0.023 μM[1].
Indimitecan shows potent DNA cleavage due to Top1 inhibition[1].
Indimitecan can be substrates for metabolic ketone reductases[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HOP-62, HCT-116, SF-539, UACC-62, OVCAR-3, SN12C, DU-145, MCF-7
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Concentration:0-100 μM
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Incubation Time:
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Result:Showed growth inhibition with GI50s of <0.01, <0.01, 0.04, <0.01, 0.08, <0.01, <0.01 and 0.01 μM against HOP-62, HCT-116, SF-539, UACC-62, OVCAR-3, SN12C, DU-145 and MCF-7 cells, respectively. And the mean-graph midpoint (MGM) for growth inhibition of all human cancer cell lines successfully tested (the National Cancer Institute’s developmental therapeutics assay (the “NCI60”)) was 0.079 ± 0.023 μM.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 915360-05-3
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Appearance Solid
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Peso molecular 459.45
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Fòrmula C25H21N3O6
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Color Brown to black
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SMILES
O=C1C2=CC(OC)=C(OC)C=C2C3=C(C(C=C(OCO4)C4=C5)=C5C3=O)N1CCCN6C=NC=C6
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Synonyms
LMP776
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 8.33 mg/mL (18.13 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C; 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. 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. 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)
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Cinelli MA, et al. Identification, synthesis, and biological evaluation of metabolites of the experimental cancer treatment drugs indotecan (LMP400) and indimitecan (LMP776) and investigation of isomerically hydroxylated indenoisoquinoline analogues as topoisomerase I poisons. J Med Chem. 2012 Dec 27;55(24):10844-62. [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. 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 | 2.1765 mL | 10.8826 mL | 21.7652 mL | 54.4129 mL |
| 5 mM | 0.4353 mL | 2.1765 mL | 4.3530 mL | 10.8826 mL | |
| 10 mM | 0.2177 mL | 1.0883 mL | 2.1765 mL | 5.4413 mL | |
| 15 mM | 0.1451 mL | 0.7255 mL | 1.4510 mL | 3.6275 mL |
Indimitecan Related Classifications
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