LMP517
Based on 1 Customer Validation
LMP517 (NSC 781517) is a potent and non-camptothecin Topoisomerase I and II (TOP1 and TOP2) dual inhibitor. LMP517 can induce TOP1 and TOP2 cleavage complexes (TOP1ccs and TOP2ccs). LMP517 can induce cancer cells DNA damage and γH2AX production. LMP517 can be used for the research of cancer, such as small cell lung cancer.
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- Pureza: 99.58%
- No. CAS: 1883730-99-1
- Fòrmula: C22H19FN2O5
- Peso molecular:410.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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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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Topoisomerase I |
Topoisomerase II |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | GI50 |
0.033 μM
Compound: 29
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Cytotoxicity against human DU145 cells by MTT assay
Cytotoxicity against human DU145 cells by MTT assay
|
[PMID: 26906474] |
| HCT-116 | GI50 |
0.019 μM
Compound: 29
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Cytotoxicity against human HCT116 cells by MTT assay
Cytotoxicity against human HCT116 cells by MTT assay
|
[PMID: 26906474] |
| HOP-62 | GI50 |
0.036 μM
Compound: 29
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Cytotoxicity against human HOP62 cells by MTT assay
Cytotoxicity against human HOP62 cells by MTT assay
|
[PMID: 26906474] |
| MCF7 | GI50 |
<0.01 μM
Compound: 29
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Cytotoxicity against human MCF7 cells by MTT assay
Cytotoxicity against human MCF7 cells by MTT assay
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[PMID: 26906474] |
| OVCAR-3 | GI50 |
0.076 μM
Compound: 29
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Cytotoxicity against human OVCAR3 cells by MTT assay
Cytotoxicity against human OVCAR3 cells by MTT assay
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[PMID: 26906474] |
| SF-539 | GI50 |
0.041 μM
Compound: 29
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Cytotoxicity against human SF539 cells by MTT assay
Cytotoxicity against human SF539 cells by MTT assay
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[PMID: 26906474] |
| SN12C | GI50 |
0.107 μM
Compound: 29
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Cytotoxicity against human SN12C cells by MTT assay
Cytotoxicity against human SN12C cells by MTT assay
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[PMID: 26906474] |
| UACC-62 | GI50 |
0.028 μM
Compound: 29
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Cytotoxicity against human UACC62 cells by MTT assay
Cytotoxicity against human UACC62 cells by MTT assay
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[PMID: 26906474] |
LMP517 (0-125 nM, 72 h) shows IC50 values of 11, 18 and 32 nM in DT40 tdp2, tdp1 and WT cells[1].
LMP517 (0.1-30 μM, 1 h) induces TOP1cc, TOP2cc, TOP2α and TOP2βccs production in HCT116 and TK6 cells[1].
LMP517 (0.05-1 μM, 1 h) induces DNA damage and histone γH2AX production in HCT116 FUCCI cells[1].
LMP517 (1 μM, 1 h) induces TOP1cc and DPC production in CCR-CEM cells[2].
LMP517 (0.1-1 μM, 0.5-1 h) induces γH2AX production in HCT1116 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT1116 cells
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Concentration:1 μM
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Incubation Time:1 h
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Result:IncreasedγH2AX production.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:H82 xenograft tumor mice models[1]
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Dosage:10 mg/kg
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Administration:Intravenously injection, daily for 5 days
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Result:Induced a reduction in tumor growth.
Prolonged survival of mice.
Had marginal body weight lost.
Chemical Information
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No. CAS 1883730-99-1
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Appearance Solid
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Peso molecular 410.40
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Fòrmula C22H19FN2O5
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Color Deep purple to brown
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SMILES
O=C1C2=CC3=C(C=C2C4=C1C5=C(C(N4CCCNCCO)=O)C=C(F)C=C5)OCO3
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Synonyms
NSC 781517
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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 : 44 mg/mL (107.21 mM; ultrasonic and adjust pH to 1 with TFA; 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 (277 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]. Marzi L, et al. The Indenoisoquinoline LMP517: A Novel Antitumor Agent Targeting both TOP1 and TOP2. Mol Cancer Ther. 2020 Aug;19(8):1589-1597. [Content Brief]
[2]. Marzi L, et al. Novel Fluoroindenoisoquinoline Non-Camptothecin Topoisomerase I Inhibitors. Mol Cancer Ther. 2018 Aug;17(8):1694-1704. [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 | 2.4366 mL | 12.1832 mL | 24.3665 mL | 60.9162 mL |
| 5 mM | 0.4873 mL | 2.4366 mL | 4.8733 mL | 12.1832 mL | |
| 10 mM | 0.2437 mL | 1.2183 mL | 2.4366 mL | 6.0916 mL | |
| 15 mM | 0.1624 mL | 0.8122 mL | 1.6244 mL | 4.0611 mL | |
| 20 mM | 0.1218 mL | 0.6092 mL | 1.2183 mL | 3.0458 mL | |
| 25 mM | 0.0975 mL | 0.4873 mL | 0.9747 mL | 2.4366 mL | |
| 30 mM | 0.0812 mL | 0.4061 mL | 0.8122 mL | 2.0305 mL | |
| 40 mM | 0.0609 mL | 0.3046 mL | 0.6092 mL | 1.5229 mL | |
| 50 mM | 0.0487 mL | 0.2437 mL | 0.4873 mL | 1.2183 mL | |
| 60 mM | 0.0406 mL | 0.2031 mL | 0.4061 mL | 1.0153 mL | |
| 80 mM | 0.0305 mL | 0.1523 mL | 0.3046 mL | 0.7615 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2437 mL | 0.6092 mL |
LMP517 Related Classifications
HY-160005 Related Classifications
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