Lucanthone
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Lucanthone is an endonuclease inhibitor of Apurinic endonuclease-1 (APE-1).
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- Reinheit: 99.63%
- CAS. Nr.: 479-50-5
- Formel: C20H24N2OS
- Molecular Weight:340.48
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
APE-1[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BT-20 | IC50 |
5.7 μM
Compound: Lucanthone
|
Cytotoxicity against human BT20 cells after 72 hrs by MTT assay
Cytotoxicity against human BT20 cells after 72 hrs by MTT assay
|
[PMID: 25699157] |
| BT-474 | IC50 |
5.7 μM
Compound: Lucanthone
|
Cytotoxicity against human BT474 cells after 72 hrs by MTT assay
Cytotoxicity against human BT474 cells after 72 hrs by MTT assay
|
[PMID: 25699157] |
| HCC1937 | IC50 |
5.7 μM
Compound: Lucanthone
|
Cytotoxicity against human HCC1937 cells after 72 hrs by MTT assay
Cytotoxicity against human HCC1937 cells after 72 hrs by MTT assay
|
[PMID: 25699157] |
| HCC1954 | IC50 |
5.7 μM
Compound: Lucanthone
|
Cytotoxicity against human HCC1954 cells after 72 hrs by MTT assay
Cytotoxicity against human HCC1954 cells after 72 hrs by MTT assay
|
[PMID: 25699157] |
| MDA-MB-231 | IC50 |
5.7 μM
Compound: Lucanthone
|
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
|
[PMID: 25699157] |
| MDA-MB-435 | IC50 |
5.7 μM
Compound: Lucanthone
|
Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay
|
[PMID: 25699157] |
| SK-BR-3 | IC50 |
5.7 μM
Compound: Lucanthone
|
Cytotoxicity against human SKBR3 cells after 72 hrs by MTT assay
Cytotoxicity against human SKBR3 cells after 72 hrs by MTT assay
|
[PMID: 25699157] |
| Vero 76 | IC50 |
12.4 μM
Compound: 19
|
Cytotoxicity against green monkey Vero 76 cells incubated for 48 to 96 hrs by crystal violet staining assay
Cytotoxicity against green monkey Vero 76 cells incubated for 48 to 96 hrs by crystal violet staining assay
|
[PMID: 36753881] |
Lucanthone is a novel inhibitor of autophagy that induces cathepsin D-mediated apoptosis. To investigate the anticancer activity of Lucanthone, cell viability is measured by MTT assay. Lucanthone reduces cell viability to a similar extent in a panel of seven breast cancer cell lines. In addition, a direct comparison reveals that Lucanthone is significantly more potent than Chloroquine (CQ) at reducing breast cancer cell viability with a mean IC50 of 7.2 μM versus 66 μM for CQ. Measurement of cell viability in two representative cell lines (MDA-MB-231 and BT-20) by ATPlite assay and trypan blue exclusion reveals comparable results[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 479-50-5
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Appearance Solid
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Molecular Weight 340.48
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Formel C20H24N2OS
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Color Off-white to orange
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SMILES
O=C1C2=C(SC3=C1C=CC=C3)C(C)=CC=C2NCCN(CC)CC
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
DMSO : 25 mg/mL (73.43 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
Cell viability is assessed by MTT assay. Cells are seeded into 96-well microculture plates at 10,000 cells per well and allowed to attach for 24 h. Cells are then treated with Lucanthone (0, 0.5, 1, 5, 10, 20 and 40 μM), Chloroquine, Vorinostat, or combinations for 72 h. Following drug treatment, MTT is added and cell viability is quantified using a BioTek microplate reader. Effects on cell viability are also determined by measuring ATP levels using the ATPlite assay system and by trypan blue exclusion. Pro-apoptotic effects following in vitro drug exposure are quantified by propidium iodide (PI) staining and fluorescence-activated cell sorting (FACS) analysis of sub-G0/G1 DNA content[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (274 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)
Verweise
[1]. Chowdhury SM, et al. Graphene nanoribbons as a drug delivery agent for lucanthone mediated therapy of glioblastoma multiforme. Nanomedicine. 2015 Jan;11(1):109-18. [Content Brief]
[2]. Carew JS, et al. Lucanthone is a novel inhibitor of autophagy that induces cathepsin D-mediated apoptosis. J Biol Chem. 2011 Feb 25;286(8):6602-13. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9370 mL | 14.6851 mL | 29.3703 mL | 73.4257 mL |
| 5 mM | 0.5874 mL | 2.9370 mL | 5.8741 mL | 14.6851 mL | |
| 10 mM | 0.2937 mL | 1.4685 mL | 2.9370 mL | 7.3426 mL | |
| 15 mM | 0.1958 mL | 0.9790 mL | 1.9580 mL | 4.8950 mL | |
| 20 mM | 0.1469 mL | 0.7343 mL | 1.4685 mL | 3.6713 mL | |
| 25 mM | 0.1175 mL | 0.5874 mL | 1.1748 mL | 2.9370 mL | |
| 30 mM | 0.0979 mL | 0.4895 mL | 0.9790 mL | 2.4475 mL | |
| 40 mM | 0.0734 mL | 0.3671 mL | 0.7343 mL | 1.8356 mL | |
| 50 mM | 0.0587 mL | 0.2937 mL | 0.5874 mL | 1.4685 mL | |
| 60 mM | 0.0490 mL | 0.2448 mL | 0.4895 mL | 1.2238 mL |