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Art. -Nr.: HY-160005

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LMP517

(Synonyms: NSC 781517)

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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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Reinheit: 99.58%
CAS. Nr.: 1883730-99-1
Formel: C₂₂H₁₉FN₂O₅
Molecular Weight:410.40

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

LMP517 Chemical Structure

CAS. Nr.: 1883730-99-1

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Topoisomerase I

Topoisomerase II

Alle Topoisomerase Isoform-spezifische Produkte anzeigen :

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
DU-145	GI₅₀	0.033 μM Compound: 29	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	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	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	Cytotoxicity against human MCF7 cells by MTT assay Cytotoxicity against human MCF7 cells by MTT assay	[PMID: 26906474]
OVCAR-3	GI₅₀	0.076 μM Compound: 29	Cytotoxicity against human OVCAR3 cells by MTT assay Cytotoxicity against human OVCAR3 cells by MTT assay	[PMID: 26906474]
SF-539	GI₅₀	0.041 μM Compound: 29	Cytotoxicity against human SF539 cells by MTT assay Cytotoxicity against human SF539 cells by MTT assay	[PMID: 26906474]
SN12C	GI₅₀	0.107 μM Compound: 29	Cytotoxicity against human SN12C cells by MTT assay Cytotoxicity against human SN12C cells by MTT assay	[PMID: 26906474]
UACC-62	GI₅₀	0.028 μM Compound: 29	Cytotoxicity against human UACC62 cells by MTT assay Cytotoxicity against human UACC62 cells by MTT assay	[PMID: 26906474]

In Vitro

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.

Immunofluorescence^[2]

Cell Line:

HCT1116 cells
Concentration:

1 μM
Incubation Time:

1 h
Result:

IncreasedγH2AX production.

In Vivo

LMP517 (10 mg/kg, i.v., daily for 5 days) inhibits tumor growth and prolongs survival in H82 xenograft tumor mice models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

H82 xenograft tumor mice models^[1]
Dosage:

10 mg/kg
Administration:

Intravenously injection, daily for 5 days
Result:

Induced a reduction in tumor growth.
Prolonged survival of mice.
Had marginal body weight lost.

Chemical Information

CAS. Nr. 1883730-99-1
Appearance Solid
Molecular Weight 410.40
Formel C₂₂H₁₉FN₂O₅
Color Deep purple to brown
SMILES

O=C1C2=CC3=C(C=C2C4=C1C5=C(C(N4CCCNCCO)=O)C=C(F)C=C5)OCO3
Synonyms

NSC 781517
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.4366 mL

12.1832 mL

24.3665 mL

5 mM

0.4873 mL

2.4366 mL

4.8733 mL

10 mM

0.2437 mL

1.2183 mL

2.4366 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise

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LMP517

Alle Topoisomerase Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LMP517 Related Classifications

HY-160005 Related Classifications