Art. -Nr.: HY-U00248A

LMP744 hydrochloride

(Synonyms: MJ-III65 hydrochloride; NSC706744 hydrochloride)

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LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.

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Reinheit: 99.08%
CAS. Nr.: 308246-57-3
Formel: C₂₄H₂₅ClN₂O₇
Molecular Weight:488.92

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

LMP744 hydrochloride Chemical Structure

CAS. Nr.: 308246-57-3

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

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

Biologische Aktivität

Beschreibung

LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity^[1].

IC₅₀ & Target

Top1

Alle Topoisomerase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
DU-145	GI₅₀	<0.01 μM Compound: 19a	Antiproliferative activity was determined for 50% growth inhibition against human Prostate c Antiproliferative activity was determined for 50% growth inhibition against human Prostate c	[PMID: 11020283]
DU-145	GI₅₀	>0.01 μM Compound: 5	Growth inhibitory activity against human prostate DU-145 cell line Growth inhibitory activity against human prostate DU-145 cell line	[PMID: 15509164]
HCT-116	GI₅₀	0.1 μM Compound: 19a	Antiproliferative activity was determined for 50% growth inhibition against human colon HCT116 cell line Antiproliferative activity was determined for 50% growth inhibition against human colon HCT116 cell line	[PMID: 11020283]
HCT-116	GI₅₀	0.1 μM Compound: 5	Growth inhibitory activity against human colon HCT116 cell line Growth inhibitory activity against human colon HCT116 cell line	[PMID: 15509164]
HOP-62	GI₅₀	0.02 μM Compound: 19a	Antiproliferative activity was determined for 50% growth inhibition against human lung HOP-62 cell line Antiproliferative activity was determined for 50% growth inhibition against human lung HOP-62 cell line	[PMID: 11020283]
HOP-62	GI₅₀	0.02 μM Compound: 5	Growth inhibitory activity against human lung HOP-62 cell line Growth inhibitory activity against human lung HOP-62 cell line	[PMID: 15509164]
MDA-MB-435	GI₅₀	0.79 μM Compound: 19a	Antiproliferative activity was determined for 50% growth inhibition against human breast MDA-MB-435 cell line Antiproliferative activity was determined for 50% growth inhibition against human breast MDA-MB-435 cell line	[PMID: 11020283]
MDA-MB-435	GI₅₀	0.79 μM Compound: 5	Growth inhibitory activity against human breast MDA-MB-435 cell line Growth inhibitory activity against human breast MDA-MB-435 cell line	[PMID: 15509164]
OVCAR-3	GI₅₀	0.35 μM Compound: 19a	Antiproliferative activity was determined for 50% growth inhibition against human ovarian OVCAR-3 cell line Antiproliferative activity was determined for 50% growth inhibition against human ovarian OVCAR-3 cell line	[PMID: 11020283]
OVCAR-3	GI₅₀	0.35 μM Compound: 5	Growth inhibitory activity against human ovarian OVCAR-3 cell line Growth inhibitory activity against human ovarian OVCAR-3 cell line	[PMID: 15509164]
SF-539	GI₅₀	0.04 μM Compound: 19a	Antiproliferative activity was determined for 50% growth inhibition against human CNS SF-539 cell line Antiproliferative activity was determined for 50% growth inhibition against human CNS SF-539 cell line	[PMID: 11020283]
SN12C	GI₅₀	<0.01 μM Compound: 19a	Antiproliferative activity was determined for 50% growth inhibition against human renal SN12C cell line Antiproliferative activity was determined for 50% growth inhibition against human renal SN12C cell line	[PMID: 11020283]
SN12C	GI₅₀	>0.01 μM Compound: 5	Growth inhibitory activity against human renal SN12C cell line Growth inhibitory activity against human renal SN12C cell line	[PMID: 15509164]
UACC-62	GI₅₀	0.03 μM Compound: 19a	Antiproliferative activity was determined for 50% growth inhibition against human melanoma UACC-62 cell line Antiproliferative activity was determined for 50% growth inhibition against human melanoma UACC-62 cell line	[PMID: 11020283]
UACC-62	GI₅₀	0.03 μM Compound: 5	Growth inhibitory activity against human melanoma UACC-62 cell line Growth inhibitory activity against human melanoma UACC-62 cell line	[PMID: 15509164]

In Vitro

The GI₅₀ value of LMP744 (MJ-III-65) for NCI60 cells is 0.1 μM^[2].
LMP744 (0.1-5 μM, 3 days) induces dose-dependent accumulation of cells in the S and G₂ phases of the cell cycle^[2].

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

Cell Cytotoxicity Assay^[2]

Cell Line:

P388 and P388 Top1-deficient murine leukemia cells.
Concentration:

0.1-100 μM
Incubation Time:

3 days
Result:

Induced dose-dependent accumulation of cells in the S and G₂ phases of the cell cycle.

In Vivo

LMP744 (MJ-III-65) (10-50 mg/kg) administered i.v. push once a week for 4 weeks in nude mice moderately actives against human A253 and FaDu tumor xenografts without significant toxicity^[1].

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

Animal Model:

Athymic nude mice (nu/nu, female, 20-25 g, 8-12 weeks old) transplanted with A253 and FaDu human head and neck xenografts^[1].
Dosage:

10, 25, or 50 mg/kg/week, 4 weeks
Administration:

I.V. push via tail vein
Result:

Moderately actived against human A253 and FaDu tumor xenografts without significant toxicity.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 308246-57-3
Appearance Solid
Molecular Weight 488.92
Formel C₂₄H₂₅ClN₂O₇
Color Light brown to brown
SMILES

OCCNCCCN1C2=C(C(C3=CC(OCO4)=C4C=C23)=O)C5=CC(OC)=C(OC)C=C5C1=O.Cl
Synonyms

MJ-III65 hydrochloride; NSC706744 hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 105 mg/mL (214.76 mM; Need ultrasonic; 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

2.0453 mL

10.2266 mL

20.4532 mL

5 mM

0.4091 mL

2.0453 mL

4.0906 mL

10 mM

0.2045 mL

1.0227 mL

2.0453 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 (sealed storage, away from moisture). 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 (274 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]. Antony S, et al. Cellular topoisomerase I inhibition and antiproliferative activity by MJ-III-65 (NSC 706744), an indenoisoquinoline topoisomerase I poison. Mol Pharmacol. 2005 Feb;67(2):523-30. [Content Brief]

[2]. Antony S, et al. Bisindenoisoquinoline bis-1,3-{( 5,6-dihydro-5,11-diketo-11H-indeno [1,2-c]isoquinoline)-6-propylamino}propane bis(trifluoroacetate) (NSC 727357), a DNA intercalator and topoisomerase inhibitor with antitumor activity. Mol Pharmacol. 2006 [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0453 mL	10.2266 mL	20.4532 mL	51.1331 mL
	5 mM	0.4091 mL	2.0453 mL	4.0906 mL	10.2266 mL
	10 mM	0.2045 mL	1.0227 mL	2.0453 mL	5.1133 mL
	15 mM	0.1364 mL	0.6818 mL	1.3635 mL	3.4089 mL
	20 mM	0.1023 mL	0.5113 mL	1.0227 mL	2.5567 mL
	25 mM	0.0818 mL	0.4091 mL	0.8181 mL	2.0453 mL
	30 mM	0.0682 mL	0.3409 mL	0.6818 mL	1.7044 mL
	40 mM	0.0511 mL	0.2557 mL	0.5113 mL	1.2783 mL
	50 mM	0.0409 mL	0.2045 mL	0.4091 mL	1.0227 mL
	60 mM	0.0341 mL	0.1704 mL	0.3409 mL	0.8522 mL
	80 mM	0.0256 mL	0.1278 mL	0.2557 mL	0.6392 mL
	100 mM	0.0205 mL	0.1023 mL	0.2045 mL	0.5113 mL

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LMP744 hydrochloride

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Alle Topoisomerase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LMP744 hydrochloride

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Alle Topoisomerase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LMP744 hydrochloride Related Classifications

HY-U00248A Related Classifications