[CAS NO. 308246-57-3] LMP744 hydrochloride
PRODUCTS SPECIFICATIONS [308246-57-3]
DESCRIPTION [308246-57-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 488.92 |
| Molecular Formula | C24H25ClN2O7 |
| SMILES | OCCNCCCN1C2=C(C(C3=CC(OCO4)=C4C=C23)=O)C5=CC(OC)=C(OC)C=C5C1=O.Cl |
Summary
LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity [1] .
IC50 & Target
|
Top1 |
In Vitro
The GI
50
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 G
2
phases of the cell cycle
[2]
.
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 G 2 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] .
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 |
|---|---|---|---|---|
| NCT03030417 | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
Solid Tumors|Lymphoma
|
February 27, 2017 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 105 mg/mL ( 214.76 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 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 |
References
- [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.
- [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