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Purity: ≥98%
LMP744 (Mj-III-65, NSC-706744) is a novel and potent DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity. LMP744 can overcome multidrug resistance and forms persistent topoisomerase I cleavage complexes. Protein-linked DNA breaks were found in cells treated with nanomolar concentrations of LMP744, which is consistent with Top1 poisoning. LMP744 was found to be cytotoxic in studies conducted on human cells cultured. Additionally, camptothecin-resistant cell lines showed some degree of cross-resistance. Moreover, LMP744 has antitumor activity in tumor xenografts from mice.
| Targets |
Top1
|
|---|---|
| ln Vitro |
LMP744 (MJ-III-65) has a GI50 value of 0.1 μM for NCI60 cells[2].
LMP744 (0.1–5 μM, 3 days) causes a dose-dependent accumulation of cells in the S and G2 phases of the cell cycle[2]. |
| ln Vivo |
LMP744 (MJ-III65) (10-50 mg/kg) moderately active against human A253 and FaDu tumor xenografts without significant toxicity when given intraperitoneally (i.v.) once a week for four weeks in nude mice[1].
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| Cell Assay |
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. |
| Animal Protocol |
Athymic nude mice (nu/nu, female, 20-25 g, 8-12 weeks old) transplanted with A253 and FaDu human head and neck xenografts[1].
10, 25, or 50 mg/kg/week, 4 weeks I.V. push via tail vein |
| References |
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| Additional Infomation |
Topoisomerase-1 Inhibitor LMP744 is an indenoisoquinoline derivative and topoisomerase 1 (Top1) inhibitor, with potential antineoplastic activity. Upon administration, LMP744 binds to and stabilizes cleaved DNA-Top1 complexes, which prevents DNA re-ligation, induces stable, irreversible DNA strand breaks, prevents DNA repair, and leads to cell cycle arrest and apoptosis. As tumor cells proliferate at a much higher rate than normal cells, LMP744 specifically targets cancer cells. Top1, a DNA modifying enzyme essential for transcription, replication, and repair of double-strand DNA breaks, is overexpressed in tumor cells.
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| Molecular Formula |
C24H24N2O7
|
|---|---|
| Molecular Weight |
452.45656
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| Exact Mass |
452.158
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| Elemental Analysis |
C, 63.71; H, 5.35; N, 6.19; O, 24.75
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| CAS # |
308246-52-8
|
| Related CAS # |
LMP744 hydrochloride;308246-57-3
|
| PubChem CID |
397888
|
| Appearance |
Brown to dark brown solid powder
|
| LogP |
2.321
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
33
|
| Complexity |
802
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
OCCNCCCN1C2=C(C(C3=CC(OCO4)=C4C=C23)=O)C5=CC(OC)=C(OC)C=C5C1=O
|
| InChi Key |
QCSDJDQOJBQTDV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H24N2O7/c1-30-17-8-13-16(11-18(17)31-2)24(29)26(6-3-4-25-5-7-27)22-14-9-19-20(33-12-32-19)10-15(14)23(28)21(13)22/h8-11,25,27H,3-7,12H2,1-2H3
|
| Chemical Name |
20-[3-(2-hydroxyethylamino)propyl]-15,16-dimethoxy-5,7-dioxa-20-azapentacyclo[10.8.0.02,10.04,8.013,18]icosa-1(12),2,4(8),9,13,15,17-heptaene-11,19-dione
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| Synonyms |
LMP744; LMP-744; LMP 744; Mj-III-65; MJ-III65; MJ-III 65; NSC 706744; NSC-706744; NSC-706744
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ≥ 4.17 mg/mL (~9.2 mM）
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2101 mL | 11.0507 mL | 22.1014 mL | |
| 5 mM | 0.4420 mL | 2.2101 mL | 4.4203 mL | |
| 10 mM | 0.2210 mL | 1.1051 mL | 2.2101 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03030417 | Completed | Drug: LMP744 | Solid Tumors Lymphoma |
National Cancer Institute (NCI) |
February 27, 2017 | Phase 1 |
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