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LMP744 HCl (Mj-III65, NSC706744; Mj-III-65, NSC-706744), the hydrochloride salt of LMP744, is a DNA intercalator and Topoisomerase I (Top1) inhibitor with anticancer activity. LMP744 produces persistent topoisomerase I cleavage complexes and can overcome multidrug resistance. Consistent with Top1 poisoning, protein-linked DNA breaks were detected in cells treated with LMP744 at nanomolar concentrations. Studies in human cells in culture found LMP744 to be cytotoxic. Furthermore, limited cross-resistance was observed in camptothecin-resistant cell lines. LMP744 also exhibits antitumor activity in mouse tumor xenografts.
ln Vitro |
LMP744 (MJ-III-65) has a GI50 value of 0.1 μM for NCI60 cells[2]. In the S and G2 phases of the cell cycle, dose-dependent cell accumulation is induced by LMP744 (0.1–5 μM, 3 days) [2].
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ln Vivo |
When given as a weekly intravenous bolus for four weeks in nude mice, LMP744 (MJ-III-65) (10-50 mg/kg) exhibits moderate effectiveness against human A253 and FaDu tumor xenografts with no obvious harm [1].
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Cell Assay |
Cytotoxicity assay[2]
Cell Types: P388 and P388 Top1-deficient mouse leukemia cells. Tested Concentrations: 0.1-100 μM Incubation Duration: 3 days Experimental Results: Induces dose-dependent accumulation of cells in S and G2 phases of the cell cycle. |
Animal Protocol |
Animal/Disease Models: Athymic nude mice (nu/nu, female, 20-25 g, 8-12 weeks old) were transplanted with A253 and FaDu human head and neck xenografts [1].
Doses: 10, 25, or 50 mg/kg/week, 4 weeks Route of Administration: intravenous (iv) (iv)bolus injection via tail vein Experimental Results: Moderate activity against human A253 and FaDu tumor xenografts with no significant toxicity. |
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 |
Molecular Formula |
C24H25CLN2O7
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Molecular Weight |
488.92
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Exact Mass |
488.135
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CAS # |
308246-57-3
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Related CAS # |
LMP744;308246-52-8
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C1N(CCCNCCO)C2=C(C(C3=C2C=C(OCO4)C4=C3)=O)C5=C1C=C(OC)C(OC)=C5.[H]Cl
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InChi Key |
POXWLZDVWCKKEX-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C24H24N2O7.ClH/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,3-7,12H2,1-2H31H
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Chemical Name |
6-(3-((2-hydroxyethyl)amino)propyl)-2,3-dimethoxy-5H-[1,3]dioxolo[4',5'
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Synonyms |
Mj-III65, NSC706744Mj-III-65, NSC-706744 LMP744 HCl LMP 744 HCl
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~105 mg/mL (~214.76 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 | 2.0453 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 |
*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.