LMP744 hydrochloride
Based on 1 Customer Validation
LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
For research use only. We do not sell to patients.
- Purity: 99.08%
- CAS No.: 308246-57-3
- Formula: C24H25ClN2O7
- Molecular Weight:488.92
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
All Topoisomerase Isoforms
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Biological Activity
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Top1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DU-145 | GI50 |
<0.01 μM
Compound: 19a
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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
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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
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[PMID: 11020283] |
| HCT-116 | GI50 |
0.1 μM
Compound: 5
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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
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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
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[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
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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
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[PMID: 11020283] |
| MDA-MB-435 | GI50 |
0.79 μM
Compound: 5
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Growth inhibitory activity against human breast MDA-MB-435 cell line
Growth inhibitory activity against human breast MDA-MB-435 cell line
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[PMID: 15509164] |
| OVCAR-3 | GI50 |
0.35 μM
Compound: 19a
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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
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[PMID: 11020283] |
| OVCAR-3 | GI50 |
0.35 μM
Compound: 5
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Growth inhibitory activity against human ovarian OVCAR-3 cell line
Growth inhibitory activity against human ovarian OVCAR-3 cell line
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[PMID: 15509164] |
| SF-539 | GI50 |
0.04 μM
Compound: 19a
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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
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[PMID: 11020283] |
| SN12C | GI50 |
<0.01 μM
Compound: 19a
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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
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[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
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[PMID: 15509164] |
| UACC-62 | GI50 |
0.03 μM
Compound: 19a
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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
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[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] |
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.
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Cell Line:P388 and P388 Top1-deficient murine leukemia cells.
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Concentration:0.1-100 μM
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Incubation Time:3 days
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Result:Induced dose-dependent accumulation of cells in the S and G2 phases of the cell cycle.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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].
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Dosage:10, 25, or 50 mg/kg/week, 4 weeks
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Administration:I.V. push via tail vein
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Result:Moderately actived against human A253 and FaDu tumor xenografts without significant toxicity.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 308246-57-3
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Appearance Solid
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Molecular Weight 488.92
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Formula C24H25ClN2O7
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Color Light brown to brown
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SMILES
OCCNCCCN1C2=C(C(C3=CC(OCO4)=C4C=C23)=O)C5=CC(OC)=C(OC)C=C5C1=O.Cl
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Synonyms
MJ-III65 hydrochloride; NSC706744 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (274 KB)
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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)
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Handling Instructions (2659 KB)
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. [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]
Complete Stock Solution Preparation Table
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.
| 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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