Antibodies
Beta-Lapachone
- 貨號 Cat. No.
- S7261
- 規格 Size
- 10mgã€50mg
- 品牌 Brand
- Selleckchem
Description
Beta-Lapachone
Catalog No.S7261
Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2. | |||||
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| Targets | DNA topoisomerase I | IDO1 | ||||
| IC50 | 0.44 μM [4] | |||||
| In vitro | Beta-Lapachone inhibits DNA relaxation induced by DNA topoisomerase I in a dose-dependent manner. [1]Treatment of beta-lapachone (100 nM or greater) results in >95% inhibition of Topo I DNA unwinding activity compared to the DMSO control. beta-lapachone (1-5 μM) causes a block in G0/G1 of the cell cycle and induces apoptosis by locking Topo I onto DNA and blocking replication fork movement in HL-60 and three human prostate cancer (DU-145, PC-3, and LNCaP) cells. [2] Beta-Lapachone facilitates the migration of mouse 3T3 fibroblasts and human endothelial EAhy926 cells through different MAPK signaling pathways, and thus accelerates scrape-wound healing in vitro. [3] In addition, beta-Lapachone inhibits purified recombinant IDO1 activity through uncompetitive inhibition with IC50 of 0.44 μM, and beta-lapachone also exhibits superior retention of intracellular IDO1 inhibitory activity with an IC50 of 1.0 μM, partially dependent on biotransformation by NQO1. [4] Beta-lapachone induces programmed necrosis of NQO1+ cancer cells by NQO1-dependent reactive oxygen species (ROS) formation and PARP1 hyperactivation. [5] | |||||
| In vivo | Beta-lapachone treatment (50 mg/kg) leads to potent inhibition of in vivo tumor growth in a xenograft mouse model of human ovarian cancer, and the combination of beta-lapachone and taxol produces a synergistic induction of apoptosis. [6] In normal and diabetic (db/db) mice, treatment of beta-lapachone results in a faster healing process than vehicle only. [3] | |||||
| Features | ||||||
Protocol(Only for Reference)
Cell Assay: [2]
| Cell lines | HL-60, PC-3, DU145, and LNCaP cells |
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| Concentrations | 0.005 to 50 μM |
| Incubation Time | 12 hours |
| Method | IC50 calculations for each cell line are determined by DNA amount (IS) and anchorage-dependent colony formation (CF) assays. For the CF assay, cells are seeded at 500 viable cells/well in 6-well plates and incubated overnight, then treated with equal volumes of media containing beta-lapachone at final concentrations ranging from 0.005 to 50 μM in half-log increments (controls were treated with 0.25% DMSO, equivalent to the highest dose of beta-lapachonc used) for 4 hour or for continuous 12-hour exposures. Plates (3 wells/condition) are stained with crystal violet, and colonies of >50 normal-appearing cells are enumerated. IC50 values for various cells are calculated using drug doses with numbers of colonies surrounding 50% of control. For DNA assays, plates are harvested for IC50 determinations 8 days after treatment using a CytoFluor 2350 fluorescence measurement system. Six-well samplings are included in the calculation of DNA fluor units for each dose. A graph of beta-lapachone dose versus percentage control DNA in fluor units is used to calculate each IC50. All experiments are repeated at least twice, each in duplicate. |
Animal Study: [6]
| Animal Models | Human ovarian cancer cells (36M2) are established in nude mice. |
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| Dosages | 25–50 mg/kg |
| Administration | Intraperitoneal administration |
References
Clinical Trial Information( data from http://clinicaltrials.gov)
| NCT Number | Recruitment | Conditions | Sponsor /Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00622063 | Completed | Cancer | ArQule | 2006-12 | Phase 1|Phase 2 |
| NCT00524524 | Completed | Advanced Solid Tumors | ArQule | 2007-08 | Phase 1 |
| NCT01285388 | Completed | Metabolic Syndrome|Obesity | KT&G Life Sciences Corp|KT&G Corporation | 2010-07 | Phase 1 |
| NCT01444677 | Completed | Metabolic Syndrome|Obesity | KT&G Life Sciences Corp|KT&G Corporation | 2011-08 | Phase 1 |
| NCT01502800 | Recruiting | Solid Tumors | University of Texas Southwestern Medical Center|ArQule | 2011-12 | Phase 1 |
Chemical Information
| Molecular Weight (MW) | 242.27 |
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| Formula | C15H14O3 |
| CAS No. | 4707-32-8 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | β-Lapachone, ARQ-501 |
| Solubility (25°C) * | In vitro | DMSO | 48 mg/mL (198 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 10 mg/mL (41 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | 2H-Naphtho[1,2-b]pyran-5,6-dione, 3,4-dihydro-2,2-dimethyl- |
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