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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Beta-Lapachone Chemical Structure

Beta-Lapachone Chemical Structure
Molecular Weight: 242.27

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description Beta-Lapachone is a selective DNA topoisomerase I inhibitor, exhibiting no inhibitory activities against DNA topoisomerase II or ligase. Phase 2.
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
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.
Dosages 25–50 mg/kg
Administration Intraperitoneal administration
1

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

Download Beta-Lapachone SDF
Molecular Weight (MW) 242.27
Formula

C15H14O3

CAS No. 4707-32-8
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms β-Lapachone, ARQ-501
Solubility (25°C) * In vitro DMSO 48 mg/mL (198 mM)
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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