Voreloxin is an anticancer quinolone derivative that intercalates DNA and inhibits topoisomerase II, causing double-strand breaks in DNA, irreversible G2 arrest, and rapid onset of apoptosis.Vosaroxin has shown efficacy as a novel cytotoxic agent, and despite a similar mechanism of action has significant advantages over anthracyclines. It evades common resistance pathways of p53 and P-glycoprotein (P- gp) and does not appear to generate significant reactive oxygen species (ROS) associated with these agents.
|Cell lines||P388 leukemia cells|
|Preparation method||Putting cells into wells of a 96-well microtiter plate in the amount of 0.1 mL/well, preincubating for 24 h except for P388 cells, and incubating with various concentrations of a test compound in the 5% CO2 incubator at 37 °Cfor 72 h. After the culturing, 0.02 mL of a MTT solution (5 mg/mL) is put in each well, and culturing the cells for a further 4 h. The medium is removed by suction, and 0.2 mL of DMSO is put in each well to dissolve the formed formazan. Measureing the absorbance by Multiskan Bichromatic. Defining the IC50 as the drug concentration needed to produce a 50% reduction of absorbance relative to the control.|
|Incubation time||72 hours|
|Animal models||Mice implanted with P388 leukemia cells.|
|Formulation||Suspended in 0.4% CMC (carboxymethyl cellulose)|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Vosaroxin: a new valuable tool with the potential to replace anthracyclines in the treatment of AML?
Freeman C, et al. Expert Opin Pharmacother. 2013 Jul;14(10):1417-27. PMID: 23688047.
Vosaroxin : a novel antineoplastic quinolone.
Abbas JA, et al. Expert Opin Investig Drugs. 2012 Aug;21(8):1223-33. PMID: 22724917.
Phase II multicenter trial of voreloxin as second-line therapy in chemotherapy-sensitive or refractory small cell lung cancer.
Krug LM, et al. J Thorac Oncol. 2011 Feb;6(2):384-6. PMID: 21252718.
|Related Topoisomerase Products|
Exatecan Mesylate is a water soluble topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL).
Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor.
Pixantrone dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
10-Hydroxycamptothecin is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones.
7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition.
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