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 Experiment | |
|---|---|
| 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. |
| Concentrations | ~10 μg/mL |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | Mice implanted with P388 leukemia cells. |
| Formulation | Suspended in 0.4% CMC (carboxymethyl cellulose) |
| Dosages | ~50 mg/kg |
| Administration | i.p. |
| Molecular Weight | 401.44 |
| Formula | C18H19N5O4S |
| CAS Number | 175414-77-4 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
[2] Abbas JA, et al. Expert Opin Investig Drugs. Vosaroxin : a novel antineoplastic quinolone.
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