Nedaplatin is a platinum complex that has potent antineoplastic activity. Nedaplatin produces less nausea, vomiting and nephrotoxicity than other platinum-containing products.NDP was developed as a second generation platinum complex.Because it has greater antitumour activity and lower nephrotoxicity than cisplatin (CDDP).Nedaplatin (NDP) is a second-generation platinum complex with reduced nephrotoxicity that may substitute for CDDP or even surpass it for use in combination with other drugs.
Cell Experiment | |
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Cell lines | Human SCLC cell line SBC-3 and human NSCLC cell line PC-14 |
Preparation method | The inhibition of cell (including human SCLC cell line SBC-3 and human NSCLC cell line PC-14) proliferation after drug treatments as the antitumor activity using a regrowth assay is messured. Briefly, exposing cells to drugs alone or in combination for 6 days at 37°C in an atmosphere of 100% humidity with 5% CO2; then pipetting the cells six to eight times until almost all cells appeared as single cells and counted with a counter. For each drug, concentration-effect curves are drawn as plots of the fraction of surviving cells (unaffected cell fraction, fu) versus drug concentration. The cell proliferation ratio of the treated:control cultures (T:C%) is calculated as follows: [(the number of treated cells on day 6)/(the number of treated cells on day 0)]/[(the number of control cells on day 6)/(the number of control cells on day 0)] × 100%. Defining the IC50 as the drug concentration required for a 50% reduction in the number of cells.Carrying four or five independent experiments out for each. Treating the cells either by simultaneous exposure to the two drugs or by sequential exposure to Nedaplatin followed by irinotecan (Nedaplatin→irinotecan) and vice versa (irinotecan→Nedaplatin) for 3 hours to check the effect of the drug treatment schedule on the effect of the combination . For the sequential exposure treatment, exposing cells to the first drug for 3 hours, ished in fresh medium once, and then immediately exposing to the second drug for 3 hours. Culturing the treated cells in drug-free medium until evaluation |
Concentrations | 0.005 μg/mL, 0.01 μg/mL, 0.025 μg/mL, 0.05 μg/mL, 0.1 μg/mL, 0.25 μg/mL, and 0.5 μg/mL |
Incubation time | 6 days |
Animal Experiment | |
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Animal models | Tumor-bearing athymic BALB/c nude mice with Ma44 or NCI-H460 cells |
Formulation | Saline |
Dosages | 10 mg/kg or 20 mg/kg |
Administration | Administered via i.v. |
Molecular Weight | 303.17 |
Formula | C2H8N2O3Pt |
CAS Number | 95734-82-0 |
Form | Solid |
Solubility (25°C) | DMSO water 10mg/mL |
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.
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