Nedaplatin

Catalog No.S1826 Batch:S182604

Technical Data

Formula	C₂H₈N₂O₃Pt
Molecular Weight	303.17	CAS No.	95734-82-0
Solubility (25°C)*	In vitro	Water	30 mg/mL (98.95 mM)
		Ethanol	Insoluble

* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Nedaplatin(NSC 375101D) is a derivative of cisplatin and DNA damage agent for tumor colony forming units with IC50 of 94 μM.DMSO is not recommended to dissolve platinum-based drugs, which can easily lead to drug inactivation.

Targets

DNA synthesis ^[1]

In vitro

Nedaplatin (Aqupla) is a derivative of cisplatin for inhibition of tumor colony forming units with IC50 of 28.5 μg/mL. ^[1] Nedaplatin is a platinum compound which is used for cancer chemotherapy. ^[2] Nedaplatin inhibits the proliferation of SBC-3 cells by 98%, 93%, 75%, 54%, 27%, 6%, and 2% at a concentration of 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, respectively. The IC50 value of Nedaplatin for growth inhibition of SBC-3 cells is 0.053 μg/mL. ^[3]

In vivo

The sequential administration of 5-FU prior to nedaplatin or CDDP (FN or FC therapy) results in synergistically enhanced inhibition of tumour growth and prolonged survival in comparison with nedaplatin, CDDP or 5-FU monotherapy. ^[4] Combined dosing of Nedaplatin with gemcitabine results in synergistically enhanced inhibition of tumor growth in the Ma44 tumor model. Nedaplatin plus Gemcitabine is also effective against Ma44 cells when given late in the therapy, a model for advanced disease. Potent augmentation of growth inhibition by Nedaplatin with Gemcitabine is also found with the NCI-H460 tumor model. ^[5]

Features

This product is not recommended to be dissolved in dimethylsulfoxide (DMSO).^[6]

Protocol (from reference)

Cell Assay:^{^[3]}	Cell lines Human SCLC cell line SBC-3 and human NSCLC cell line PC-14 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 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, cells are exposed to drugs alone or in combination for 6 days at 37°C in an atmosphere of 100% humidity with 5% CO₂; the cells are then pipetted 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%. The IC50 is defined as the drug concentration required for a 50% reduction in the number of cells. Four or five independent experiments are carried out for each. To check the effect of the drug treatment schedule on the effect of the combination, the cells are treated 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. For the sequential exposure treatment, cells are exposed to the first drug for 3 hours, ished in fresh medium once, and then immediately exposed to the second drug for 3 hours. The treated cells are cultured in drug-free medium until evaluation.
Animal Study:^{^[5]}	Animal Models Tumor-bearing athymic BALB/c nude mice with Ma44 or NCI-H460 cells Dosages 10 mg/kg or 20 mg/kg Administration Administered via i.v.

Cell Assay:^{^[3]}

Cell lines
Human SCLC cell line SBC-3 and human NSCLC cell line PC-14
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
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, cells are exposed to drugs alone or in combination for 6 days at 37°C in an atmosphere of 100% humidity with 5% CO₂; the cells are then pipetted 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%. The IC50 is defined as the drug concentration required for a 50% reduction in the number of cells. Four or five independent experiments are carried out for each. To check the effect of the drug treatment schedule on the effect of the combination, the cells are treated 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. For the sequential exposure treatment, cells are exposed to the first drug for 3 hours, ished in fresh medium once, and then immediately exposed to the second drug for 3 hours. The treated cells are cultured in drug-free medium until evaluation.

Animal Study:^{^[5]}

Animal Models
Tumor-bearing athymic BALB/c nude mice with Ma44 or NCI-H460 cells
Dosages
10 mg/kg or 20 mg/kg
Administration
Administered via i.v.

References

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Selleck's Nedaplatin has been cited by 3 publications

Selective small molecule PARG inhibitor causes replication fork stalling and cancer cell death. [ Nat Commun, 2019, 10(1):5654]	PubMed: 31827085
Tailoring Chemotherapy for the African-Centric S47 Variant of TP53. [ Cancer Res, 2018, 78(19):5694-5705]	PubMed: 30115697
Nedaplatin enhanced apoptotic effects of ABT-737 in human cancer cells via Mcl-1 inhibition [Zhang C Oncol Lett, 2016, 12(5):4195-4202]	PubMed: 27895791

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SHIPPING AND STORAGE
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