Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor Nedaplatin For research use only.

Nedaplatin

Synonyms: NSC 375101D

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.

Nedaplatin Chemical Structure

Nedaplatin Chemical Structure

CAS No. 95734-82-0

Purity & Quality Control

Nedaplatin Related Products

Signaling Pathway

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis Signaling Pathway

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.
Features This product is not recommended to be dissolved in dimethylsulfoxide (DMSO).[6]
Targets
DNA synthesis [1]
In vitro
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]
Cell Research 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.
In Vivo
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]
Animal Research 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.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02964455 Completed
Esophageal Squamous Cell Carcinoma
Sun Yat-sen University
 November 2016 Phase 1
NCT01175460 Completed
Esophageal Cancer
Zhejiang Cancer Hospital
 January 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 303.17 Formula

C2H8N2O3Pt
CAS No. 95734-82-0 SDF --
Smiles C(C(=O)O)O.N.N.[Pt]
Storage (From the date of receipt) 2 years 4°C(in the dark) powder

In vitro
Batch:

Water : 30 mg/mL

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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