Nedaplatin DNA/RNA Synthesis inhibitor

Cat.No.S1826

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  DNA/RNA Synthesis inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 303.17

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 303.17 Formula

C2H8N2O3Pt

Storage (From the date of receipt) 2 years 4°C(in the dark) powder
CAS No. 95734-82-0 -- Storage of Stock Solutions

Synonyms NSC 375101D Smiles C(C(=O)O)O.N.N.[Pt]

Solubility

In vitro
Batch:

Water : 30 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features
This product is not recommended to be dissolved in dimethylsulfoxide (DMSO).[6]
Targets/IC50/Ki
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] This compound is a platinum compound which is used for cancer chemotherapy. [2] It 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 this chemical 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 this compound, CDDP or 5-FU monotherapy. [4] Combined dosing of this compound with gemcitabine results in synergistically enhanced inhibition of tumor growth in the Ma44 tumor model. This chemical 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 this compound with Gemcitabine is also found with the NCI-H460 tumor model. [5]

References
  • https://pubmed.ncbi.nlm.nih.gov/9893671/
  • https://pubmed.ncbi.nlm.nih.gov/11173544/
  • https://pubmed.ncbi.nlm.nih.gov/24812268/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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