Nedaplatin (NSC 375101D)

Alias: NSC 375101D; NSC-375101D; NSC 37510D; NSC-375101 D; NSC 375101-D
Cat No.:V1471 Purity: ≥98%
Nedaplatin (formerly NSC-375101D; NSC 37510D;NSC-375101 D;NSC 375101-D; trade name Aqupla) is a cisplatin analog and DNA damaging agent approved as an anticancer medication.
Nedaplatin (NSC 375101D) Chemical Structure CAS No.: 95734-82-0
Product category: DNA(RNA) Synthesis
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Nedaplatin (formerly NSC-375101D; NSC 37510D; NSC-375101 D; NSC 375101-D; trade name Aqupla) is a cisplatin analog and DNA damaging agent approved as an anticancer medication. At 94 μM, it inhibits the formation of tumor colonies. Nedaplatin is a platinum compound used in cancer chemotherapy; however, compared to other drugs containing platinum, it has fewer side effects, including nephrotoxicity, nausea, and vomiting.

Biological Activity I Assay Protocols (From Reference)
Targets
DNA synthesis
ln Vitro

Nedaplatin (Aqupla) is a cisplatin derivative that inhibits tumor colony forming units, with an IC50 value of 28.5 μg/mL. [1] A platinum compound called nedaplatin is used as a cancer chemotherapy drug. The proliferation of SBC-3 cells is inhibited by nedaplatin at concentrations 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. Nedaplatin's IC50 value for suppressing SBC-3 cell growth is 0.053 μg/mL.[3]

ln Vivo
In comparison to nedaplatin, CDDP, or 5-FU monotherapy, the sequential administration of 5-FU before nedaplatin or CDDP (FN or FC therapy) results in synergistically enhanced inhibition of tumour growth and prolonged survival.[4] When Nedaplatin and Gemcitabine are administered together, the Ma44 tumor model exhibits a synergistically enhanced inhibition of tumor growth. When administered toward the end of the therapy, nedaplatin plus gemcitabine is also effective against Ma44 cells, a model for advanced disease. The NCI-H460 tumor model also demonstrates a strong enhancement of growth inhibition by neoplatin when combined with gemcitabine.[5]
Cell Assay
An assay for regrowth is used to measure the antitumor activity of the drug treatments, which include the inhibition of cell proliferation (including that of human SCLC cell line SBC-3 and human NSCLC cell line PC-14). To put it briefly, cells are treated with drugs alone or in combination for six days at 37°C in a 100% humidity and 5% CO2 environment. After that, the cells are pipetted six to eight times, or nearly all of them become single cells, and they are counted using a counter. Plotting the percentage of surviving cells (the unaffected cell fraction, fu) against drug concentration yields concentration-effect curves for each drug. To calculate the treated:control cultures' cell proliferation ratio (T:C%), use the formula below: [(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 drug concentration needed to cause a 50% decrease in the number of cells is known as the IC50. For each, four or five separate experiments are conducted. In order to assess the impact of the drug treatment schedule on the combination's effect, the cells are treated for three hours either sequentially—first with Nedaplatin and then with irinotecan (Nedaplatin→irinotecan) or simultaneously with both drugs. Cells are exposed to the first drug for three hours during the sequential exposure treatment, then they are immediately exposed to the second drug for three hours after being ished in fresh medium once. Up until assessment, the treated cells are cultivated in a drug-free medium.
Animal Protocol
Tumor-bearing athymic BALB/c nude mice with Ma44 or NCI-H460 cells
10 mg/kg or 20 mg/kg
Administered via i.v.
References

[1]. Cancer Chemother Pharmacol . 1997;39(6):493-7.

[2]. Dalton Trans . 2010 Sep 21;39(35):8113-27.

[3]. Clin Cancer Res . 2001 Jan;7(1):202-9.

[4]. Eur J Cancer . 1998 Oct;34(11):1796-801.

[5]. Jpn J Cancer Res . 2001 Jan;92(1):51-8.

[6]. Cancer Res . 2014 Jul 15;74(14):3913-22.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C2H8N2O3PT
Molecular Weight
303.17
Exact Mass
303.02
Elemental Analysis
C, 7.98; H, 2.01; N, 9.30; O, 15.94; Pt, 64.78
CAS #
95734-82-0
Appearance
Solid powder
SMILES
C(C(=O)O)O.N.N.[Pt]
InChi Key
ZAXCMPAWRCMABN-UHFFFAOYSA-N
InChi Code
InChI=1S/C2H4O3.2H3N.Pt/c3-1-2(4)5;;;/h3H,1H2,(H,4,5);2*1H3;
Chemical Name
azane;2-hydroxyacetic acid;platinum
Synonyms
NSC 375101D; NSC-375101D; NSC 37510D; NSC-375101 D; NSC 375101-D
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: <1 mg/mL
Water: ~18 mg/mL (~59.4 mM)
Ethanol: <1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.2985 mL 16.4924 mL 32.9848 mL
5 mM 0.6597 mL 3.2985 mL 6.5970 mL
10 mM 0.3298 mL 1.6492 mL 3.2985 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04212052 Active
Recruiting
Radiation: split-course
radiotherapy
Drug: concurrent chemotherapy
Non-small Cell Lung Cancer Sun Yat-sen University December 1, 2019 Phase 2
NCT02279134 Active
Recruiting
Drug: Cisplatin or Nedaplatin
Drug: Paclitaxel
Esophageal Cancer
Esophageal Neoplasms
Zefen Xiao October 2014 Phase 2
Phase 3
NCT04437329 Recruiting Drug: Nedaplatin
Drug: Cisplatin
Nasopharyngeal Carcinoma Affiliated Cancer Hospital &
Institute of Guangzhou Medical
University
August 1, 2020 Phase 3
NCT05039606 Not yet recruiting Drug: Nedaplatin
Drug: Cisplatin
Head and Neck Squamous Carcinoma Guiyang Medical University September 2021 Phase 2
NCT04844385 Recruiting Drug: Nedaplatin
Radiation: SMART
Esophageal Squamous Cell
Carcinoma
Sun Yat-sen University February 20, 2021 Phase 2
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