Artesunate (WR-256283)

Catalog No.S2265

For research use only.

Artesunate (WR-256283) is a part of the artemisinin group of agents with an IC50 of < 5 μM for small cell lung carcinoma cell line H69. It is a potential inhibitor of STAT-3 and exhibits selective cytotoxicity of cancer cells over normal cells in vitro; A potent inhibitor of EXP1.

Artesunate (WR-256283) Chemical Structure

CAS No. 88495-63-0

Selleck's Artesunate (WR-256283) has been cited by 10 Publications

Purity & Quality Control

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Biological Activity

Description Artesunate (WR-256283) is a part of the artemisinin group of agents with an IC50 of < 5 μM for small cell lung carcinoma cell line H69. It is a potential inhibitor of STAT-3 and exhibits selective cytotoxicity of cancer cells over normal cells in vitro; A potent inhibitor of EXP1.
Targets
EXP1(a membrane glutathione S-transferase) [4] STAT3 [7]
In vitro

ART could alter the biomechanical properties of the glioma cells to inhibit cell proliferation, migration and invasion [2]. The ART significantly suppresses the cell proliferation, induces the apoptosis and promoted cell cycle arrest at G0/G1 phase in SKM-1 cells. The mechanisms of ART anti-MDS is associated with the increase of intracellular calciumion concentration and ROS levels. In addition, the pro-apoptotic activity of ART may be involved in the regulation of BCL-2 /BAX ratio and the expressions of P-bad and survivin[3]. ART treatment demethylates CDH1, which, in turn recovers the E-cadherin activation in SKM-1 cells[1].

In vivo Artesunate is a medication used to treat malaria. Artesunate can induce radiosensitivity of HeLa cells in vivo using Xenograft model of nude mice[5]. Artesunate had a relatively high immunosuppressive activity with low toxicity, and could inhibit T lymphocyte proliferation induced by mitogen and alloantigen[6].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: SKM-1 cells
  • Concentrations: 0, 12.5, 25, 50 µg/mL
  • Incubation Time: 0, 24, 48, and 72 h
  • Method:

    Growth inhibition assay: The SKM-1 cells (1×105/mL) are firstly seeded in 96-well plates. Artesunate is diluted in 0.1% dimethyl sulfoxide (DMSO) producing 0, 12.5, 25, 50µg/mL concentrations and added to the SKM-1 cells with 100 µl per well. A negative control is treated with 0.1% DMSO. At 0, 24, 48, and 72 hours, same amount of MTT solution is added into each well and cultured for extra 4 hours. MTT treated cells are fixed with 150 µL DMSO for 30 min at room temperature and then determined with Evolution 201 and 220 UV-Vis spectrophotometer system at 540 nm.

  • (Only for Reference)
Animal Research:

[5]

  • Animal Models: BALB/c mice
  • Dosages: 100 mg/kg/day 
  • Administration: i.p.
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 77 mg/mL
(200.3 mM)
Ethanol 77 mg/mL
(200.3 mM)
Water 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.

Chemical Information

Molecular Weight 384.42
Formula

C19H28O8

CAS No. 88495-63-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CCC2C(C(OC3C24C1CCC(O3)(OO4)C)OC(=O)CCC(=O)O)C

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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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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04921930 Not yet recruiting Drug: Artesunate Oral Product Friedreich Ataxia Institut National de la Santé Et de la Recherche Médicale France|Imagine Institute July 1 2021 Phase 1|Phase 2
NCT03893097 Completed Drug: Praziquantel|Drug: Artesunate + Mefloquine Schistosoma Haematobium|Schistosoma Mansoni Institute of Tropical Medicine Belgium|Institut de Recherche en Santé de Surveillance Épidémiologique et de Formation (IRESSEF) October 14 2019 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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