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Catalog No.S2265 Synonyms: WR-256283

7 publications

Artesunate Chemical Structure

CAS No. 88495-63-0

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.

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Selleck's Artesunate has been cited by 7 publications

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Choose Selective ADC Cytotoxin Inhibitors

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.
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].


Cell Research:


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  • 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:


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  • 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


CAS No. 88495-63-0
Storage powder
in solvent
Synonyms WR-256283
Smiles CC1CCC2C(C(OC3C24C1CCC(O3)(OO4)C)OC(=O)CCC(=O)O)C

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03893097 Active not recruiting 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
NCT03792516 Recruiting Drug: artesunate ointment 40% Vulvar Dysplasia|HPV-Related Vulvar Intraepithelial Neoplasia|Preinvasive Vulvar Disease|Vulva Intraepithelial Neoplasia|Vulvar Diseases Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins|Frantz Viral Therapeutics LLC April 17 2019 Phase 1
NCT03093129 Recruiting Drug: artesunate|Other: placebo Colorectal Cancer The 108 Military Central Hospital|Institute of Tropical Medicine University of Tuebingen January 8 2018 Phase 2

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID