Home JAK/STAT ADC Cytotoxin inhibitor - STAT inhibitor Artesunate For research use only.

Artesunate

Synonyms: WR-256283

Artesunate 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 Chemical Structure

Artesunate Chemical Structure

CAS No. 88495-63-0

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Biological Activity

Description Artesunate 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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models BALB/c mice
Dosages 100 mg/kg/day 
Administration i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05929157 Not yet recruiting
Severe Malarial Treatment
Centre de Recherche Médicale de Lambaréné|Institute of Tropical Medicine University of Tuebingen
 September 1 2023 Phase 1|Phase 2
NCT05555862 Active not recruiting
Anal High Grade Squamous Intraepithelial Lesion|Anal Precancerous Condition|AIN 2/3|HPV Infection|Anal Dysplasia|HPV Disease
Frantz Viral Therapeutics LLC|Amarex CRO|University of California San Francisco|Anal Dysplasia Clinic MidWest|Laser Surgery Care
 February 10 2023 Phase 2
NCT04921930 Recruiting
Friedreich Ataxia
Institut National de la Santé Et de la Recherche Médicale France|Imagine Institute
 May 6 2022 Phase 1|Phase 2
NCT05343312 Active not recruiting
Malaria
Centro de Investigacao em Saude de Manhica|United States Agency for International Development (USAID)
 March 16 2022 Phase 4

Chemical Information & Solubility

Molecular Weight 384.42 Formula

C19H28O8
CAS No. 88495-63-0 SDF Download Artesunate SDF
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 77 mg/mL ( (200.3 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 77 mg/mL

Water : Insoluble


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In vivo
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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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