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: 88495-63-0

Selleck's Artesunate has been cited by 15 publications

Purity & Quality Control

Batch: Purity: 99.56%
99.56

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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 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 lnformation & 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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