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Artesunate

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Artesunate is an inhibitor of both STAT-3 and exported protein 1 (EXP1).

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Pureté: 99.89%
CAS No.: 88495-63-0
Formule: C₁₉H₂₈O₈
Masse moléculaire:384.42

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Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Artesunate Chemical Structure

CAS No.: 88495-63-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (41)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
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Activité biologique

Description

Artesunate is an inhibitor of both STAT-3 and exported protein 1 (EXP1).

IC₅₀ & Target^[1]^[2]

Stat-3

EXP1

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Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	15.921 μM Compound: 1; ART	Antiproliferative activity against human A549 cells assessed as growth inhibition after 72 hrs by CCK-8 assay Antiproliferative activity against human A549 cells assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 26615886]
A549	IC₅₀	50.68 μM Compound: ATS	Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay Antiproliferative activity against human A549 cells measured after 48 hrs by MTT assay	[PMID: 30837097]
A549	IC₅₀	5.4 μM Compound: 3; ARS	Cytotoxicity against human A549 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability by MTT assay	[PMID: 33691167]
ADR5000 cell line	IC₅₀	1.2 μM Compound: 1	Cytotoxicity against human CEM/ADR5000 by XTT assay Cytotoxicity against human CEM/ADR5000 by XTT assay	[PMID: 20527917]
ADR5000 cell line	IC₅₀	1.2 μM Compound: 1	Cytotoxicity against human CEM/ADR5000 by CCK-8 assay Cytotoxicity against human CEM/ADR5000 by CCK-8 assay	[PMID: 22884578]
ADR5000 cell line	IC₅₀	1.2 μM Compound: 2	Cytotoxicity against human multidrug-resistant CEM/ADR5000 cells expressing p-glycoprotein by resazurin assay Cytotoxicity against human multidrug-resistant CEM/ADR5000 cells expressing p-glycoprotein by resazurin assay	[PMID: 24561670]
ADR5000 cell line	IC₅₀	0.19 μM Compound: 3	Cytotoxicity against human CEM/ADR5000 cells assessed as cell viability after 72 hrs by resazurin assay Cytotoxicity against human CEM/ADR5000 cells assessed as cell viability after 72 hrs by resazurin assay	[PMID: 26260339]
ADR5000 cell line	EC₅₀	0.5 μM Compound: Artesunic acid	Cytotoxicity against human CEM/ADR5000 cells assessed as reduction in cell growth Cytotoxicity against human CEM/ADR5000 cells assessed as reduction in cell growth	[PMID: 29656203]
ADR5000 cell line	EC₅₀	0.189 μM Compound: 3	Cytotoxicity against human CEM/ADR5000 cells over-expressing P-gp assessed as reduction in cell viability after 72 hrs by resazurin dye based assay Cytotoxicity against human CEM/ADR5000 cells over-expressing P-gp assessed as reduction in cell viability after 72 hrs by resazurin dye based assay	[PMID: 29887512]
ADR5000 cell line	EC₅₀	0.1 μM Compound: 2	Cytotoxicity against human CEM/ADR5000 cells overexpressing P-gp assessed as reduction in cell viability after 72 hrs by resazurin dye based assay Cytotoxicity against human CEM/ADR5000 cells overexpressing P-gp assessed as reduction in cell viability after 72 hrs by resazurin dye based assay	[PMID: 29937978]
BT-474	IC₅₀	7.8 μM Compound: Artesunate	Cytotoxicity against human BT474 cells after 48 hrs by MTT assay Cytotoxicity against human BT474 cells after 48 hrs by MTT assay	[PMID: 23790541]
C-33-A	EC₅₀	1.83 μM Compound: 7	Antiproliferative activity against human C33A cells after 72 hrs by MTT assay Antiproliferative activity against human C33A cells after 72 hrs by MTT assay	[PMID: 30429957]
CCRF-CEM	IC₅₀	1.8 μM Compound: 1	Cytotoxicity against human CCRF-CEM by XTT assay Cytotoxicity against human CCRF-CEM by XTT assay	[PMID: 20527917]
CCRF-CEM	IC₅₀	1.8 μM Compound: 1	Cytotoxicity against human CCRF-CEM cells by CCK-8 assay Cytotoxicity against human CCRF-CEM cells by CCK-8 assay	[PMID: 22884578]
CCRF-CEM	IC₅₀	1.8 μM Compound: 2	Cytotoxicity against human CCRF-CEM cells by resazurin assay Cytotoxicity against human CCRF-CEM cells by resazurin assay	[PMID: 24561670]
CCRF-CEM	IC₅₀	0.07 μM Compound: 3	Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 72 hrs by resazurin assay Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 72 hrs by resazurin assay	[PMID: 26260339]
CCRF-CEM	EC₅₀	0.069 μM Compound: 3	Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay	[PMID: 29887512]
CCRF-CEM	EC₅₀	0.4 μM Compound: 2	Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay Cytotoxicity against human CCRF-CEM cells assessed as reduction in cell viability after 72 hrs by resazurin dye based assay	[PMID: 29937978]
CHO	IC₅₀	>100 μM Compound: ARS	Cytotoxicity against CHO cells assessed as reduction in cell viability measured after 48 hrs by MTT assay Cytotoxicity against CHO cells assessed as reduction in cell viability measured after 48 hrs by MTT assay	[PMID: 27448920]
Erythrocyte	CC₅₀	>100 μg/mL Compound: Artesunate	Cytotoxicity against human erythrocytes Cytotoxicity against human erythrocytes	[PMID: 37556947]
HCT-116	IC₅₀	7.1 μM Compound: Artesunate	Antiproliferative activity against human HCT-116 cells assessed as growth after 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as growth after 48 hrs by MTT assay	[PMID: 27010926]
HCT-116	IC₅₀	0.89 μM Compound: AS	Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 48 hrs by MTS assay Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 48 hrs by MTS assay	[PMID: 31494469]
HCT-116	IC₅₀	7.1 μM Compound: Artesunate	Antiproliferative activity against human HCT-116 cells Antiproliferative activity against human HCT-116 cells	[PMID: 31945642]
HCT-116	IC₅₀	7.1 μM Compound: Artesunate	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability	[PMID: 31945642]
HCT-116	IC₅₀	0.46 μM Compound: ASU	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth by Cell-titer Glo luminescent assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth by Cell-titer Glo luminescent assay	[PMID: 38287228]
HEK293	IC₅₀	150 μM Compound: artesunate	Selectivity index, ratio of IC50 for human HEK293 cells to IC50 for chloroquine, pyrimethamine, and mefloquine-resistant Plasmodium falciparum Dd2 Selectivity index, ratio of IC50 for human HEK293 cells to IC50 for chloroquine, pyrimethamine, and mefloquine-resistant Plasmodium falciparum Dd2	[PMID: 21155593]
HEK293	IC₅₀	2.9 μM Compound: artesunate	Cytotoxicity against human HEK293 cells after 72 hrs by alamar blue assay Cytotoxicity against human HEK293 cells after 72 hrs by alamar blue assay	[PMID: 21155593]
HEK293	IC₅₀	10 μM Compound: Artesunate	Cytotoxicity against HEK293 cells assessed as cell growth inhibition after 72 hrs by Alamar blue assay Cytotoxicity against HEK293 cells assessed as cell growth inhibition after 72 hrs by Alamar blue assay	[PMID: 28774427]
HEK293	IC₅₀	7 μM Compound: Artesunate	Cytotoxicity against HEK293 cells after 72 hrs by resazurin dye based assay Cytotoxicity against HEK293 cells after 72 hrs by resazurin dye based assay	[PMID: 29236492]
HeLa	IC₅₀	3.2 μM Compound: Artesunate	Cytotoxicity against human HeLa cells incubated for 48 hrs by resazurin dye reduction assay Cytotoxicity against human HeLa cells incubated for 48 hrs by resazurin dye reduction assay	[PMID: 23013253]
HeLa	IC₅₀	19.014 μM Compound: 1; ART	Antiproliferative activity against human HeLa cells assessed as growth inhibition after 72 hrs by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 26615886]
HeLa	IC₅₀	7.1 μM Compound: Artesunate	Antiproliferative activity against human Hela cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human Hela cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 27010926]
HeLa	EC₅₀	12.03 μM Compound: 7	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay	[PMID: 30429957]
HeLa	IC₅₀	0.5 μM Compound: Artesunate	Cytotoxicity against human HeLa cells assessed as cell viability incubated for 48 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as cell viability incubated for 48 hrs by MTT assay	[PMID: 31945642]
HeLa	IC₅₀	11.3 μM Compound: Artesunate	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability Antiproliferative activity against human HeLa cells assessed as reduction in cell viability	[PMID: 31945642]
HeLa	IC₅₀	7.1 μM Compound: Artesunate	Antiproliferative activity against human HeLa cells Antiproliferative activity against human HeLa cells	[PMID: 31945642]
HepG2	IC₅₀	12.7 μM Compound: artesunate	Cytotoxicity against human HepG2 cells after 72 hrs by alamar blue assay Cytotoxicity against human HepG2 cells after 72 hrs by alamar blue assay	[PMID: 21155593]
HepG2	IC₅₀	374 μM Compound: artesunate	Selectivity index, ratio of IC50 for human HepG2 cells to IC50 for chloroquine, pyrimethamine, and mefloquine-resistant Plasmodium falciparum Dd2 Selectivity index, ratio of IC50 for human HepG2 cells to IC50 for chloroquine, pyrimethamine, and mefloquine-resistant Plasmodium falciparum Dd2	[PMID: 21155593]
HepG2	IC₅₀	20 μM Compound: ARS	Cytotoxicity against human HepG2 cells after 72 hrs by formazan test Cytotoxicity against human HepG2 cells after 72 hrs by formazan test	[PMID: 23685181]
HepG2	IC₅₀	<1 μM Compound: Artesunate	Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin	[PMID: 23927658]
HepG2	IC₅₀	22.24 μM Compound: 1; ART	Antiproliferative activity against human HepG2 cells assessed as growth inhibition after 72 hrs by CCK-8 assay Antiproliferative activity against human HepG2 cells assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 26615886]
HepG2	IC₅₀	6.5 μM Compound: ART	Dark toxicity against human HepG2 cells assessed as reduction in cell viability incubated overnight by MTT assay Dark toxicity against human HepG2 cells assessed as reduction in cell viability incubated overnight by MTT assay	[PMID: 28882481]
HepG2	IC₅₀	7.7 μM Compound: ART	Phototoxicity against human HepG2 cells assessed as reduction in cell viability preincubated overnight followed by irradiation with LED light at 1.7 J/cm'2 for 10 mins measured post overnight incubation by MTT assay Phototoxicity against human HepG2 cells assessed as reduction in cell viability preincubated overnight followed by irradiation with LED light at 1.7 J/cm'2 for 10 mins measured post overnight incubation by MTT assay	[PMID: 28882481]
HepG2	IC₅₀	39.93 μM Compound: ATS	Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay	[PMID: 30837097]
HepG2	IC₅₀	59.4 μM Compound: Artesunate	Antiproliferative activity against human HepG2 cells by MTT assay Antiproliferative activity against human HepG2 cells by MTT assay	[PMID: 31546197]
HepG2	IC₅₀	59.4 μM Compound: Artesunate	Antiproliferative activity against human HepG2 cells Antiproliferative activity against human HepG2 cells	[PMID: 31945642]
HepG2	IC₅₀	267 μM Compound: Artesunate	Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as cell viability after 72 hrs by MTT assay	[PMID: 33158577]
HepG2	IC₅₀	47 μM Compound: 3; ARS	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay	[PMID: 33691167]
HepG2 2.2.15	IC₅₀	2.3 μM Compound: 21	Antiviral activity against Hepatitis B virus infected in human HepG2.2.15 cells assessed as decrease in HBV surface antigen secretion after 21 days Antiviral activity against Hepatitis B virus infected in human HepG2.2.15 cells assessed as decrease in HBV surface antigen secretion after 21 days	[PMID: 24549242]
HL-60	IC₅₀	2 μM Compound: ASN	Cytotoxicity against human HL60 cells assessed as cell viability after 24 hrs by MTT assay Cytotoxicity against human HL60 cells assessed as cell viability after 24 hrs by MTT assay	[PMID: 24148834]
Huh-7	CC₅₀	>100 μg/mL Compound: AS	Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 36306538]
HUVEC	IC₅₀	1.092 μM Compound: 1; ART	Antiproliferative activity against HUVEC assessed as growth inhibition after 72 hrs by CCK-8 assay Antiproliferative activity against HUVEC assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 26615886]
HUVEC	IC₅₀	86.1 μM Compound: 3; ARS	Cytotoxicity against HUVEC assessed as reduction in cell viability by MTT assay Cytotoxicity against HUVEC assessed as reduction in cell viability by MTT assay	[PMID: 33691167]
J82	IC₅₀	75.7 μM Compound: 3; ARS	Cytotoxicity in human J82 cells assessed as reduction in cell viability by MTT assay Cytotoxicity in human J82 cells assessed as reduction in cell viability by MTT assay	[PMID: 33691167]
K562	IC₅₀	5.999 μM Compound: 1; ART	Antiproliferative activity against human K562 cells assessed as growth inhibition after 72 hrs by CCK-8 assay Antiproliferative activity against human K562 cells assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 26615886]
K562/Adr	IC₅₀	6.256 μM Compound: 1; ART	Antiproliferative activity against human K562/ADR cells assessed as growth inhibition after 72 hrs by CCK-8 assay Antiproliferative activity against human K562/ADR cells assessed as growth inhibition after 72 hrs by CCK-8 assay	[PMID: 26615886]
KB	IC₅₀	78.5 μM Compound: Artesunate	Antiproliferative activity against human KB cells by MTT assay Antiproliferative activity against human KB cells by MTT assay	[PMID: 31546197]
KB	IC₅₀	78.5 μM Compound: Artesunate	Antiproliferative activity against human KB cells Antiproliferative activity against human KB cells	[PMID: 31945642]
L02	IC₅₀	72.17 μM Compound: ATS	Cytotoxicity against human L02 cells measured after 48 hrs by MTT assay Cytotoxicity against human L02 cells measured after 48 hrs by MTT assay	[PMID: 30837097]
L6	IC₅₀	1.5 μM Compound: Artesunate	Cytotoxicity against rat L6 cells incubated for 690 hrs by Alamar blue assay Cytotoxicity against rat L6 cells incubated for 690 hrs by Alamar blue assay	[PMID: 23013253]
L6	IC₅₀	24 μM Compound: AS	Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay	[PMID: 25195945]
L6	IC₅₀	6.63 μM Compound: 2	Cytotoxicity in rat L6 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue dye based assay Cytotoxicity in rat L6 cells assessed as reduction in cell viability incubated for 72 hrs by alamar blue dye based assay	[PMID: 28988153]
Leukemia cell	IC₅₀	6.887 μM Compound: Artesunate	Antiproliferative activity against human Leukemia cell assessed as reduction in cell viability Antiproliferative activity against human Leukemia cell assessed as reduction in cell viability	[PMID: 31945642]
LS174T	IC₅₀	10 μM Compound: ARS	Cytotoxicity against human LS 174T cells after 72 hrs by formazan test Cytotoxicity against human LS 174T cells after 72 hrs by formazan test	[PMID: 23685181]
Lymphocyte	IC₅₀	80 μM Compound: Artesunate	Cytotoxicity against human lymphocytes Cytotoxicity against human lymphocytes	[PMID: 31784199]
MCF-10A	IC₅₀	21 μM Compound: Artesunate	Cytotoxicity against human MCF10A cells after 48 hrs by MTT assay Cytotoxicity against human MCF10A cells after 48 hrs by MTT assay	[PMID: 23790541]
MCF7	EC₅₀	4.21 μM Compound: 7	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30429957]
MCF7	IC₅₀	38.71 μM Compound: ATS	Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells measured after 48 hrs by MTT assay	[PMID: 30837097]
MDA-MB-231	IC₅₀	46 μM Compound: Artesunate	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay	[PMID: 23790541]
MDA-MB-231	EC₅₀	10.04 μM Compound: 7	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 30429957]
MDA-MB-231	IC₅₀	75.69 μM Compound: ATS	Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by MTT assay	[PMID: 30837097]
MDA-MB-361	EC₅₀	2.27 μM Compound: 7	Antiproliferative activity against human MDA-MB-361 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-361 cells after 72 hrs by MTT assay	[PMID: 30429957]
MRC5	IC₅₀	6.8 μM Compound: Artesunate	Cytotoxicity against human MRC5 cells incubated for 48 hrs by resazurin dye reduction assay Cytotoxicity against human MRC5 cells incubated for 48 hrs by resazurin dye reduction assay	[PMID: 23013253]
MRC5	IC₅₀	36 μM Compound: Artesunate	Cytotoxicity against human MRC5 cells Cytotoxicity against human MRC5 cells	[PMID: 25089179]
OVCAR-3	IC₅₀	67.3 μM Compound: 3; ARS	Cytotoxicity against human OVCAR3 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human OVCAR3 cells assessed as reduction in cell viability by MTT assay	[PMID: 33691167]
SiHa	EC₅₀	>30 μM Compound: 7	Antiproliferative activity against human SiHa cells after 72 hrs by MTT assay Antiproliferative activity against human SiHa cells after 72 hrs by MTT assay	[PMID: 30429957]
SK-HEP1	IC₅₀	10 μM Compound: ARS	Cytotoxicity against human SKHEP1 cells after 72 hrs by formazan test Cytotoxicity against human SKHEP1 cells after 72 hrs by formazan test	[PMID: 23685181]
SMMC-7721	IC₅₀	72.3 μM Compound: 3; ARS	Cytotoxicity against human SMMC-7721 cells assessed as reduction in cell viability by MTT assay Cytotoxicity against human SMMC-7721 cells assessed as reduction in cell viability by MTT assay	[PMID: 33691167]
T47D	EC₅₀	2.22 μM Compound: 7	Antiproliferative activity against human T47D cells after 72 hrs by MTT assay Antiproliferative activity against human T47D cells after 72 hrs by MTT assay	[PMID: 30429957]
WI-38	IC₅₀	>100 μM Compound: Artesunate	Cytotoxicity against human WI38 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay Cytotoxicity against human WI38 cells assessed as growth inhibition after 48 hrs by sulforhodamine B assay	[PMID: 27210430]
WI-38	IC₅₀	>100 μM Compound: ARS	Cytotoxicity against human WI38 cells assessed as reduction in cell viability measured after 48 hrs by SRB assay Cytotoxicity against human WI38 cells assessed as reduction in cell viability measured after 48 hrs by SRB assay	[PMID: 27448920]
WM 266-4	IC₅₀	8.46 μM Compound: AS	Antiproliferative activity against human WM266.4 cells assessed as inhibition of cell viability after 48 hrs by MTS assay Antiproliferative activity against human WM266.4 cells assessed as inhibition of cell viability after 48 hrs by MTS assay	[PMID: 31494469]

In Vitro

Artesunate is an inhibitor of both STAT-3^[1] and exported protein 1 (EXP1)^[2]. Artesunate treatment for 24 h causes a significant increase in the levels of reactive oxygen species (ROS) in a dose-dependent manner in both cell lines. Moreover, Western blotting shows that the levels ofγ-H2AX are significantly elevated when cancer cells are treated with Artesunate in the higher dose range for 24 h. Artesunate also shows a time-dependent effect on the level of RAD51 in A2780 and HO8910 cells. In two types of non-malignant cells, normal human fibroblasts and immortalized epithelial cells, FTE-187, the level of RAD51 is not altered by Artesunate. In A2780 cells, the level of RAD51 mRNA is indeed decreased by the addition of Artesunate, in a dose-dependent manner. Correspondingly, the promoter activity of RAD51 is significantly inhibited by Artesunate. In contrast, the RAD51 mRNA level in H8910 cells is not affected by Artesunate^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Tumor growth is significantly reduced in the group receiving combined treatment of Artesunate and cisplatin (P<0.01). In comparison, Artesunate alone has no significant effect on the growth of tumor xenografts for both cell lines^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 88495-63-0
Appearance Solid
Masse moléculaire 384.42
Formule C₁₉H₂₈O₈
Color White to off-white
SMILES

O=C(O[C@H]1[C@H](C)[C@]2([H])CC[C@@H](C)[C@]3([H])CC[C@@](O4)(C)OO[C@]32[C@]4([H])O1)CCC(O)=O
Structure Classification
- Terpenoids
- Sesquiterpenes
Initial Source
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (41)

All Cell Imaging/StainingCell Proliferation/Viability AssayFlow CytometryRT-PCRWB

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Journal Impact Factor

ACS Nano

Targeted Knockdown of Epithelial Estrogen Receptor α to Mitigate Ferroptosis and Epithelial-Mesenchymal Transition in Eosinophilic Asthma. [Abstract]

2025 Jun 10;19(22):21105-21117. PMID: 40424612

Artesunate purchased from MedChemExpress. Usage Cited in: ACS Nano. 2025 Jun 10;19(22):21105-21117. [Abstract]

Ferroptosis inducers (Artesunate, 10 μM) increased lipid peroxide levels in dEoL-1 cells.
Cell Commun Signal

Artesunate induces melanoma cell ferroptosis and augments antitumor immunity through targeting Ido1. [Abstract]

2024 Jul 26;22(1):378. PMID: 39061097

Artesunate purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Jul 26;22(1):378. [Abstract]

SK-MEL-28 cells were treated with indicated concentrations of ART (0, 10, 20, 40 µM) for 24 h, cells were stained with FerroOrange and photographed by fluorescence microscopy.

Artesunate purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Jul 26;22(1):378. [Abstract]

Cells were treated with indicated concentrations of ART (0, 10, 20, 40 µM) or Erastin for 24 h, flow cytometry detected the lipid peroxidation level by staining with C11-BODIPY.

Artesunate purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Jul 26;22(1):378. [Abstract]

Artesunate (0-40 μM, 24 h). qPCR detected the mRNA expression of Hmox1 in ART-treated B16F10 cells.

Artesunate purchased from MedChemExpress. Usage Cited in: Cell Commun Signal. 2024 Jul 26;22(1):378. [Abstract]

Artesunate (0-40 μM, 24 h). Western blot was employed to detect the expression of Hmox1 in ART-treated B16F10 cells.
Free Radic Biol Med

Mifepristone protects acetaminophen induced liver injury through NRF2/GSH/GST mediated ferroptosis suppression. [Abstract]

2024 Jun 19:S0891-5849(24)00531-8. PMID: 38906233
Biomed Pharmacother

Artesunate alleviates Sjögren's Syndrome by inhibiting the interferon-α signaling in plasmacytoid dendritic cells via TLR-MyD88-IRF7. [Abstract]

2024 Jun 14:177:116885. PMID: 38878633
Redox Rep

Artesunate ameliorates experimental autoimmune uveitis by inhibiting the LCN2-STAT3 axis and suppressing microglial activation. [Abstract]

2026 Dec;31(1):2627096. PMID: 41674301
Chin Med

Targeting the ferritinophagy axis: multi-target regulation of TFRC/FTH1/NCOA4 by artesunate ameliorates salivary gland dysfunction in Sjögren's Disease. [Abstract]

2026 Mar 19;21(1):97. PMID: 41851758
Biomater Sci

A cRGD-modified liposome for targeted delivery of artesunate to inhibit angiogenesis in endometriosis. [Abstract]

2025 Feb 11;13(4):1045-1058. PMID: 39829388
Biochem Pharmacol

Artesunate reduces oxidative stress and inflammation in NAFLD by activating the Nrf2 pathway. [Abstract]

2025 Dec 16:245:117643. PMID: 41412549
Chem Biol Interact

Artesunate induces autophagy dependent apoptosis through upregulating ROS and activating AMPK-mTOR-ULK1 axis in human bladder cancer cells. [Abstract]

2020 Nov 1;331:109273. PMID: 33002460
Drug Des Devel Ther

Role of GRP78 inhibiting artesunate-induced ferroptosis in KRAS mutant pancreatic cancer cells. [Abstract]

2019 Jul 2;13:2135-2144. PMID: 31456633
J Nutr Biochem

Artemisinin and its derivatives modulate glucose homeostasis and gut microbiota remodeling in a nutritional context. [Abstract]

2024 Jun 10:109687. PMID: 38866191
Int Immunopharmacol

Artesunate protects against ischemic stroke through THBS2/CD36/TLR4 pathway. [Abstract]

2026 Jun 1:178:116562. PMID: 41903303
Int Immunopharmacol

Artesunate alleviates chronic allergic rhinitis and asthma syndrome via the CCR3/NF-κB pathway: a comprehensive analysis. [Abstract]

2025 Sep 18:166:115562. PMID: 40972333
Int Immunopharmacol

Artesunate-induced ATG5-related autophagy enhances the cytotoxicity of NK92 cells on endometrial cancer cells via interactions between CD155 and CD226/TIGIT. [Abstract]

2021 Aug:97:107705. PMID: 33933849
Cancers (Basel)

Antineoplastic Drug Synergy of Artesunate with Navitoclax in Models of High-Grade Serous Ovarian Cancer. [Abstract]

2024 Mar 28;16(7):1321. PMID: 38610999
ACS Omega

Identification of New Modulators and Inhibitors of Palmitoyl-Protein Thioesterase 1 for CLN1 Batten Disease and Cancer. [Abstract]

2024 Feb 28;9(10):11870-11882. PMID: 38496939
FASEB J

Artesunate induces ferroptosis in osteosarcoma through NCOA4-mediated ferritinophagy. [Abstract]

2025 Apr 15;39(7):e70488. PMID: 40168090
J Inflamm Res

Study on the Mechanism of Artesunate in Modulating AR Epithelial Injury and Th2-Type Inflammatory Status. [Abstract]

2025 Apr 18:18:5329-5342. PMID: 40270560
J Neurochem

Artesunate restores mitochondrial fusion-fission dynamics and alleviates neuronal injury in Alzheimer's disease models. [Abstract]

2022 Aug;162(3):290-304. PMID: 35598091
Sci Rep

Combination of artesunate and ruxolitinib suppresses T cell leukemia/lymphoma proliferation via the JAK STAT pathway. [Abstract]

2026 Feb 11;16(1):8354. PMID: 41673103
Front Mol Neurosci

Artesunate Alleviates Paclitaxel-Induced Neuropathic Pain in Mice by Decreasing Metabotropic Glutamate Receptor 5 Activity and Neuroinflammation in Primary Sensory Neurons. [Abstract]

2022 May 27;15:902572. PMID: 35694442
Cell Signal

HDAC inhibitor enhances ferroptosis susceptibility of AML cells by stimulating iron metabolism. [Abstract]

2025 Jan 3:111583. PMID: 39756501
Heliyon

Artesunate induces ferroptosis by regulating MT1G and has an additive effect with doxorubicin in diffuse large B-cell lymphoma cells. [Abstract]

2024 Mar 22;10(7):e28584. PMID: 38560249
Toxicol Appl Pharmacol

Artesunate attenuates pulmonary fibrosis by suppressing fibroblast senescence through inhibition of the STAT3/p53 signaling pathway. [Abstract]

2026 Jan:506:117646. PMID: 41271031
Toxicol Appl Pharmacol

Artesunate attenuates osteoarthritis in mice by promoting MTA1 transcription through a USP7/FoxO1 axis. [Abstract]

2024 Aug 20:117075. PMID: 39173720
Pathogens

2026 Feb;15(2):169.
Basic Clin Pharmacol Toxicol

Artesunate inhibits osteoclast differentiation by inducing ferroptosis and prevents iron overload induced bone loss. [Abstract]

2023 Feb;132(2):144-153. PMID: 36433916

Artesunate purchased from MedChemExpress. Usage Cited in: Basic Clin Pharmacol Toxicol. 2023 Feb;132(2):144-153. [Abstract]

Artesunate (ART; 1, 2 μM) significantly reduces cell viability in RAW264.7 cells in the presence of RANKL but does not influence undifferentiating cells.
Diagnostics (Basel)

Preclinical Evaluation of Artesunate as an Antineoplastic Agent in Ovarian Cancer Treatment. [Abstract]

2021 Feb 26;11(3):395. PMID: 33652561
Front Vet Sci

Unrevealing the therapeutic potential of artesunate against emerging zoonotic Babesia microti infection in the murine model. [Abstract]

2024 May 9:11:1383291. PMID: 38784653
Neuroscience

Artesunate Reduces Remifentanil-induced Hyperalgesia and Peroxiredoxin-3 Hyperacetylation via Modulating Spinal Metabotropic Glutamate Receptor 5 in Rats. [Abstract]

2022 Apr 1:487:88-98. PMID: 35026318
Vet Microbiol

The Chinese medicine monomer Schisandrin C inhibits PRRSV infection by regulating the OGT-PI3K/AKT/mTOR signaling pathway. [Abstract]

2026 May:316:110992. PMID: 41865607
Appl Biol Chem

2026 Mar 13;69(1):19.
Oncologie

2025 Aug 12.
World J Surg Oncol

Inhibition of HOXC11 by artesunate induces ferroptosis and suppresses ovarian cancer progression through transcriptional regulation of the PROM2/PI3K/AKT pathway. [Abstract]

2024 Oct 8;22(1):268. PMID: 39380001
Biochem Biophys Res Commun

Ticlopidine protects hepatic ischemia-reperfusion injury via suppressing ferroptosis. [Abstract]

2024 Jul 23:733:150436. PMID: 39053102
J Gastrointest Oncol

Inhibition of hepatocellular carcinoma progression by artesunate via modulation of the TLR4/MyD88/NF-κB signaling pathway. [Abstract]

2025 Apr 30;16(2):599-614. PMID: 40386608
SSRN

2026 Mar 20.
Res Sq

2025 Sep 25.
SSRN

2025 Aug 27.
Loughborough University

2025.
Research Square Print

November 28th, 2022.

Solvant et solubilité

In Vitro:

DMSO : 83.33 mg/mL (216.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

7.5% Sodium bicarbonate : 2 mg/mL (5.20 mM; ultrasonic and warming and heat to 60°C)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6013 mL

13.0066 mL

26.0132 mL

5 mM

0.5203 mL

2.6013 mL

5.2026 mL

10 mM

0.2601 mL

1.3007 mL

2.6013 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Kinase Assay^[3]

After treatment with Artesunate for 24 h, cells are harvested and lysed in 1×cell lysis buffer. Total proteins of 15 to 25 μg are separated by SDS-PAGE and transferred to polyvinylidenedifluoride (PVDF) membranes. Membranes are blocked with 5% non-fat milk for 1 to 2 h at room temperature and then probed with primary antibodies and incubated at 4°C overnight. After extensive washing with TBS-T, membranes are incubated with appropriate HRP-conjugated secondary antibody for 1 h at room temperature, and then are detected by Western ECL-enhanced luminol reagent ^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[3]

A2780 and HO8910 cells are cultured in RPMI 1640, Normal human fibroblasts (NHF) in DMEM, and FTE-187 in M199, supplemented with 10% fetal bovine serum, 100 units/mL penicillin, and 100 mg/mL streptomycin. All the cells are incubated in a humidified atmosphere of 95% air and 5% CO₂. Artesunate is applied to the cultured cells at the concentration of 0, 5, 10, 25, or 50 µg/mL for various periods. The reactive oxygen species (ROS) production following Artesunate treatment is determined. Briefly, cells are loaded with 5 μM of CM-H2DCFDA and incubated at 37°C for 20 min after treatment with Artesunate. Cells are resuspended using preserving fluid and analyzed with a FACSCanto II. The peak excitation wavelength for oxidized CM-H2DCFDA is 490 nm and emission is 530 nm^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[3]

Four to six weeks old female athymic nude mice (BALB/c, nu/nu) are used. A2780 and HO8910 cells are harvested and resuspended in 0.1 ml of PBS, 5×10⁶ cells/0.2 mL are injected subcutaneously into the left inguinal area of the mice. Two weeks later, mice bearing tumors (~70 mm³ for A2780 and HO8910) are randomly divided into 4 groups. Artesunate is administered daily via i.p. injection at doses of 50 mg/kg alone for 16 days. The tumor growth is monitored every other day. Tumor volume is determined by the formula 1/2a×b² where a is the long diameter (mm) and b is the short diameter (mm)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (285 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Ilamathi M, et al. Artesunate as an Anti-Cancer Agent Targets Stat-3 and Favorably Suppresses Hepatocellular Carcinoma. Curr Top Med Chem. 2016;16(22):2453-63. [Content Brief]

[2]. Lisewski AM, et al. Supergenomic network compression and the discovery of EXP1 as a glutathione transferase inhibited by artesunate. Cell. 2014 Aug 14;158(4):916-928. [Content Brief]

[3]. Wang B, et al. Artesunate sensitizes ovarian cancer cells to cisplatin by downregulating RAD51. Cancer Biol Ther. 2015;16(10):1548-56. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
7.5% Sodium bicarbonate / DMSO	1 mM	2.6013 mL	13.0066 mL	26.0132 mL	65.0330 mL
7.5% Sodium bicarbonate / DMSO	5 mM	0.5203 mL	2.6013 mL	5.2026 mL	13.0066 mL
DMSO	10 mM	0.2601 mL	1.3007 mL	2.6013 mL	6.5033 mL
	15 mM	0.1734 mL	0.8671 mL	1.7342 mL	4.3355 mL
	20 mM	0.1301 mL	0.6503 mL	1.3007 mL	3.2517 mL
	25 mM	0.1041 mL	0.5203 mL	1.0405 mL	2.6013 mL
	30 mM	0.0867 mL	0.4336 mL	0.8671 mL	2.1678 mL
	40 mM	0.0650 mL	0.3252 mL	0.6503 mL	1.6258 mL
	50 mM	0.0520 mL	0.2601 mL	0.5203 mL	1.3007 mL
	60 mM	0.0434 mL	0.2168 mL	0.4336 mL	1.0839 mL
	80 mM	0.0325 mL	0.1626 mL	0.3252 mL	0.8129 mL
	100 mM	0.0260 mL	0.1301 mL	0.2601 mL	0.6503 mL

Keywords

Artesunate

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