1. JAK/STAT Signaling
    Stem Cell/Wnt
    Apoptosis
    Anti-infection
  2. STAT
    Ferroptosis
    Parasite
    Virus Protease
  3. Artesunate

Artesunate 

Cat. No.: HY-N0193 Purity: >98.0%
Handling Instructions

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

For research use only. We do not sell to patients.

Artesunate Chemical Structure

Artesunate Chemical Structure

CAS No. : 88495-63-0

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Description

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

IC50 & Target[1][2]

Stat-3

 

EXP1

 

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].

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].

Clinical Trial
Molecular Weight

384.42

Formula

C₁₉H₂₈O₈

CAS No.

88495-63-0

SMILES
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (216.77 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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].

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].

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].

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

References

Purity: >98.0%

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Keywords:

ArtesunateSTATFerroptosisParasiteVirus ProteaseInhibitorinhibitorinhibit

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