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88495-63-0 182824-33-5
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88495-63-0

88495-63-0 structure
88495-63-0 structure
  • Name: Artesunate
  • Chemical Name: Artesunate
  • CAS Number: 88495-63-0
  • Molecular Formula: C19H28O8
  • Molecular Weight: 384.421
  • Catalog: API Antiparasitic drug Antimalarial
  • Create Date: 2018-02-06 08:00:00
  • Modify Date: 2024-01-02 15:14:13
  • Artesunate is an inhibitor of both STAT-3 and exported protein 1 (EXP1).
Name Artesunate
Synonyms 4-Oxo-4-{[(1R,4S,5R,8S,9R,10R,12R,13R)-1,5,9-trimethyl-11,14,15,16-tetraoxatetracyclo[10.3.1.0.0]hexadec-10-yl]oxy}butanoic acid
Cosunate
Qinghaozhi
Saphnate
Arteannuinum
AsuMax
4-oxo-4-{[(3R,5aS,6R,8aS,9R,10R,12R,12aR)-3,6,9-trimethyldecahydro-3,12-epoxy[1,2]dioxepino[4,3-i]isochromen-10-yl]oxy}butanoic acid
PlasMotriM
MFCD00866204
PlasMotrin
Butanedioic acid, mono[(3R,5aS,6R,8aS,9R,10R,12R,12aR)-decahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin-10-yl] ester
vARTESUNATE
Description Artesunate is an inhibitor of both STAT-3 and exported protein 1 (EXP1).
Related Catalog
Target

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].
Kinase Assay 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].
Cell Assay 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].
Animal Admin 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].
References

[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.

[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.

[3]. Wang B, et al. Artesunate sensitizes ovarian cancer cells to cisplatin by downregulating RAD51. Cancer Biol Ther. 2015;16(10):1548-56.
Density 1.3±0.1 g/cm3
Boiling Point 507.1±50.0 °C at 760 mmHg
Melting Point 132-135ºC
Molecular Formula C19H28O8
Molecular Weight 384.421
Flash Point 175.6±23.6 °C
Exact Mass 384.178406
PSA 100.52000
LogP 2.94
Vapour Pressure 0.0±2.8 mmHg at 25°C
Index of Refraction 1.544
Storage condition Room temp
Water Solubility acetone: soluble33.4mg/mL
Hazard Codes Xn
Risk Phrases R20/21/22
Safety Phrases 24/25
HS Code 29419090
108-30-5 structure

108-30-5
63968-64-9 structure

63968-64-9

~97%

88495-63-0 structure

88495-63-0
Literature: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH Patent: WO2004/50661 A1, 2004 ; Location in patent: Page 7 ;
71939-50-9 structure

71939-50-9

~%

88495-63-0 structure

88495-63-0
Literature: European Journal of Organic Chemistry, , # 1 p. 113 - 132
Precursor  3

DownStream  0


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