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Artesunate (Synonyms: Artesunic Acid, NSC 712571, WR 256283)

Katalog-Nr.GC10889

Ableitung des Naturprodukts Artemisinin

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Artesunate Chemische Struktur

Cas No.: 88495-63-0

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10mM (in 1mL DMSO)
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10mg
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50mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment:

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 experiment:

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 experiment:

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.

Background

Artesunat ist ein Hemmstoff sowohl von STAT-3 als auch von exportiertem Protein 1 (EXP1).

Artesunat ist ein Inhibitor sowohl von STAT-3[1] als auch von exportiertem Protein 1 (EXP1)[2]. Eine Behandlung mit Artesunat für 24 Stunden führt in beiden Zelllinien dosisabhängig zu einer signifikanten Erhöhung der reaktiven Sauerstoffspezies (ROS). Darüber hinaus zeigt die Western-Blot-Analyse, dass die γ-H2AX-Spiegel signifikant erhöht sind, wenn Krebszellen im höheren Dosisbereich für 24 Stunden mit Artesunat behandelt werden. Artesunat zeigt auch eine zeitabhängige Wirkung auf den RAD51-Spiegel in A2780- und HO8910-Zellen. Bei zwei Arten von nicht-malignen Zellen, normalen menschlichen Fibroblasten und immortalisierten epithelialen Zellen FTE-187, wird der RAD51-Spiegel durch Artesunat nicht verändert. In A2780-Zellen wird der RAD51-mRNA-Spiegel tatsächlich durch Zugabe von Artesunat dosisabhängig verringert. Entsprechend wird die Promotoraktivität von RAD51 signifikant durch Artesunat gehemmt. Im Gegensatz dazu wird der RAD51-mRNA-Spiegel in H8910-Zellen nicht durch Artesunate beeinflusst[3].

Das Tumorwachstum wird signifikant reduziert in der Gruppe, die eine kombinierte Behandlung mit Artesunat und Cisplatin erhält (P<0.01). Im Vergleich dazu hat Artesunat allein keinen signifikanten Effekt auf das Wachstum von Tumor-Xenografts für beide Zelllinien[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.

Chemical Properties

Cas No. 88495-63-0 SDF
Überlieferungen Artesunic Acid, NSC 712571, WR 256283
Canonical SMILES O=C(CCC(O)=O)O[C@H]1O[C@@H]2O[C@@]3(C)OO[C@]42[C@@H](CC3)[C@H](C)CC[C@H]4[C@H]1C
Formula C19H28O8 M.Wt 384.42
Löslichkeit ≥ 16.3mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
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
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