| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Artesunate (Amivas; SM-804; WR-256283; HSDB-7458; Armax 200), an approved antimalaria agent, is a semisynthetic derivative of artemisinin with an IC50 of < 5 μM for small cell lung carcinoma cell line H69. It is an active ingredient in the Chinese herb Artemisia annua and has been used in Malaria studies. Artesunate has been tested against 55 cell lines and demonstrated anti-cancer activity. Research shows that conditional expression of CDC25A heightens the sensitivity of tumor cells to artesunate.
| ln Vitro |
Artesunate inhibits exportin 1 (EXP1)[2] and STAT-3[1]. Both cell lines showed a notable dose-dependent rise in reactive oxygen species (ROS) following a 24-hour treatment with artesunate. Furthermore, artesunate treatment of cancer cells at greater doses for 24 hours was found to considerably raise γ-H2AX levels, as demonstrated by Western blotting. Additionally, in A2780 and HO8910 cells, artesunate exhibited time-dependent impacts on RAD51 levels. Two types of non-malignant cells (normal human fibroblasts and immortalized epithelial cells FTE-187) showed no change in RAD51 levels in response to artesunate. In fact, artesunate decreased RAD51 mRNA levels in A2780 cells in a dose-dependent way. Correspondingly, artesunate markedly reduced the promoter activity of RAD51. In contrast, artesunate had no effect on the amounts of RAD51 mRNA in H8910 cells [3].
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| ln Vivo |
In the group receiving combined treatment with artesunate and cisplatin, tumor development was considerably inhibited (P<0.01). On the other hand, neither cell line's tumor xenografts grew significantly when artesunate was used alone [3].
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| 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 |
| Molecular Formula |
C19H28O8
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| Molecular Weight |
384.42
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| CAS # |
88495-63-0
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| Related CAS # |
Artesunate-d3;1316303-44-2;Artesunate-d4;1316753-15-7
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| SMILES |
O1[C@@]23[C@]4([H])OC([H])(C([H])(C([H])([H])[H])[C@@]2([H])C([H])([H])C([H])([H])C([H])(C([H])([H])[H])[C@@]3([H])C([H])([H])C([H])([H])[C@@](C([H])([H])[H])(O1)O4)OC(C([H])([H])C([H])([H])C(=O)O[H])=O
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| InChi Key |
FIHJKUPKCHIPAT-AHIGJZGOSA-N
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| InChi Code |
InChI=1S/C19H28O8/c1-10-4-5-13-11(2)16(23-15(22)7-6-14(20)21)24-17-19(13)12(10)8-9-18(3,25-17)26-27-19/h10-13,16-17H,4-9H2,1-3H3,(H,20,21)/t10-,11-,12+,13+,16-,17-,18-,19-/m1/s1
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| Chemical Name |
4-oxo-4-(((3R,5aS,6R,8aS,9R,10S,12R,12aR)-3,6,9-trimethyldecahydro-12H-3,12-epoxy[1,2]dioxepino[4,3-i]isochromen-10-yl)oxy)butanoic acid
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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