Fluvastatin (Synonyms: NSC 758896) |
Catalog No.GC13535
One-Click Copy Product Info
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Fluvastatin, a lipophilic 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor, suppresses proliferation and induces apoptosis in various cancer cells.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 93957-54-1
Sample solution is provided at 25 µL, 10mM.
Fluvastatin, a lipophilic 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor, suppresses proliferation and induces apoptosis in various cancer cells[1-2]. Fluvastatin, which structurally mimics HMG-CoA to competitively block the enzyme’s active site, lowers total and low-density lipoprotein (LDL) cholesterol while exerting anti-atherogenic, antithrombotic, and antioxidant effects and improving vascular function[2-3].
In vitro, after 72h of treatment with the increasing concentrations of Fluvastatin (5, 10, and 20μM), human endometrial cancer (EC) cells exhibited a concentration-dependent decline in viability and proliferation, markedly reduced migration and invasion, and elevated apoptosis accompanied by progressive up-regulation of p53 and cleaved caspase-3[4]. A 24h incubation with 2.5μM Fluvastatin reproducibly gave over 50% inhibition of thrombin-induced von Willebrand factor (vWF) secretion, was more effective than shorter incubation times, did not disrupt the human umbilical-vein endothelial cells (HUVEC) culture monolayer, and did not change vWF antigen levels measured in cell lysates[5].
In vivo, after four daily intraperitoneal injections of 10mg/kg Fluvastatin in female C57BL/6J mice, total peritoneal cell counts remained unchanged, yet the proportion and absolute number of mast cells recovered from peritoneal lavage were markedly reduced[6]. The rats treated by gavage with 10mg/kg Fluvastatin showed a reduced number of polymorphonuclear neutrophils (PMN) compared to the control rats at 4h postinjection[7].
References:
[1] Zhang W, Wu J, Zhou L, et al. Fluvastatin, a lipophilic statin, induces apoptosis in human hepatocellular carcinoma cells through mitochondria-operated pathway. Indian J Exp Biol. 2010;48(12):1167-1174.
[2] Langtry HD, Markham A. Fluvastatin: a review of its use in lipid disorders. Drugs. 1999;57(4):583-606.
[3] Bonds M, Bordoni B. Fluvastatin. In: StatPearls. StatPearls Publishing; 2023.
[4] Cai Y, Zhao F. Fluvastatin suppresses the proliferation, invasion, and migration and promotes the apoptosis of endometrial cancer cells by upregulating Sirtuin 6 (SIRT6). Bioengineered. 2021;12(2):12509-12520.
[5] Fish RJ, Yang H, Viglino C, et al. Fluvastatin inhibits regulated secretion of endothelial cell von Willebrand factor in response to diverse secretagogues. Biochem J. 2007;405(3):597-604.
[6] Paez PA, Kolawole M, Taruselli MT, et al. Fluvastatin Induces Apoptosis in Primary and Transformed Mast Cells. J Pharmacol Exp Ther. 2020;374(1):104-112.
[7] Fischetti F, Carretta R, Borotto G, et al. Fluvastatin treatment inhibits leucocyte adhesion and extravasation in models of complement-mediated acute inflammation. Clin Exp Immunol. 2004;135(2):186-193.
| Cell experiment [1]: | |
Cell lines | Human endometrial cancer (EC) cell lines (RL95-2 and KLE) |
Preparation Method | Cells were maintained at 37°C with 5% CO2 and cultivated in DMEM containing 10% FBS. 48h later, Fluvastatin with different concentrations (5, 10, 20μM) was employed to incubate cells for 72h for the following experiments. |
Reaction Conditions | 5, 10, 20μM; 72h |
Applications | Fluvastatin inhibited the viability and proliferation of KLE and RL95-2 endometrial cancer cells in a concentration-dependent manner, while markedly suppressing their migratory and invasive capacities. Fluvastatin dose-dependently triggered apoptosis in KLE and RL95-2 cells, accompanied by progressive increases in p53 and cleaved caspase-3 levels. |
| Animal experiment [2]: | |
Animal models | Female C57BL/6J mice |
Preparation Method | Female C57BL/6J mice received 10mg/kg Fluvastatin or vehicle (DMSO diluted in PBS to match Fluvastatin solvent) daily by intraperitoneal injection for 4 days. Mice were sacrificed, and peritoneal lavage was harvested and analyzed for mast cells by staining for CD45+ cells and gating on FcεRI+/c-Kit+ cells. Cross sections of the small intestine were also analyzed by histology, using staining with pinacyanol erythosinate to identify mast cells. |
Dosage form | 10mg/kg; intraperitoneal injection |
Applications | Fluvastatin did not reduce total peritoneal cells but greatly reduced the proportion and total number of mast cells found in peritoneal lavage. |
References: | |
| Cas No. | 93957-54-1 | SDF | |
| Synonyms | NSC 758896 | ||
| Chemical Name | (E,3R,5S)-7-[3-(4-fluorophenyl)-1-propan-2-ylindol-2-yl]-3,5-dihydroxyhept-6-enoic acid | ||
| Canonical SMILES | CC(C)N1C2=CC=CC=C2C(=C1C=CC(CC(CC(=O)O)O)O)C3=CC=C(C=C3)F | ||
| Formula | C24H26FNO4 | M.Wt | 411.47 |
| Solubility | ≥ 20.57 mg/mL in DMSO, ≥ 42.2 mg/mL in EtOH with gentle warming, ≥ 32.53 mg/mL in Water with gentle warming | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4303 mL | 12.1516 mL | 24.3031 mL |
| 5 mM | 486.1 μL | 2.4303 mL | 4.8606 mL |
| 10 mM | 243 μL | 1.2152 mL | 2.4303 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)