Bufalin (Synonyms: NSC 89595) |
Katalog-Nr.GN10365
One-Click Copy Product Info
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Bufalin is a Na+/K+-ATPase inhibitor (α1: Kd = 42.5nM; α2: Kd = 45nM; α3: Kd = 40nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 465-21-4
Sample solution is provided at 25 µL, 10mM.
Bufalin is a Na+/K+-ATPase inhibitor (α1: Kd = 42.5nM; α2: Kd = 45nM; α3: Kd = 40nM) [1]. Bufalin primarily inhibits the activity of Na⁺/K⁺-ATPase on cell membranes, leading to elevated intracellular calcium concentrations [2]. Bufalin induction of apoptosis and inhibition of tumor cell proliferation can also have multiple anti-tumor mechanisms, including triggering autophagy and inhibiting tumor angiogenesis [3]. Bufalin is used to treat various tumors, including liver cancer, lung cancer, breast cancer, and leukemia [4].
In NCI-H640 cells, after treatment with Bufalin (1μM, 2μM, 4μM; 24h), the activity of cells decreased significantly [5]. In Ishikawa, SK-OV-3 and OMC-3 ovarian cancer cells, Bufalin (0.1-10ng/mL; 48h) can inhibit the proliferation of endometrial and ovarian cancer cells [6]. In human RCC ACHN cells, Bufalin (0-80nM; 12-72h) suppresses the proliferation and metastasis of renal cell carcinoma by inhibiting the PI3K/Akt/mTOR signaling pathway [7].
In carrageenan-induced paw edema rat model, after Bufalin (0.15mg/kg, 0.3mg/kg, 0.6mg/kg; ip; single injection) treatmentthe, volume of paw edema in rats was significantly reduced [8]. In HCCLM3 cell metastatic orthotopic tumor mouse model, orthotopic transplanted tumor tissues undergo necrosis and apoptosis induced by Bufalin (1mg/kg, 1.5mg/kg; ip; 30d) treatment [9].
References:
[1]. Katz A, Lifshitz Y, Bab-Dinitz E, et al. Selectivity of digitalis glycosides for isoforms of human Na, K-ATPase[J]. Journal of Biological Chemistry, 2010, 285(25): 19582-19592.
[2]. Wu S H, Bau D T, Hsiao Y T, et al. Bufalin induces apoptosis in vitro and has Antitumor activity against human lung cancer xenografts in vivo[J]. Environmental Toxicology, 2017, 32(4): 1305-1317.
[3]. Yin P H, Liu X, Qiu Y Y, et al. Anti-tumor activity and apoptosis-regulation mechanisms of bufalin in various cancers: new hope for cancer patients[J]. Asian Pacific journal of cancer prevention, 2012, 13(11): 5339-5343.
[4]. Lan Y L, Lou J C, Jiang X W, et al. A research update on the anticancer effects of bufalin and its derivatives[J]. Oncology letters, 2019, 17(4): 3635-3640.
[5]. Wu S H, Wu T Y, Hsiao Y T, et al. Bufalin induces cell death in human lung cancer cells through disruption of DNA damage response pathways[J]. The American Journal of Chinese Medicine, 2014, 42(03): 729-742.
[6]. Takai N, Ueda T, Nishida M, et al. Bufalin induces growth inhibition, cell cycle arrest and apoptosis in human endometrial and ovarian cancer cells[J]. International journal of molecular medicine, 2008, 21(5): 637-643.
[7]. Xie J, Lin W, Huang L, et al. Bufalin suppresses the proliferation and metastasis of renal cell carcinoma by inhibiting the PI3K/Akt/mTOR signaling pathway[J]. Oncology letters, 2018, 16(3): 3867-3873.
[8]. Wen L, Huang Y, Xie X, et al. Anti‐inflammatory and antinociceptive activities of bufalin in rodents[J]. Mediators of inflammation, 2014, 2014(1): 171839.
[9]. Zhang Z J, Yang Y K, Wu W Z. Bufalin attenuates the stage and metastatic potential of hepatocellular carcinoma in nude mice[J]. Journal of translational medicine, 2014, 12(1): 57.
| Cell experiment [1]: | |
Cell lines | NCI-H640 cells |
Preparation Method | Approximately 2 × 105 cells/well of NCI-H640 cells in 12-well plates were incubated with Bufalin at final concentrations of 0 (vehicle, 0.5% DMSO), 1, 2 and 4μM for 24 hours. Cells from each treatment were stained with PI (5 g/ml) and analyzed by flow cytometry and cell viability was calculated. |
Reaction Conditions | 1μM, 2μM, 4μM; 24h |
Applications | After treatment with Bufalin, the activity of cells decreased significantly. |
| Animal experiment [2]: | |
Animal models | Carrageenan-induced paw edema rat model |
Preparation Method | The anti-inflammatory effect was based on the inhibition of carrageenan-induced hind paw edema. Bufalin (0.15, 0.3, and 0.6mg/kg, i.p.), indomethacin (10mg/kg, i.p.), and vehicle were administered intraperitoneally 30min prior to carrageenan injection. Each rat received a subplantar injection of carrageenan (0.1mL, 1% w/v in saline) in the right hind paw. A plethysmometer measured the volume of paw edema before and at various times (1, 2, 4, and 6h) after the carrageenan injection. The paw swelling ratio was calculated as a percentage increase from the paw volume measured prior to carrageenan injection. Rat paws were collected after the final assessment. Each hind paw was cut at the level of the calcaneus bone and used for Western blot analysis. |
Dosage form | 0.15mg/kg, 0.3mg/kg, 0.6mg/kg; ip; single injection |
Applications | After Bufalin treatment, the volume of paw edema in rats was significantly reduced. |
References: | |
| Cas No. | 465-21-4 | SDF | |
| Überlieferungen | NSC 89595 | ||
| Chemical Name | 5-[(3S,5R,8R,9S,10S,13R,14S,17R)-3,14-dihydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,11,12,15,16,17-tetradecahydrocyclopenta[a]phenanthren-17-yl]pyran-2-one | ||
| Canonical SMILES | CC12CCC(CC1CCC3C2CCC4(C3(CCC4C5=COC(=O)C=C5)O)C)O | ||
| Formula | C24H34O4 | M.Wt | 386.52 |
| Löslichkeit | ≥ 38.7mg/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. |
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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 | 2.5872 mL | 12.9359 mL | 25.8719 mL |
| 5 mM | 517.4 μL | 2.5872 mL | 5.1744 mL |
| 10 mM | 258.7 μL | 1.2936 mL | 2.5872 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)