Bufalin
Based on 9 publication(s) in Google Scholar
Bufalin is an active component isolated from Chan Su, acts as a potent Na+/K+-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively. Anti-cancer activity.
For research use only. We do not sell to patients.
- Purity: 99.86%
- CAS No.: 465-21-4
- Formula: C24H34O4
- Molecular Weight:386.52
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Bufalin
More- Pharmacol Res. 2021 Dec:174:105927. [Abstract]
- Apoptosis. 2023 Oct;28(9-10):1390-1405. [Abstract]
- Int J Mol Med. 2020 Dec;46(6):2137-2149. [Abstract]
- J Ethnopharmacol. 2025 Apr 9:345:119589. [Abstract]
- Int J Mol Sci. 2022 Nov 1;23(21):13354. [Abstract]
- Cancers. 2020 Aug 4;12(8):2169. [Abstract]
- Chem Res Toxicol. 2019 Dec 16;32(12):2479-2487. [Abstract]
- Vet Microbiol. 2025 Sep 15:310:110730. [Abstract]
- J Assist Reprod Genet. 2025 Feb;42(2):665-678. [Abstract]
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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WB
Biological Activity
Kd: 42.5 nM (Na,K-ATPase α1), 45 nM (Na,K-ATPase α2), 40 nM (Na,K-ATPase α3)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 786-0 | EC50 |
7.5 nM
Compound: 4
|
Cytotoxicity against human 786-O cells assessed as decrease in cell viability after 72 hrs by MTS assay
Cytotoxicity against human 786-O cells assessed as decrease in cell viability after 72 hrs by MTS assay
|
[PMID: 30369239] |
| A549 | IC50 |
0.6 μM
Compound: 7
|
Cytotoxicity against human A549 cells after 24 hrs by MTT assay
Cytotoxicity against human A549 cells after 24 hrs by MTT assay
|
[PMID: 24050254] |
| Bel-7402 | IC50 |
7 nM
Compound: 1
|
Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay
Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay
|
[PMID: 15844967] |
| Bel-7402 | IC50 |
7 x 10-3 μM
Compound: 1
|
Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay
Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay
|
[PMID: 15844967] |
| Bel-7402 | IC50 |
7*10-3 μmol/L
Compound: 1
|
Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay
Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay
|
[PMID: 15844967] |
| BGC-823 | IC50 |
4.5 x 10-2 μM
Compound: 1
|
Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay
Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay
|
[PMID: 15844967] |
| BGC-823 | IC50 |
4.5*10-2 μmol/L
Compound: 1
|
Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay
Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay
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[PMID: 15844967] |
| BGC-823 | IC50 |
0.99 μM
Compound: 6, bufalin
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Cytotoxicity against human BGC823 cells
Cytotoxicity against human BGC823 cells
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[PMID: 17911017] |
| BGC-823 | IC50 |
0.99 μM/L
Compound: 6, bufalin
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Cytotoxicity against human BGC823 cells
Cytotoxicity against human BGC823 cells
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[PMID: 17911017] |
| BXPC-3 | EC50 |
11 nM
Compound: 4
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Cytotoxicity against human BxPC3 cells assessed as decrease in cell viability after 72 hrs by MTS assay
Cytotoxicity against human BxPC3 cells assessed as decrease in cell viability after 72 hrs by MTS assay
|
[PMID: 30369239] |
| CCRF S-180 | IC50 |
>50 μM
Compound: 1
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Cytotoxicity against mouse S180 cells expressing mutated alpha-1 Na+/K+-ATPase assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against mouse S180 cells expressing mutated alpha-1 Na+/K+-ATPase assessed as growth inhibition after 48 hrs by MTT assay
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[PMID: 23799775] |
| CCRF S-180 | EC50 |
>20000 nM
Compound: 4
|
Cytotoxicity against mouse S180 cells assessed as decrease in cell viability after 72 hrs by MTS assay
Cytotoxicity against mouse S180 cells assessed as decrease in cell viability after 72 hrs by MTS assay
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[PMID: 30369239] |
| CNE | IC50 |
0.279 μM
Compound: 1
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Cytotoxicity against human CNE1 cells assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against human CNE1 cells assessed as growth inhibition after 48 hrs by MTT assay
|
[PMID: 23799775] |
| CNE2Z | IC50 |
0.46 μM
Compound: 1
|
Cytotoxicity against human CNE2Z cells assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against human CNE2Z cells assessed as growth inhibition after 48 hrs by MTT assay
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[PMID: 23799775] |
| H22 | IC50 |
>50 μM
Compound: 1
|
Cytotoxicity against mouse H22 cells expressing mutated alpha-1 Na+/K+-ATPase assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against mouse H22 cells expressing mutated alpha-1 Na+/K+-ATPase assessed as growth inhibition after 48 hrs by MTT assay
|
[PMID: 23799775] |
| HCT-116 | EC50 |
11 nM
Compound: 4
|
Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by MTS assay
Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by MTS assay
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[PMID: 30369239] |
| HeLa | IC50 |
2.8 x 10-2 μM
Compound: 1
|
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
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[PMID: 15844967] |
| HeLa | IC50 |
2.8*10-2 μmol/L
Compound: 1
|
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
|
[PMID: 15844967] |
| HeLa | IC50 |
0.73 μM
Compound: 6, bufalin
|
Cytotoxicity against human HeLa cells
Cytotoxicity against human HeLa cells
|
[PMID: 17911017] |
| HeLa | IC50 |
0.73 μM/L
Compound: 6, bufalin
|
Cytotoxicity against human HeLa cells
Cytotoxicity against human HeLa cells
|
[PMID: 17911017] |
| HeLa | IC50 |
279.9 nM
Compound: Bufalin
|
Cytotoxicity activity against human HeLa cells after 48 hrs by MTT assay
Cytotoxicity activity against human HeLa cells after 48 hrs by MTT assay
|
[PMID: 30245398] |
| HeLa | IC50 |
594.2 nM
Compound: Bufalin
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Cytotoxicity activity against human HeLa cells after 24 hrs by MTT assay
Cytotoxicity activity against human HeLa cells after 24 hrs by MTT assay
|
[PMID: 30245398] |
| HepG2 | IC50 |
0.64 μM
Compound: 6, bufalin
|
Cytotoxicity against human HepG2 cells
Cytotoxicity against human HepG2 cells
|
[PMID: 17911017] |
| HepG2 | IC50 |
0.64 μM/L
Compound: 6, bufalin
|
Cytotoxicity against human HepG2 cells
Cytotoxicity against human HepG2 cells
|
[PMID: 17911017] |
| HepG2 | IC50 |
0.345 μM
Compound: 1
|
Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay
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[PMID: 23799775] |
| HepG2 | IC50 |
0.589 μM
Compound: 1
|
Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay
|
[PMID: 23799775] |
| HepG2 | IC50 |
0.6 μM
Compound: 7
|
Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay
|
[PMID: 24050254] |
| HepG2 | EC50 |
35 nM
Compound: 4
|
Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTS assay
Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTS assay
|
[PMID: 30369239] |
| HL-60 | IC50 |
<0.01 μg/mL
Compound: 16
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Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
|
[PMID: 11575946] |
| HUVEC | EC50 |
12 nM
Compound: 4
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Cytotoxicity against human HUVEC cells assessed as decrease in cell viability after 72 hrs by MTS assay
Cytotoxicity against human HUVEC cells assessed as decrease in cell viability after 72 hrs by MTS assay
|
[PMID: 30369239] |
| KB | IC50 |
0.67 μg/mL
Compound: 16
|
Cytotoxicity against human KB cells after 72 hrs by MTT assay
Cytotoxicity against human KB cells after 72 hrs by MTT assay
|
[PMID: 11575946] |
| MCF7 | EC50 |
42 nM
Compound: 4
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Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 72 hrs by MTS assay
Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 72 hrs by MTS assay
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[PMID: 30369239] |
| MES-SA | EC50 |
28 nM
Compound: 4
|
Cytotoxicity against human MESSA cells assessed as decrease in cell viability after 72 hrs by MTS assay
Cytotoxicity against human MESSA cells assessed as decrease in cell viability after 72 hrs by MTS assay
|
[PMID: 30369239] |
| MES-SA/Dx5 | EC50 |
18 nM
Compound: 4
|
Cytotoxicity against human MES-SA/Dx5 cells assessed as decrease in cell viability after 72 hrs by MTS assay
Cytotoxicity against human MES-SA/Dx5 cells assessed as decrease in cell viability after 72 hrs by MTS assay
|
[PMID: 30369239] |
| MH60 | IC50 |
>25 μg/mL
Compound: 16
|
Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay
Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay
|
[PMID: 11575946] |
| MH60 | IC50 |
>64.8 μM
Compound: 3
|
Growth inhibition of IL-6-independent mouse MH60 cells after 72 hrs by MTT assay
Growth inhibition of IL-6-independent mouse MH60 cells after 72 hrs by MTT assay
|
[PMID: 15620253] |
| MH60 | IC50 |
31.9 μM
Compound: 3
|
Growth inhibition of IL6-dependent mouse MH60 cells after 72 hrs by MTT assay in presence of human recombinant IL6
Growth inhibition of IL6-dependent mouse MH60 cells after 72 hrs by MTT assay in presence of human recombinant IL6
|
[PMID: 15620253] |
| NCI-H1975 | EC50 |
13 nM
Compound: 4
|
Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by MTS assay
Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by MTS assay
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[PMID: 30369239] |
| SK-OV-3 | EC50 |
10 nM
Compound: 4
|
Cytotoxicity against human SKOV3 cells assessed as decrease in cell viability after 72 hrs by MTS assay
Cytotoxicity against human SKOV3 cells assessed as decrease in cell viability after 72 hrs by MTS assay
|
[PMID: 30369239] |
| U-87MG ATCC | EC50 |
14 nM
Compound: 4
|
Cytotoxicity against human U87MG cells assessed as decrease in cell viability after 72 hrs by MTS assay
Cytotoxicity against human U87MG cells assessed as decrease in cell viability after 72 hrs by MTS assay
|
[PMID: 30369239] |
Bufalin (0, 1, 2, 4 μM for 48 hours) decreases cell viability in NCI-H460 cells[2].
Bufalin (2 μM) increases caspae-3, Endo G and GADD153 mRNA expression, but decreases the GRP78 mRNA expression[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H460 cells
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Concentration:0, 1, 2, 4 μM
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Incubation Time:48 hours
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Result:Decreased viability of NCI-H460 cells in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Forty male athymic BALB/c nu/nu mice (6-8 weeks old)[2]
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Dosage:0.1, 0.2, or 0.4 mg/kg
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Administration:I.P. every day until 14 days
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Result:Dose-dependently suppressed tumor growth.
Chemical Information
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CAS No. 465-21-4
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Appearance Solid
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Molecular Weight 386.52
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Formula C24H34O4
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Color White to off-white
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SMILES
O[C@]([C@@](CC[C@@]1([H])[C@@]2(CC[C@H](O)C1)C)([H])[C@]2([H])CC3)(CC[C@@H]4C(C=C5)=COC5=O)[C@]34C
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Structure Classification
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Initial Source
toad
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (9)
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Journal Impact Factor
-
Most Recent
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Pharmacol Res
2021 Dec:174:105927. PMID: 34740818
Bufalin purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2021 Dec:174:105927. [Abstract]
CCK8 assay of HCT116 cells upon Bufalin (BFL) (0-0.3 μM; 24 h) treatment at indicated doses.
Bufalin purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2021 Dec:174:105927. [Abstract]
Bufalin (BFL) (0.03-0.3 μM; 24 h) caused TOP3β depletion in HCT116 cells.
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Apoptosis
Bufalin targeting BFAR inhibits the occurrence and metastasis of gastric cancer through PI3K/AKT/mTOR signal pathway. [Abstract]2023 Oct;28(9-10):1390-1405. PMID: 37253905
Bufalin purchased from MedChemExpress. Usage Cited in: Apoptosis. 2023 Oct;28(9-10):1390-1405. [Abstract]
Bufalin (12.5, 25, 50, 100, 200 nM; 24, 48, 72 h) significantly reduces the viability of MKN-45 and HGC-27 GC cells in a dose- and time-dependent manner.
Bufalin purchased from MedChemExpress. Usage Cited in: Apoptosis. 2023 Oct;28(9-10):1390-1405. [Abstract]
Bufalin (20-80 nM; 12-24 h) significantly inhibited the migration ability of MKN-45 and HGC-27 GC cell lines in a dose-dependent manner.
Bufalin purchased from MedChemExpress. Usage Cited in: Apoptosis. 2023 Oct;28(9-10):1390-1405. [Abstract]
Bufalin (1 mg/kg; 100 μL; i.p.; every two days for 2–3 weeks) significantly decreased the tumor volume of gastric cancer (GC) xenograft mice.
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Int J Mol Med
Bufalin exerts antitumor effects in neuroblastoma via the induction of reactive oxygen species‑mediated apoptosis by targeting the electron transport chain. [Abstract]2020 Dec;46(6):2137-2149. PMID: 33125107 -
J Ethnopharmacol
Integrated network pharmacology, proteomics, molecular docking, and experiments in vivo and in vitro to explore the efficacy and potential mechanism of bufalin against hepatocellular carcinoma angiogenesis. [Abstract]2025 Apr 9:345:119589. PMID: 40057142 -
Int J Mol Sci
Bufalin Inhibits Tumorigenesis, Stemness, and Epithelial-Mesenchymal Transition in Colorectal Cancer through a C-Kit/Slug Signaling Axis. [Abstract]2022 Nov 1;23(21):13354. PMID: 36362141 -
Cancers
Identification of Cardiac Glycosides as Novel Inhibitors of eIF4A1-Mediated Translation in Triple-Negative Breast Cancer Cells. [Abstract]2020 Aug 4;12(8):2169. PMID: 32759815 -
Chem Res Toxicol
Cardiac Glycoside Compound Isolated from Helleborus thibetanus Franch Displays Potent Toxicity against HeLa Cervical Carcinoma Cells through ROS-Independent Autophagy. [Abstract]2019 Dec 16;32(12):2479-2487. PMID: 31714069 -
Vet Microbiol
Identification and evaluation of Nordihydroguaiaretic acid (NDGA) as an active traditional Chinese medicine compound inhibiting the 3C-like protease of feline infectious peritonitis virus. [Abstract]2025 Sep 15:310:110730. PMID: 40976146 -
J Assist Reprod Genet
FXYD1 was identified as a hub gene in recurrent miscarriage and involved in decidualization via regulating Na/K-ATPase activity. [Abstract]2025 Feb;42(2):665-678. PMID: 39730944
Solvent & Solubility
DMSO : 100 mg/mL (258.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[1]. Katz A, et al. Selectivity of digitalis glycosides for isoforms of human Na,K-ATPase. J Biol Chem. 2010 Jun 18;285(25):19582-92. [Content Brief]
[2]. Wu SH, et al. Bufalin induces apoptosis in vitro and has Antitumor activity against human lung cancer xenografts in vivo. Environ Toxicol. 2017 Apr;32(4):1305-1317. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5872 mL | 12.9359 mL | 25.8719 mL | 64.6797 mL |
| 5 mM | 0.5174 mL | 2.5872 mL | 5.1744 mL | 12.9359 mL | |
| 10 mM | 0.2587 mL | 1.2936 mL | 2.5872 mL | 6.4680 mL | |
| 15 mM | 0.1725 mL | 0.8624 mL | 1.7248 mL | 4.3120 mL | |
| 20 mM | 0.1294 mL | 0.6468 mL | 1.2936 mL | 3.2340 mL | |
| 25 mM | 0.1035 mL | 0.5174 mL | 1.0349 mL | 2.5872 mL | |
| 30 mM | 0.0862 mL | 0.4312 mL | 0.8624 mL | 2.1560 mL | |
| 40 mM | 0.0647 mL | 0.3234 mL | 0.6468 mL | 1.6170 mL | |
| 50 mM | 0.0517 mL | 0.2587 mL | 0.5174 mL | 1.2936 mL | |
| 60 mM | 0.0431 mL | 0.2156 mL | 0.4312 mL | 1.0780 mL | |
| 80 mM | 0.0323 mL | 0.1617 mL | 0.3234 mL | 0.8085 mL | |
| 100 mM | 0.0259 mL | 0.1294 mL | 0.2587 mL | 0.6468 mL |