Cat. No.: HY-N0878

Bufotalin

4 Cited Publications

Customer Review

Based on 4 publication(s) in Google Scholar

Bufotalin is a steroid lactone isolated from Venenum Bufonis with potently antitumor activities. Bufotalin induces cancer cell apoptosis and also induces endoplasmic reticulum (ER) stress activation.

For research use only. We do not sell to patients.

Purity: 99.82%
CAS No.: 471-95-4
Formula: C₂₆H₃₆O₆
Molecular Weight:444.56

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Bufotalin Chemical Structure

CAS No.: 471-95-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	14 nM Compound: 2a	Cytotoxicity against human A549 cells after 3 days by MTT assay Cytotoxicity against human A549 cells after 3 days by MTT assay	[PMID: 23706005]
A549	IC₅₀	0.9 μM Compound: 9	Cytotoxicity against human A549 cells after 24 hrs by MTT assay Cytotoxicity against human A549 cells after 24 hrs by MTT assay	[PMID: 24050254]
A549	IC₅₀	4.21 μM Compound: BT	Antitumor activity against human A549 cells xenografted in mouse assessed as tumor growth inhibition at 10 mg/ml,ip administrated for 21 days Antitumor activity against human A549 cells xenografted in mouse assessed as tumor growth inhibition at 10 mg/ml,ip administrated for 21 days	[PMID: 38838547]
A549	IC₅₀	4.21 μM Compound: BT	Antitumor activity against human A549 cells xenografted in mouse assessed as tumor growth inhibition at 5 mg/ml,ip administrated for 21 days Antitumor activity against human A549 cells xenografted in mouse assessed as tumor growth inhibition at 5 mg/ml,ip administrated for 21 days	[PMID: 38838547]
B16-F10	IC₅₀	>10000 nM Compound: 2a	Cytotoxicity against mouse B16F10 cells after 3 days by MTT assay Cytotoxicity against mouse B16F10 cells after 3 days by MTT assay	[PMID: 23706005]
CT26.WT	IC₅₀	>10000 nM Compound: 2a	Cytotoxicity against mouse CT26.WT cells after 3 days by MTT assay Cytotoxicity against mouse CT26.WT cells after 3 days by MTT assay	[PMID: 23706005]
HepG2	IC₅₀	0.5 μM Compound: 9	Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay	[PMID: 24050254]
HL-60	IC₅₀	<0.01 μg/mL Compound: 17	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 11575946]
Hs 683	IC₅₀	9 nM Compound: 2a	Cytotoxicity against human Hs683 cells after 3 days by MTT assay Cytotoxicity against human Hs683 cells after 3 days by MTT assay	[PMID: 23706005]
KB	IC₅₀	0.19 μg/mL Compound: 17	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	IC₅₀	37 nM Compound: 2a	Cytotoxicity against human MCF7 cells after 3 days by MTT assay Cytotoxicity against human MCF7 cells after 3 days by MTT assay	[PMID: 23706005]
MH60	IC₅₀	>25 μg/mL Compound: 17	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	>56.2 μM Compound: 7	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]
MH60	IC₅₀	>56.2 μM Compound: 7	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]
PC-3	IC₅₀	34 nM Compound: 2a	Cytotoxicity against human PC3 cells after 3 days by MTT assay Cytotoxicity against human PC3 cells after 3 days by MTT assay	[PMID: 23706005]
SK-MEL-28	IC₅₀	65 nM Compound: 2a	Cytotoxicity against human SK-MEL-28 cells after 3 days by MTT assay Cytotoxicity against human SK-MEL-28 cells after 3 days by MTT assay	[PMID: 23706005]
U-373MG ATCC	IC₅₀	74 nM Compound: 2a	Cytotoxicity against human U373 cells after 3 days by MTT assay Cytotoxicity against human U373 cells after 3 days by MTT assay	[PMID: 23706005]

In Vitro

Bufotalin (0.1-2.5 μM; 12-96 hours) treatment dose- and time-dependently inhibits MG-63 osteoblastoma cell survival^[1].
Bufotalin (0.5-2.5 μM; 48 hours) treatment dose-dependently increases the percentage of Annexin V positive cells (apoptotic cells) and caspase-12 activity in MG-63 cells. Bufotalin-induced osteoblastoma cell apoptosis is associated with caspase-12 activation^[1].
Bufotalin (0.5-2.5 μM; 12 hours) treatment dose-dependently induces C/EBP homologous protein (CHOP) expression as well as PERK and IRE1 phosphorylation in MG-63 cells. Bufotalin induces endoplasmic reticulum (ER) stress activation in cells^[1].
Bufotalin treatment induces cell cycle arrest at G2/M phase through down-regulation of Aurora A, CDC25, CDK1, cyclin A and cyclin B1, as well as up-regulation of p53 and p21 in HepG2 cells. Bufotalin treatment also induces apoptosis which was accompanied by decrease in mitochondrial membrane potential, increases in intracellular calcium level and reactive oxygen species production, activations of caspase-9 and -3, cleavage of poly ADP-ribose polymerase (PARP) as well as changes in the expressions of bcl-2 and bax^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:

MG-63 osteoblastoma cells
Concentration:

0.1 μM, 0.5 μM, 1 μM, 2.5 μM
Incubation Time:

12 hours, 24 hours, 48 hours, 72 hours, 96 hours
Result:

Inhibited MG-63 osteoblastoma cell survival.

Apoptosis Analysis^[1]

Cell Line:

MG-63 cells
Concentration:

0.5 μM, 1 μM, 2.5 μM
Incubation Time:

48 hours
Result:

Dose-dependently increased the percentage of Annexin V positive cells (apoptotic cells) and caspase-12 activity in MG-63 cells.

Western Blot Analysis^[1]

Cell Line:

MG-63 cells
Concentration:

0.5 μM, 1 μM, 2.5 μM
Incubation Time:

12 hours
Result:

Dose-dependently induced CHOP expression as well as PERK and IRE1 phosphorylation in MG-63 cells.

In Vivo

Bufotalin (0.5-1 mg/kg; intraperitoneal injection; twice daily; for 7 days) treatment shows a significantly reduced tumor growth in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

SCID male mice (4-6 weeks old) injected with U2OS cells^[1]
Dosage:

0.5 mg/kg, 1 mg/kg
Administration:

Intraperitoneal injection; twice daily; for 7 days
Result:

Inhibited U2OS osteoblastoma cell growth in mice.

Chemical Information

CAS No. 471-95-4
Appearance Solid
Molecular Weight 444.56
Formula C₂₆H₃₆O₆
Color White to off-white
SMILES

C[C@@]1(CC[C@@]2([H])[C@@]3([H])CC[C@@]4([H])[C@@]2(CC[C@H](O)C4)C)[C@@H](C(C=C5)=COC5=O)[C@@H](OC(C)=O)C[C@@]13O
Structure Classification
- Steroids
Initial Source
- Animals
toad
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

All Cell Proliferation/Viability AssayCell Imaging/StainingIFELISAWBIPHistological Imaging/StainingIn Vivo Efficacy Study

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Journal Impact Factor

Pharmacol Res

Small molecule targeting topoisomerase 3β for cancer therapy. [Abstract]

2021 Dec:174:105927. PMID: 34740818
Phytomedicine

Compound-composed Chinese medicine of Huachansu triggers apoptosis of gastric cancer cells through increase of reactive oxygen species levels and suppression of proteasome activities. [Abstract]

2024 Jan:123:155169. PMID: 37992493
Free Radic Biol Med

Bufotalin induces ferroptosis in non-small cell lung cancer cells by facilitating the ubiquitination and degradation of GPX4. [Abstract]

2022 Feb 20:180:75-84. PMID: 35038550

Bufotalin purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2022 Feb 20:180:75-84. [Abstract]

The cell viability of A549 cells treated by Bufotalin (BT) were examined by CCK-8 assay.

Bufotalin purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2022 Feb 20:180:75-84. [Abstract]

A549 cells were treated with different concentrations of Bufotalin (BT) (0, 1, 2, 4 μM), and colony formation was assessed by staining with crystal violet.

Bufotalin purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2022 Feb 20:180:75-84. [Abstract]

A549 cells were treated with different concentrations of Bufotalin (BT) (0, 1, 2, 4 μM) for 12 h, then the lipid ROS (C11-BODIPY 581/591 fluorescence staining) were assessed by fluorescence microscope.

Bufotalin purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2022 Feb 20:180:75-84. [Abstract]

4-HNE were measured by an ELISA assay treatment with different concentrations of Bufotalin (BT) (0, 1, 2, 4 μM).

Bufotalin purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2022 Feb 20:180:75-84. [Abstract]

The expression of GPX4 in A549 cells were measured by immunoblotting after treatment with different concentrations of Bufotalin (BT) (0, 1, 2, 4 μM) for 24 h.

Bufotalin purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2022 Feb 20:180:75-84. [Abstract]

A549 cells were treated with different concentrations of Bufotalin (BT) (0, 1, 2, 4 μM) for 24 h. The cell lysates were subjected to immunoprecipitation using a GPX4 antibody, and coprecipitating endogenous proteins were detected by immunoblotting.

Bufotalin purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2022 Feb 20:180:75-84. [Abstract]

Histopathology of xenograft tumors stained with GPX4 and Ki67 treated with Bufotalin (BT) (5 mg/kg and 10 mg/kg).

Bufotalin purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2022 Feb 20:180:75-84. [Abstract]

Changes of tumor volume, tumor weight, and body weight were showed after treated with Bufotalin (BT) (5 mg/kg and 10 mg/kg) in the xenograft model.
Microb Pathog

Bufotalin ameliorates ovalbumin-induced allergic rhinitis by restoring the Tregs. [Abstract]

2023 Jan:174:105918. PMID: 36455750

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (224.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2494 mL

11.2471 mL

22.4942 mL

5 mM

0.4499 mL

2.2494 mL

4.4988 mL

10 mM

0.2249 mL

1.1247 mL

2.2494 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.62 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 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.62 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
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)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Zhu YR, et al. Bufotalin-induced apoptosis in osteoblastoma cells is associated with endoplasmic reticulum stress activation. Biochem Biophys Res Commun. 2014 Aug 15;451(1):112-8. [Content Brief]

[2]. Zhang DM, et al. Bufotalin from Venenum Bufonis inhibits growth of multidrug resistant HepG2 cells through G2/M cell cycle arrest and apoptosis. Eur J Pharmacol. 2012 Oct 5;692(1-3):19-28. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2494 mL	11.2471 mL	22.4942 mL	56.2354 mL
	5 mM	0.4499 mL	2.2494 mL	4.4988 mL	11.2471 mL
	10 mM	0.2249 mL	1.1247 mL	2.2494 mL	5.6235 mL
	15 mM	0.1500 mL	0.7498 mL	1.4996 mL	3.7490 mL
	20 mM	0.1125 mL	0.5624 mL	1.1247 mL	2.8118 mL
	25 mM	0.0900 mL	0.4499 mL	0.8998 mL	2.2494 mL
	30 mM	0.0750 mL	0.3749 mL	0.7498 mL	1.8745 mL
	40 mM	0.0562 mL	0.2812 mL	0.5624 mL	1.4059 mL
	50 mM	0.0450 mL	0.2249 mL	0.4499 mL	1.1247 mL
	60 mM	0.0375 mL	0.1875 mL	0.3749 mL	0.9373 mL
	80 mM	0.0281 mL	0.1406 mL	0.2812 mL	0.7029 mL
	100 mM	0.0225 mL	0.1125 mL	0.2249 mL	0.5624 mL

Bioz

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Bufotalin

Bufalin

Cinobufagin

Resibufogenin

Convallatoxin

Delanzomib

Arenobufagin

Gamabufotalin

Periplogenin

Bruceine D

Alantolactone

Bufotalin (Standard)

AT-533

Publications Citing Use of MedChemExpress (MCE) Bufotalin

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

Bufotalin

Bufalin

Cinobufagin

Resibufogenin

Convallatoxin

Delanzomib

Arenobufagin

Gamabufotalin

Periplogenin

Bruceine D

Alantolactone

Bufotalin (Standard)

AT-533

Publications Citing Use of MedChemExpress (MCE) Bufotalin

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Bufotalin Related Classifications

HY-N0878 Related Classifications

Bioz