Cat. No.: HY-N0883

Gamabufotalin

(Synonyms: Gamabufagin)

4 Cited Publications

Customer Review

Based on 4 publication(s) in Google Scholar

Gamabufotalin (Gamabufagin), a main active compound isolated from Chinese medicine Chansu, has been shown to strongly inhibit cancer cell growth and inflammatory response. Gamabufotalin could inhibite angiogenesis by inhibiting the activation of VEGFR-2 signaling pathways.

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

Purity: 99.30%
CAS No.: 465-11-2
Formula: C₂₄H₃₄O₅
Molecular Weight:402.52

Storage:

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

Gamabufotalin Chemical Structure

CAS No.: 465-11-2

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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

All VEGFR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Hep 3B2	IC₅₀	27 nM Compound: CS-6	Antiproliferative activity against human Hep3B cells assessed as cell viability incubated for 24 hrs by CCK-8 Antiproliferative activity against human Hep3B cells assessed as cell viability incubated for 24 hrs by CCK-8	[PMID: 37043698]
HL-60	IC₅₀	0.014 μg/mL Compound: 20	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 11575946]
Huh-7	IC₅₀	23 nM Compound: CS-6	Antiproliferative activity against human Huh-7 cells assessed as cell viability incubated for 24 hrs by CCK-8 Antiproliferative activity against human Huh-7 cells assessed as cell viability incubated for 24 hrs by CCK-8	[PMID: 37043698]
KB	IC₅₀	0.75 μg/mL Compound: 20	Cytotoxicity against human KB cells after 72 hrs by MTT assay Cytotoxicity against human KB cells after 72 hrs by MTT assay	[PMID: 11575946]
MH60	IC₅₀	>25 μg/mL Compound: 20	Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay	[PMID: 11575946]

In Vitro

Gamabufotalin (0-500 nM, 48 h) inhibits cell viability of human lung cancer A549, H1299, H322 cells, and inhibits colony formation and migration (0-100 nM, 48 h), with no cytotoxicity in human normal lung cell line (HLF cells)^[1].
Gamabufotalin (0-100 nM, 12-48 h) inhibits COX-2 expression and inhibits NF-κB and p300 translocation in A549 cells^[1].
Gamabufotalin (0-100 nM, 12-48 h) induces apoptosis by activating the cytochrome c release and caspase-dependent apoptotic pathway in A549 cells^[1].
Gamabufotalin (0-100 nM, 48 h) induces hyperphosphorylation of p38, increases the expression of ATP1A3 and decreases AQP4 expression in U87 cells^[3].
Gamabufotalin (0-50 nM, 24 h) inhibits VEGF (50 ng/mL)-induced angiogenesis in an HUVECs in vitro angiogenesis tube formation assay^[4].

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

Apoptosis Analysis^[1]

Cell Line:

A549 cells
Concentration:

0-100 nM
Incubation Time:

12-48 h
Result:

Increase the expression levels of the cleaved caspase-3, caspase-9 and PARP.
Induced the release of cyt c from mitochondria to cytosol.

Immunofluorescence^[1]

Cell Line:

A549 cells
Concentration:

0-100 nM
Incubation Time:

12-48 h
Result:

Inhibited translocation of the NF-κB p65/p50 proteins from cell cytoplasm to nucleus, and induced p300 into the cytoplasm.

In Vivo

Gamabufotalin (5 and 20 mg/kg/day, i.p., for 17 days) inhibits tumor growth in the A549-xenografts mice^[1].
Gamabufotalin (1 mg/kg, i.p., three times per week) together with Temozolomide (HY-17364) (20 mg/kg. i.p., three times per week) shows a synergistic antitumor effect, and inhibits tumor growth and prolongs mice survival in mice U87 xenografts^[3].

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

Animal Model:

A549-xenografts mice^[1]
Dosage:

5 and 20 mg/kg/day
Administration:

i.p., for 17 days
Result:

Reduced tumor volume and the tumor weights.
Decreased COX-2 and p-p65 level in tumors.

Chemical Information

CAS No. 465-11-2
Appearance Solid
Molecular Weight 402.52
Formula C₂₄H₃₄O₅
Color White to off-white
SMILES

C[C@]([C@@H](C(C=C1)=COC1=O)CC2)(C[C@@H](O)[C@@]3([H])[C@@]4([H])CC[C@@]5([H])[C@@]3(CC[C@H](O)C5)C)[C@]24O
Synonyms

Gamabufagin
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 AssayWBIF

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Journal Impact Factor

Nat Microbiol

Fluorogenic reporter enables identification of compounds that inhibit SARS-CoV-2. [Abstract]

2023 Jan;8(1):121-134. PMID: 36604514
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
Front Pharmacol

Gamabufotalin Inhibits Osteoclastgenesis and Counteracts Estrogen-Deficient Bone Loss in Mice by Suppressing RANKL-Induced NF-κB and ERK/MAPK Pathways. [Abstract]

2021 Apr 23:12:629968. PMID: 33967763
J Nat Prod

Gamabufotalin Induces Apoptosis and Cytoprotective Autophagy through the mTOR Signaling Pathway in Hepatocellular Carcinoma. [Abstract]

2023 Apr 28;86(4):966-978. PMID: 37043698

Gamabufotalin purchased from MedChemExpress. Usage Cited in: J Nat Prod. 2023 Apr 28;86(4):966-978. [Abstract]

Gamabufotalin (CS-6; 10-1000 nM; 48 h) reduces the viability of Hep3B and Huh7 cells in a dose-dependent manner.

Gamabufotalin purchased from MedChemExpress. Usage Cited in: J Nat Prod. 2023 Apr 28;86(4):966-978. [Abstract]

Gamabufotalin (CS-6; 15, 20, 25 nM; 48 h) inhibits the proliferation of Hep3B and Huh7 cells in a dose-dependent manner.

Gamabufotalin purchased from MedChemExpress. Usage Cited in: J Nat Prod. 2023 Apr 28;86(4):966-978. [Abstract]

Gamabufotalin (CS-6; 15, 20, 25 nM; 48 h) significantly increases the expression of cleaved PARP/PARP, caspase-3/caspase-3, and Bax and decreases the expression of Bcl-2 in Hep3B cells.

Gamabufotalin purchased from MedChemExpress. Usage Cited in: J Nat Prod. 2023 Apr 28;86(4):966-978. [Abstract]

Gamabufotalin (CS-6; 25 nM; 15 min) significantly increases the formation of yellow-spotted autophagosomes (GFP+RFP+) and red-spotted autolysosomes (GFP-RFP+) in Hep3B and Huh7 cells.

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (124.22 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

2.4843 mL

12.4217 mL

24.8435 mL

5 mM

0.4969 mL

2.4843 mL

4.9687 mL

10 mM

0.2484 mL

1.2422 mL

2.4843 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)

Volume _(final) Volume _(final)

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 (6.21 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 (6.21 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 (6.21 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 (284 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Yu Z, et al. Gamabufotalin, a bufadienolide compound from toad venom, suppresses COX-2 expression through targeting IKKβ/NF-κB signaling pathway in lung cancer cells. Mol Cancer. 2014 Aug 31;13:203. [Content Brief]

[2]. Dong Y, et al. Bufadienolide compounds sensitize human breast cancer cells to TRAIL-induced apoptosis via inhibition of STAT3/Mcl-1 pathway. Apoptosis. 2011 Apr;16(4):394-403. [Content Brief]

[3]. Lan YL, et al. Gamabufotalin induces a negative feedback loop connecting ATP1A3 expression and the AQP4 pathway to promote temozolomide sensitivity in glioblastoma cells by targeting the amino acid Thr794. Cell Prolif. 2020;53(1):e12732. [Content Brief]

[4]. Tang N, et al. Gamabufotalin, a major derivative of bufadienolide, inhibits VEGF-induced angiogenesis by suppressing VEGFR-2 signaling pathway. Oncotarget. 2016;7(3):3533-3547. [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	2.4843 mL	12.4217 mL	24.8435 mL	62.1087 mL
	5 mM	0.4969 mL	2.4843 mL	4.9687 mL	12.4217 mL
	10 mM	0.2484 mL	1.2422 mL	2.4843 mL	6.2109 mL
	15 mM	0.1656 mL	0.8281 mL	1.6562 mL	4.1406 mL
	20 mM	0.1242 mL	0.6211 mL	1.2422 mL	3.1054 mL
	25 mM	0.0994 mL	0.4969 mL	0.9937 mL	2.4843 mL
	30 mM	0.0828 mL	0.4141 mL	0.8281 mL	2.0703 mL
	40 mM	0.0621 mL	0.3105 mL	0.6211 mL	1.5527 mL
	50 mM	0.0497 mL	0.2484 mL	0.4969 mL	1.2422 mL
	60 mM	0.0414 mL	0.2070 mL	0.4141 mL	1.0351 mL
	80 mM	0.0311 mL	0.1553 mL	0.3105 mL	0.7764 mL
	100 mM	0.0248 mL	0.1242 mL	0.2484 mL	0.6211 mL

Keywords

Gamabufotalin

4 Cited Publications

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Gamabufotalin

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Publications Citing Use of MedChemExpress (MCE) Gamabufotalin

All VEGFR Isoforms

Biological Activity

Chemical Information

Publications (4)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Gamabufotalin Related Classifications

HY-N0883 Related Classifications