Cat. No.: HY-N0876

Arenobufagin

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

Arenobufagin is a natural bufadienolide that can be extracted from toad venom. Arenobufagin can induce apoptosis and autophagy in human hepatocellular carcinoma cells through inhibition of PI3K/Akt/mTOR pathway. Arenobufagin has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells. Arenobufagin can inhibit VEGF-mediated angiogenesis through suppression of VEGFR-2 signaling pathway.

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Pureté: 99.82%
CAS No.: 464-74-4
Formule: C₂₄H₃₂O₆
Masse moléculaire:416.51

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Arenobufagin Chemical Structure

CAS No.: 464-74-4

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	0.02 μM Compound: Arenobufagin	Antiproliferative activity against human HepG2 cells by MTT assay Antiproliferative activity against human HepG2 cells by MTT assay	[PMID: 30181060]
HepG2	IC₅₀	0.0001 μM Compound: Arenobufagin	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 30181060]
HepG2	IC₅₀	0.1 nM Compound: Arenobufagin	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	[PMID: 30181060]
HepG2/Adm	IC₅₀	0.056 μM Compound: Arenobufagin	Antiproliferative activity against human HepG2/ADM cells by MTT assay Antiproliferative activity against human HepG2/ADM cells by MTT assay	[PMID: 30181060]
MCF7	IC₅₀	8.88 nM Compound: Arenobufagin	Antiproliferative activity against FAP-alpha deficient human MCF7 cells incubated for 48 hrs by MTT assay Antiproliferative activity against FAP-alpha deficient human MCF7 cells incubated for 48 hrs by MTT assay	[PMID: 28595013]
MDA-MB-231	IC₅₀	15.67 nM Compound: Arenobufagin	Antiproliferative activity against FAP-alpha deficient human MDA-MB-231 cells incubated for 48 hrs by MTT assay Antiproliferative activity against FAP-alpha deficient human MDA-MB-231 cells incubated for 48 hrs by MTT assay	[PMID: 28595013]
MDA-MB-435	IC₅₀	22.45 nM Compound: Arenobufagin	Antiproliferative activity against wild type human MDA-MB-435 cells expressing FAP-alpha incubated for 48 hrs by MTT assay Antiproliferative activity against wild type human MDA-MB-435 cells expressing FAP-alpha incubated for 48 hrs by MTT assay	[PMID: 28595013]

In Vitro

Arenobufagin (10 nM-10 μM, 48-72 h) potently inhibits the growth of both HepG2 and HepG2/ADM cells in a dose- and time-dependent manner, with the IC₅₀ of 20.24 and 7.46 nM after 72 h^[1].
Arenobufagin (20-500 nM, 24 h) increases the percentage of apoptotic (annexin positive) cells in HCC cells^[1].
Arenobufagin (20-500 nM, 48 h) induces a specific cleavage of poly (ADP-ribose) polymerase (PARP) and a decrease in pro-caspase-9 and -3^[1].
Arenobufagin (20 nM, 0-24 h) induces autophagic cell death and a significant increase in LC3-II in HepG2/ADM cells^[1].
Arenobufagin (0-500 nM, 0-24 h) inhibits the activation of PI3K/Akt pathways in HCC cells^[1].
Arenobufagin (0-125 nM, 12-48 h) inhibits cell viability in a dose- and time-dependent manner in HUVECs^[2].
Arenobufagin (5-125 nM, 12-48 h) significantly suppresses VEGF-induced HUVECs viability in a dose- and time-dependent manner^[2].
Arenobufagin (0-50 nM, 6 h) inhibits VEGF-induced endothelial cell migration and invasion^[2].

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

Immunofluorescence^[1]

Cell Line:

Hepatoma carcinoma cells
Concentration:

20, 200, 500 nM
Incubation Time:

24 h
Result:

Depolarized mitochondrial membrane potential dose-dependently.

In Vivo

Arenobufagin (3-6 mg/kg, i.p., 28 d) inhibits growth of HepG2/ADM cells xenografts in nude mice^[1].
Arenobufagin (0-10 mg/kg, s.c., 21 d) inhibits VEGF-induced blood vessel formation in C57BL/6J mice^[2].

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

Animal Model:

Nude mice with HepG2/ADM xenografts^[1]
Dosage:

3 and 6 mg/kg
Administration:

Intraperitoneal injection (i.p.), 28 d
Result:

Significantly reduced the tumor volume.
Resulted in remarkable decrease in levels of proliferating cell nuclear antigen, PARP, total and phosphorylated mTOR as well as increase of LC3-II.
Decreased the degree of phposphorylation of mTOR at Ser²⁴⁴⁸.

Chemical Information

CAS No. 464-74-4
Appearance Solid
Masse moléculaire 416.51
Formule C₂₄H₃₂O₆
Color White to off-white
SMILES

C[C@]([C@@H](C(C=C1)=COC1=O)CC2)(C3=O)[C@]2([C@@](CC[C@@]4([H])[C@@]5(CC[C@H](O)C4)C)([H])[C@]5([H])[C@@H]3O)O
Structure Classification
- Steroids
Initial Source
- Animals
toad
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (4)

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Molecules

Arenobufagin Induces Apoptotic Cell Death in Human Non-Small-Cell Lung Cancer Cells via the Noxa-Related Pathway. [Abstract]

2017 Sep 11;22(9):1525. PMID: 28892004

Arenobufagin purchased from MedChemExpress. Usage Cited in: Molecules. 2017 Sep 11;22(9):1525. [Abstract]

A549 and NCI-H460 cells are treated with Arenobufagin at the indicated concentrations for 24 h, and protein extracts are subjected to Western blot assay with indicated antibodies;
Toxicon

Arenobufagin suppresses lung cancer cell growth by disrupting mitochondrial function and inducing relocalization of ATP synthase. [Abstract]

2026 Jun 15:276:109067. PMID: 41833738
Research Square Preprint

2023 Aug 11.
Evid Based Complement Alternat Med

Arenobufagin Promoted Oxidative Stress-Associated Mitochondrial Pathway Apoptosis in A549 Non-Small-Cell Lung Cancer Cell Line. [Abstract]

2020 Apr 22:2020:8909171. PMID: 32382311

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (240.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 10 mg/mL (24.01 mM; Need ultrasonic)

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

2.4009 mL

12.0045 mL

24.0090 mL

5 mM

0.4802 mL

2.4009 mL

4.8018 mL

10 mM

0.2401 mL

1.2005 mL

2.4009 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, 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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: ≥ 6.25 mg/mL (15.01 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (15.01 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (15.01 mM); Clear solution

This protocol yields a clear solution of ≥ 6.25 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 (62.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

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

Solubility: ≥ 1 mg/mL (2.40 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (10.0 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 5

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

Solubility: ≥ 1 mg/mL (2.40 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 6

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

Solubility: ≥ 1 mg/mL (2.40 mM); Clear solution

This protocol yields a clear solution of ≥ 1 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 EtOH stock solution (10.0 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
Instruction de manipulation (2659 KB)

Références

[1]. Zhang DM, et al. Arenobufagin, a natural bufadienolide from toad venom, induces apoptosis and autophagy in human hepatocellular carcinoma cells through inhibition of PI3K/Akt/mTOR pathway. Carcinogenesis. 2013 Jun;34(6):1331-42. [Content Brief]

[2]. Li M, et al. Arenobufagin, a bufadienolide compound from toad venom, inhibits VEGF-mediated angiogenesis through suppression of VEGFR-2 signaling pathway. Biochem Pharmacol. 2012 May 1;83(9):1251-60. [Content Brief]

[3]. Cruz Jdos S, et al. Arenobufagin, a compound in toad venom, blocks Na(+)-K+ pump current in cardiac myocytes. Eur J Pharmacol. 1993 Aug 3;239(1-3):223-6. [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, 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
Ethanol / DMSO	1 mM	2.4009 mL	12.0045 mL	24.0090 mL	60.0226 mL
	5 mM	0.4802 mL	2.4009 mL	4.8018 mL	12.0045 mL
	10 mM	0.2401 mL	1.2005 mL	2.4009 mL	6.0023 mL
	15 mM	0.1601 mL	0.8003 mL	1.6006 mL	4.0015 mL
	20 mM	0.1200 mL	0.6002 mL	1.2005 mL	3.0011 mL
DMSO	25 mM	0.0960 mL	0.4802 mL	0.9604 mL	2.4009 mL
	30 mM	0.0800 mL	0.4002 mL	0.8003 mL	2.0008 mL
	40 mM	0.0600 mL	0.3001 mL	0.6002 mL	1.5006 mL
	50 mM	0.0480 mL	0.2401 mL	0.4802 mL	1.2005 mL
	60 mM	0.0400 mL	0.2001 mL	0.4002 mL	1.0004 mL
	80 mM	0.0300 mL	0.1501 mL	0.3001 mL	0.7503 mL
	100 mM	0.0240 mL	0.1200 mL	0.2401 mL	0.6002 mL

Keywords

Arenobufagin

4 Cited Publications

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Arenobufagin

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Publications Citing Use of MedChemExpress (MCE) Arenobufagin

Voir tous les produits spécifiques à Isoform PI3K

Voir tous les produits spécifiques à Isoform Akt

Voir tous les produits spécifiques à Isoform mTOR

Voir tous les produits spécifiques à Isoform PARP

Voir tous les produits spécifiques à Isoform Caspase

Activité biologique

Chemical Information

Publications (4)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Arenobufagin Related Classifications

HY-N0876 Related Classifications