Arenobufagin

Name: Arenobufagin
Brand: MedChemExpress
SKU: HY-N0876
Rating: 5.0 (4 reviews)

Cat. No.: HY-N0876 Purity: 99.86%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Arenobufagin is a natural bufadienolide from toad venom; has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells.

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

Arenobufagin Chemical Structure

CAS No. : 464-74-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 165	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 165	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 4 publication(s) in Google Scholar

3 Publications Citing Use of MCE Arenobufagin

: Arenobufagin purchased from MedChemExpress. Usage Cited in: Molecules. 2017 Sep 11;22(9). pii: E1525. [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;

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Biological Activity
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References
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Description

Arenobufagin is a natural bufadienolide from toad venom; has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells. IC50 value: Target: in vitro: arenobufagin induced mitochondria-mediated apoptosis in HCC cells, with decreasing mitochondrial potential, as well as increasing Bax/Bcl-2 expression ratio, Bax translocation from cytosol to mitochondria. Arenobufagin also induced autophagy in HepG2/ADM cells. Autophagy-specific inhibitors (3-methyladenine, chloroquine and bafilomycin A1) or Beclin1 and Atg 5 small interfering RNAs (siRNAs) enhanced arenobufagin-induced apoptosis, indicating that arenobufagin-mediated autophagy may protect HepG2/ADM cells from undergoing apoptotic cell death [1]. arenobufagin inhibited vascular endothelial growth factor (VEGF)-induced viability, migration, invasion and tube formation in human umbilical vein endothelial cells (HUVECs) in vitro [2]. Arenobufagin blocked the Na+/K+ pump current in a dose-dependent manner with a half-maximal concentration of 0.29 microM and a Hill coefficient of 1.1 [3]. in vivo: arenobufagin inhibited the growth of HepG2/ADM xenograft tumors, which were associated with poly (ADP-ribose) polymerase cleavage, light chain 3-II activation and mTOR inhibition [1]. Arenobufagin also suppressed sprouting formation from VEGF-treated aortic rings in an ex vivo model [2].

Cellular Effect

Cell Line	Type	Value	Description	References
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	0.02 μM Compound: Arenobufagin	Antiproliferative activity against human HepG2 cells by MTT assay Antiproliferative activity against human HepG2 cells by MTT assay	[PMID: 30181060]
HepG2/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]

Molecular Weight

416.51

Formula

C₂₄H₃₂O₆

CAS No.

464-74-4

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.86%

Select Batch:

Data Sheet (280 KB) SDS (251 KB)

COA (255 KB) HNMR (246 KB) CNMR (208 KB) RP-HPLC (291 KB) MS (629 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

Arenobufagin Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Arenobufagin464-74-4OthersInhibitorinhibitorinhibit

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Arenobufagin

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Arenobufagin Related Antibodies

3 Publications Citing Use of MCE Arenobufagin

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Complete Stock Solution Preparation Table

Arenobufagin Related Classifications

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