Cat. No.: HY-N0815

Resibufogenin

(Synonyms: Bufogenin; Recibufogenin)

7 Cited Publications

Customer Review

Based on 7 publication(s) in Google Scholar

Resibufogenin is an orally active anticancer agent. Resibufogenin can be extracted from toad venom. Resibufogenin blocks signaling pathways such as PI3K/Akt, NF-κB, AP-1, activates GSK-3β, and regulates cyclin D1. Resibufogenin can activate central neurons. Resibufogenin has anti-inflammatory activity. Resibufogenin has anti-tumor effects on a variety of tumors such as multiple myeloma, renal cancer, colorectal cancer, pancreatic cancer, and glioma.

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

Purity: 99.93%
CAS No.: 465-39-4
Formula: C₂₄H₃₂O₄
Molecular Weight:384.51

Storage:

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

Resibufogenin Chemical Structure

CAS No.: 465-39-4

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (7)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]^[2]^[3]^[4]^[5]^[6]^[7]^[8]^[9]

GSK-3β

All PI3K Isoforms :

All Akt Isoforms :

All NF-κB Isoforms :

All AP-1 Isoforms :

All GSK-3 Isoforms :

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	>100 μM Compound: 6	Cytotoxicity against human A549 cells after 24 hrs by MTT assay Cytotoxicity against human A549 cells after 24 hrs by MTT assay	[PMID: 24050254]
BGC-823	IC₅₀	7.89 μM Compound: 1, resibufogenin	Cytotoxicity against human BGC823 cells Cytotoxicity against human BGC823 cells	[PMID: 17911017]
BGC-823	IC₅₀	7.89 μM/L Compound: 1, resibufogenin	Cytotoxicity against human BGC823 cells Cytotoxicity against human BGC823 cells	[PMID: 17911017]
HeLa	IC₅₀	>50 μM Compound: 1, resibufogenin	Cytotoxicity against human HeLa cells Cytotoxicity against human HeLa cells	[PMID: 17911017]
HeLa	IC₅₀	>50 μM/L Compound: 1, resibufogenin	Cytotoxicity against human HeLa cells Cytotoxicity against human HeLa cells	[PMID: 17911017]
HepG2	IC₅₀	>50 μM Compound: 1, resibufogenin	Cytotoxicity against human HepG2 cells Cytotoxicity against human HepG2 cells	[PMID: 17911017]
HepG2	IC₅₀	>50 μM/L Compound: 1, resibufogenin	Cytotoxicity against human HepG2 cells Cytotoxicity against human HepG2 cells	[PMID: 17911017]
HepG2	IC₅₀	43.3 μM Compound: 6	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	0.5 μg/mL Compound: 11	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 11575946]
KB	IC₅₀	1.3 μg/mL Compound: 11	Cytotoxicity against human KB cells after 72 hrs by MTT assay Cytotoxicity against human KB cells after 72 hrs by MTT assay	[PMID: 11575946]
KB	IC₅₀	1.34 μg/mL Compound: 6	Cytotoxicity against human KB cells after 72 hrs by MTT assay Cytotoxicity against human KB cells after 72 hrs by MTT assay	[PMID: 12141860]
MH60	IC₅₀	10 μg/mL Compound: 11	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	10.48 μg/mL Compound: 6	Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay	[PMID: 12141860]
MH60	IC₅₀	>65.1 μM Compound: 4	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	22.9 μM Compound: 4	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]

In Vitro

Resibufogenin (2-8 µM; 12-48 h) inhibits RPMI8226 cell viability in a dose- and time-dependent manner, with an IC₅₀ value of 7.694 µM at 48 h^[1].
Resibufogenin (10 mM) irreversibly activates mitral cells (MCs) in mouse main olfactory bulb (MOB) slices, evoking a lasting increase in depolarization and firing rate, and some cells die^[2].
Resibufogenin (10-200 nM; 12 h) inhibits the growth activity of Caki-1 cells in a dose-dependent manner, with an IC₅₀ value of 408.2 nM^[3].
Resibufogenin (0.1-10 μM; 24-48 h) decreases the cell viability of HCT116 cells dose-dependently^[4].
Resibufogenin (20 μM; 12 h) inhibits the migration of ES-2 and TOV-21G OCCC cells^[5].
Resibufogenin (2-5 μM; 1-3 days) inhibits the growth of human colon cancer HT-29 cells and induces G1-phase arrest in HT-29 cells^[6].
Resibufogenin (20-80 μM; 1 h) suppresses LPS-induced inflammation via inhibiting NF-κB and AP-1 pathways in RAW264.7 cells^[7].
Resibufogenin (1-10 μM; 24-72 h) inhibits the viability of human pancreatic cancer cells Panc-1 and Aspc^[8].

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

Western Blot Analysis^[1]

Cell Line:

RPMI8226
Concentration:

2 µM, 4 µM, 8 µM
Incubation Time:

12, 24, 48 h
Result:

Upregulated E-cadherin, downregulated N-cadherin and Vimentin, and reduced the protein expression of p-AKT and p-PI3K in a dose-dependent manner.
Did not alter the expression of AKT and PI3K.

In Vivo

Resibufogenin (20 mg/kg; i.p.; daily; 21 days) suppresses the growth of TOV-21G cell tumor xenografts in nude mice, as indicated by a significant decrease in tumor volumes and changes in the expression of Ki-67^[5].
Resibufogenin (5-20 mg/kg; i.p.; 30 min before LPS challenge) ameliorates endotoxemia in ICR mice, as indicated by a significant decrease in serum TNF-α, IL-6 and MCP-1 levels^[7].
Resibufogenin (10-20 mg/kg; i.g.; every day; 20 days) suppresses human pancreatic tumor xenograft growth in athymic nude mice without causing systemic toxicity^[8].
Resibufogenin (10 mg/kg/day; i.p.; daily) exerts antitumor effects in BALB/c nude mice with orthotopic P3#GBM tumor xenografts, prolonging the median survival of tumor-bearing mice and suppressing tumor proliferation^[9].

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

Animal Model:

BALB/c-nu/nu mice (female, 18-22 g, 2-month-old) with Aspc xenograft^[8]
Dosage:

10 mg/kg, 20 mg/kg
Administration:

Intragastric injection, every day, 20 days
Result:

Significantly inhibited the growth of Aspc tumor xenografts.
Showed mean tumor masses of 0.39 g and 0.21 g at 10 mg/kg and 20 mg/kg, respectively.
Increased the phosphorylation levels of PKCα/β and GSK-3β, decreased the phosphorylation level of p65 in tumors.
Did not remarkably alter organ indexes, suggesting no systemic toxicity.

Chemical Information

CAS No. 465-39-4
Appearance Solid
Molecular Weight 384.51
Formula C₂₄H₃₂O₄
Color White to off-white
SMILES

C[C@]([C@@H](C(C=C1)=COC1=O)C2)(CC[C@@]3([H])[C@@]4([H])CC[C@@]5([H])[C@@]3(CC[C@H](O)C5)C)[C@@]64[C@@H]2O6
Synonyms

Bufogenin; Recibufogenin
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 (7)

All Cell Proliferation/Viability AssayCell Imaging/StainingWBFlow CytometryCell Migration/Invasion Assay

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Journal Impact Factor

Pharmacol Res

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

2021 Dec:174:105927. PMID: 34740818
Environ Int

Evidence of promoting effects of 6:2 Cl-PFESA on hepatocellular carcinoma proliferation in humans: An ideal alternative for PFOS in terms of environmental health?. [Abstract]

2024 Apr:186:108582. PMID: 38513556
Front Pharmacol

Resibufogenin Targets the ATP1A1 Signaling Cascade to Induce G2/M Phase Arrest and Inhibit Invasion in Glioma. [Abstract]

2022 May 17;13:855626. PMID: 35656311

Resibufogenin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2022 May 17;13:855626. [Abstract]

Using the CCK-8 assay, proliferation curves of P3#GBM, U251 and A172 GBM cells treated with vehicle, DMSO (0), 2 μM or 4 μM Resibufogenin (RB) for 0, 24, 48 or 72 h.

Resibufogenin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2022 May 17;13:855626. [Abstract]

EdU assays conducted on U251 and A172 cells treated with vehicle, DMSO (0) and 2 or 4 μM Resibufogenin (RB) for 48 h.

Resibufogenin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2022 May 17;13:855626. [Abstract]

Western blot analysis of MMP2 and EMT-related proteins after 4 μM Resibufogenin (RB) treatment for 48 h.

Resibufogenin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2022 May 17;13:855626. [Abstract]

Intracellular Ca2⁺ was measured by Fluo-4/AM with flow cytometry treated with 4 μM Resibufogenin (RB).

Resibufogenin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2022 May 17;13:855626. [Abstract]

Resibufogenin (RB) (2, 4 μM) inhibits the invasion of GBM cells by transwell invasion assays.
Int Immunopharmacol

Cisatracurium besylate rescues Mycobacterium Tuberculosis-infected macrophages from necroptosis and enhances the bactericidal effect of isoniazid. [Abstract]

2023 Jul:120:110291. PMID: 37182451
Sci Rep

UPLC-Q-TOF/MS, network pharmacology, molecular docking, and experimental validation to explore the mechanisms of toad clothing on rheumatoid arthritis. [Abstract]

2025 Aug 16;15(1):30005. PMID: 40819108
Anat Rec

Resibufogenin suppresses growth and metastasis through inducing caspase-1-dependent pyroptosis via ROS-mediated NF-κB suppression in non-small cell lung cancer. [Abstract]

2021 Feb;304(2):302-312. PMID: 32396707
Am J Transl Res

Resibufogenin inhibits ovarian clear cell carcinoma (OCCC) growth in vivo, and migration of OCCC cells in vitro, by down-regulating the PI3K/AKT and actin cytoskeleton signaling pathways. [Abstract]

2019 Oct 15;11(10):6290-6303. PMID: 31737183

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (260.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.6007 mL

13.0036 mL

26.0071 mL

5 mM

0.5201 mL

2.6007 mL

5.2014 mL

10 mM

0.2601 mL

1.3004 mL

2.6007 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)

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Volume _(start) Volume _(start)

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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 (6.50 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 (6.50 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 (6.50 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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 (285 KB)
SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Portuguese - PT (479 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]. Zhou Y, et al. Resibufogenin inhibits the malignant characteristics of multiple myeloma cells by blocking the PI3K/Akt signaling pathway. Exp Ther Med. 2022 May 13;24(1):441. [Content Brief]

[2]. Wang ZJ, et al. Resibufogenin and cinobufagin activate central neurons through an ouabain-like action. PLoS One. 2014 Nov 24;9(11):e113272. [Content Brief]

[3]. Wu Y, et al. Effectiveness and Mechanism of Resibufogenin on Human Renal Cancer Cell Caki-1. Biology (Basel). 2024 Dec 19;13(12):1064. [Content Brief]

[4]. Han Q, et al. Resibufogenin suppresses colorectal cancer growth and metastasis through RIP3-mediated necroptosis. J Transl Med. 2018 Jul 20;16(1):201. [Content Brief]

[5]. Zhou G, et al. Resibufogenin inhibits ovarian clear cell carcinoma (OCCC) growth in vivo, and migration of OCCC cells in vitro, by down-regulating the PI3K/AKT and actin cytoskeleton signaling pathways. Am J Transl Res. 2019 Oct 15;11(10):6290-6303. [Content Brief]

[6]. Ichikawa M, et al. Resibufogenin Induces G1-Phase Arrest through the Proteasomal Degradation of Cyclin D1 in Human Malignant Tumor Cells. PLoS One. 2015 Jun 29;10(6):e0129851. [Content Brief]

[7]. Gao Y, et al. Resibufogenin, one of bufadienolides in toad venom, suppresses LPS-induced inflammation via inhibiting NF-κB and AP-1 pathways. Int Immunopharmacol. 2022 Dec;113(Pt A):109312. [Content Brief]

[8]. Liu L, et al. Resibufogenin suppresses transforming growth factor-β-activated kinase 1-mediated nuclear factor-κB activity through protein kinase C-dependent inhibition of glycogen synthase kinase 3. Cancer Sci. 2018 Nov;109(11):3611-3622. [Content Brief]

[9]. Zhang X, et al. Resibufogenin Targets the ATP1A1 Signaling Cascade to Induce G2/M Phase Arrest and Inhibit Invasion in Glioma. Front Pharmacol. 2022 May 17;13:855626. [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	2.6007 mL	13.0036 mL	26.0071 mL	65.0178 mL
	5 mM	0.5201 mL	2.6007 mL	5.2014 mL	13.0036 mL
	10 mM	0.2601 mL	1.3004 mL	2.6007 mL	6.5018 mL
	15 mM	0.1734 mL	0.8669 mL	1.7338 mL	4.3345 mL
	20 mM	0.1300 mL	0.6502 mL	1.3004 mL	3.2509 mL
	25 mM	0.1040 mL	0.5201 mL	1.0403 mL	2.6007 mL
	30 mM	0.0867 mL	0.4335 mL	0.8669 mL	2.1673 mL
	40 mM	0.0650 mL	0.3251 mL	0.6502 mL	1.6254 mL
	50 mM	0.0520 mL	0.2601 mL	0.5201 mL	1.3004 mL
	60 mM	0.0433 mL	0.2167 mL	0.4335 mL	1.0836 mL
	80 mM	0.0325 mL	0.1625 mL	0.3251 mL	0.8127 mL
	100 mM	0.0260 mL	0.1300 mL	0.2601 mL	0.6502 mL

Keywords

Resibufogenin

7 Cited Publications

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Resibufogenin

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Publications Citing Use of MedChemExpress (MCE) Resibufogenin

All PI3K Isoforms

All Akt Isoforms

All NF-κB Isoforms

All AP-1 Isoforms

All GSK-3 Isoforms

All CDK Isoforms

Biological Activity