1. PI3K/Akt/mTOR NF-κB Immunology/Inflammation Stem Cell/Wnt Cell Cycle/DNA Damage
  2. PI3K Akt NF-κB AP-1 GSK-3 CDK
  3. Resibufogenin

Resibufogenin  (Synonyms: Bufogenin; Recibufogenin)

Cat. No.: HY-N0815 Purity: 99.93%
Handling Instructions Technical Support

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.

Resibufogenin Chemical Structure

Resibufogenin Chemical Structure

CAS No. : 465-39-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Resibufogenin:

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3][4][5][6][7][8][9].

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

GSK-3β

 

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]
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
> 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
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
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.
Molecular Weight

384.51

Formula

C24H32O4

CAS No.
Appearance

Solid

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

Structure Classification
Initial Source

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
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6007 mL 13.0036 mL 26.0071 mL
5 mM 0.5201 mL 2.6007 mL 5.2014 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, 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

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 2.75 mg/mL (7.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (7.15 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

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Animal weight
(per animal)

g

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: 99.93%

References

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, 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
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  • 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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