Resibufogenin
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.93%
- No. CAS: 465-39-4
- Fòrmula: C24H32O4
- Peso molecular:384.51
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Resibufogenin
More- Pharmacol Res. 2021 Dec:174:105927. [Abstract]
- Environ Int. 2024 Apr:186:108582. [Abstract]
- Int Immunopharmacol. 2023 Jul:120:110291. [Abstract]
- Front Pharmacol. 2022 May 17;13:855626. [Abstract]
- Sci Rep. 2025 Aug 16;15(1):30005. [Abstract]
- Anat Rec. 2021 Feb;304(2):302-312. [Abstract]
- Am J Transl Res. 2019 Oct 15;11(10):6290-6303. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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WB
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Flow Cytometry
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Cell Migration/Invasion Assay
Ver todos los productos específicos de isoformas AP-1
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Actividad biológica
Descripciòn
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GSK-3β |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>100 μM
Compound: 6
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Cytotoxicity against human A549 cells after 24 hrs by MTT assay
Cytotoxicity against human A549 cells after 24 hrs by MTT assay
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[PMID: 24050254] |
| BGC-823 | IC50 |
7.89 μM
Compound: 1, resibufogenin
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Cytotoxicity against human BGC823 cells
Cytotoxicity against human BGC823 cells
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[PMID: 17911017] |
| BGC-823 | IC50 |
7.89 μM/L
Compound: 1, resibufogenin
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Cytotoxicity against human BGC823 cells
Cytotoxicity against human BGC823 cells
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[PMID: 17911017] |
| HeLa | IC50 |
>50 μM
Compound: 1, resibufogenin
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Cytotoxicity against human HeLa cells
Cytotoxicity against human HeLa cells
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[PMID: 17911017] |
| HeLa | IC50 |
>50 μM/L
Compound: 1, resibufogenin
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Cytotoxicity against human HeLa cells
Cytotoxicity against human HeLa cells
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[PMID: 17911017] |
| HepG2 | IC50 |
>50 μM
Compound: 1, resibufogenin
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Cytotoxicity against human HepG2 cells
Cytotoxicity against human HepG2 cells
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[PMID: 17911017] |
| HepG2 | IC50 |
>50 μM/L
Compound: 1, resibufogenin
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Cytotoxicity against human HepG2 cells
Cytotoxicity against human HepG2 cells
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[PMID: 17911017] |
| HepG2 | IC50 |
43.3 μM
Compound: 6
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Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay
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[PMID: 24050254] |
| HL-60 | IC50 |
0.5 μg/mL
Compound: 11
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Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
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[PMID: 11575946] |
| KB | IC50 |
1.3 μg/mL
Compound: 11
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Cytotoxicity against human KB cells after 72 hrs by MTT assay
Cytotoxicity against human KB cells after 72 hrs by MTT assay
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[PMID: 11575946] |
| KB | IC50 |
1.34 μg/mL
Compound: 6
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Cytotoxicity against human KB cells after 72 hrs by MTT assay
Cytotoxicity against human KB cells after 72 hrs by MTT assay
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[PMID: 12141860] |
| MH60 | IC50 |
10 μg/mL
Compound: 11
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Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay
Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay
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[PMID: 11575946] |
| MH60 | IC50 |
10.48 μg/mL
Compound: 6
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Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay
Cytotoxicity against mouse MH60 cells after 72 hrs by MTT assay
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[PMID: 12141860] |
| MH60 | IC50 |
>65.1 μM
Compound: 4
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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
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[PMID: 15620253] |
| MH60 | IC50 |
22.9 μM
Compound: 4
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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
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[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.
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Cell Line:RPMI8226
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Concentration:2 µM, 4 µM, 8 µM
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Incubation Time:12, 24, 48 h
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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 (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.
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Animal Model:BALB/c-nu/nu mice (female, 18-22 g, 2-month-old) with Aspc xenograft[8]
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Dosage:10 mg/kg, 20 mg/kg
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Administration:Intragastric injection, every day, 20 days
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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
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No. CAS 465-39-4
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Appearance Solid
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Peso molecular 384.51
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Fòrmula C24H32O4
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Color White to off-white
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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
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Synonyms
Bufogenin; Recibufogenin
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Structure Classification
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Initial Source
toad
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Pharmacol Res
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 -
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 -
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.
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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
Solvente y solubilidad
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.
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.
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.
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (285 KB)
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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)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
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 |
Resibufogenin Related Classifications
HY-N0815 Related Classifications
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