2. Apoptosis
  3. Apoptosis
  4. Cinobufagin

Cinobufagin  (Synonyms: Cinobufagine)

Cat. No.: HY-N0421 Purity: 99.84%
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Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models.

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

Cinobufagin Chemical Structure

Cinobufagin Chemical Structure

CAS No. : 470-37-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
1 mg USD 57 In-stock
5 mg USD 120 In-stock
10 mg USD 180 In-stock
50 mg USD 380 In-stock
100 mg USD 590 In-stock
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Based on 3 publication(s) in Google Scholar

Cinobufagin Related Antibodies

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Description

Cinobufagin is an anticancer agent that can be secreted by the Asiatic toad Bufo gargarizans. Cinobufagin induces the cell cycle arrests in the G1 phase or G2/M phase, leading to apoptosis in cancer cells. Cinobufagin inhibits tumor growth in melanoma and glioblastoma multiforme xenograft mouse models[1][2][3].

In Vitro

Conobufagin (30-300 nM, 7 days) exerts potent antitumor activity in a dose-dependent manner in uveal melanoma OCM1 cells[1].
Conobufagin (30-300 nM, 24 hours) arrests the cell cycle in the G1 phase in a concentrationdependent manner and induces cell apoptosis and alterations of apoptosis-related proteins in OCM1 cells[1].
Conobufagin (0.01-1 μM, 6 hours) blocks EGFR phosphorylation and induces cell apoptosis and cytotoxicity in glioblastoma multiforme U87MG-EGFR and U87MG-PTEN cells[2].
Cinobufagin (0.4,0.7,1.0 μM, 24-48 hours) induces cell cycle arrest at the G2/M phase and cell apoptosis, leading to inhibition of malignant melanoma A375/B16 cell proliferation[3].

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

Cinobufagin Related Antibodies

Cell Proliferation Assay[1]

Cell Line: OCM1 cell
Concentration: 30,100,300 nM
Incubation Time: 7 days
Result: Exerted potent cytotoxic in OCM1 cells with an IC50 of 8.023 nM.

Apoptosis Analysis[1]

Cell Line: OCM1 cell
Concentration: 30,100,300 nM
Incubation Time: 24 hours
Result: Induced cell apoptosis and upregulate the expression levels of cleaved caspase-3, cleaved poly(ADP-ribose) polymerase (PARP), and cleaved caspase-9.
Activated the intrinsic mitochondrial apoptosis pathway, which was demonstrated by increased cell apoptosis with increased expression of Bad and Bax, decreased expression of Bcl-2 and Bcl-xl, and reduced mitochondrial membrane potential (MMP).
In Vivo

Cinobufagin (5 mg/kg for i.p., once a day for 10 days) inhibits xenograft growth by inducing cell apoptosis in tumor xenograft mice model[1].
Cinobufagin (5 mg/kg for i.p., once a day for 10 days) suppresses tumor growth in both subcutaneous and intracranial U87MG-EGFR xenograft mouse models and increases the median survival of nude mice bearing intracranial U87MGEGFR tumors[2].

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

Animal Model: OCM1 cells tumor xenograft in Nu/Nu nude mice [1]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection (i.p.), once a day for 10 days
Result: Made the tumors grew more slowly than those treated with intraperitoneal injection of saline or untreated.
Increased the expression of caspase-3 and PARP in tumor tissues and decreased Bcl-2 and Bcl-xl expression in mouse tumor tissues and increased expression of Bad and Bax.
Animal Model: U87MG-EGFR subcutaneous and intracranial xenograft model[2]
Dosage: 5 mg/kg
Administration: Intraperitoneal injection (i.p.), once a day for 10 days
Result: Decreased the luminescence intensity of brain tumor about 70%.
Decreased p-EGFR, p-STAT3, and p-Akt levels in the intracranial tumors as compared with the vehicles.
Decreased Ki67 and active caspase-3 immunostaining of intracranial tumors.
Molecular Weight

442.54

Formula

C26H34O6
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@]([C@@H](C(C=C1)=COC1=O)[C@H]2OC(C)=O)(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 (225.97 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2597 mL 11.2984 mL 22.5968 mL
5 mM 0.4519 mL 2.2597 mL 4.5194 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.5 mg/mL (5.65 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.65 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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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
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: 99.84%

COA (252 KB) HNMR (298 KB) RP-HPLC (225 KB) LCMS (96 KB) Elemental Analysis Report (110 KB)

Handling Instructions (2659 KB)
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 2.2597 mL 11.2984 mL 22.5968 mL 56.4921 mL
5 mM 0.4519 mL 2.2597 mL 4.5194 mL 11.2984 mL
10 mM 0.2260 mL 1.1298 mL 2.2597 mL 5.6492 mL
15 mM 0.1506 mL 0.7532 mL 1.5065 mL 3.7661 mL
20 mM 0.1130 mL 0.5649 mL 1.1298 mL 2.8246 mL
25 mM 0.0904 mL 0.4519 mL 0.9039 mL 2.2597 mL
30 mM 0.0753 mL 0.3766 mL 0.7532 mL 1.8831 mL
40 mM 0.0565 mL 0.2825 mL 0.5649 mL 1.4123 mL
50 mM 0.0452 mL 0.2260 mL 0.4519 mL 1.1298 mL
60 mM 0.0377 mL 0.1883 mL 0.3766 mL 0.9415 mL
80 mM 0.0282 mL 0.1412 mL 0.2825 mL 0.7062 mL
100 mM 0.0226 mL 0.1130 mL 0.2260 mL 0.5649 mL
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Cinobufagin 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.

Keywords:

Cinobufagin470-37-1CinobufagineApoptosisUveal melanomaOCM1anticancer agentMalignant MelanomaGlioblastoma multiformeInhibitorinhibitorinhibit

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