Cinobufagin (Synonyms: Cinobufagine)

Name: Cinobufagin
Brand: MedChemExpress
SKU: HY-N0421
Rating: 5.0 (9 reviews)

Cat. No.: HY-N0421 Purity: 99.69%: Data Sheet
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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.

CAS No. : 470-37-1

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

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Customer Review

Based on 9 publication(s) in Google Scholar

Other Forms of Cinobufagin:

Cinobufagine-d₃ Get quote
Cinobufagin (Standard) Get quote

9 Publications Citing Use of MCE Cinobufagin

Cell Imaging/Staining

In Vivo Imaging

Flow Cytometry

: Cinobufagin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Feb 3;44(1):35. [Abstract]; Propidium iodide (PI) staining showing the death of G003 and G007 cells treated with Cinobufagin (CB), pyroptosis inhibitor (Belnacasan), apoptosis inhibitor (V-ZAD-FMK), and necroptosis inhibitor (Necrostatin) for 24 h.

: Cinobufagin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Feb 3;44(1):35. [Abstract]; Western blot (WB) analysis of PANoptosis markers (CASP3/7, c-CASP3/7, GSDMD, GSDME, MLKL, and p-MLKL) in GBM cell lines and primary GBM cells treated with Cinobufagin.

: Cinobufagin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Feb 3;44(1):35. [Abstract]; In vivo imaging on day 15 postimplantation for GL261 and CT2A tumors treated with Cinobufagin (5 mg/kg, i.p.).

: Cinobufagin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Feb 3;44(1):35. [Abstract]; Immunofluorescence (IF) showing infiltration of CD45⁺, CD4⁺, CD8⁺, and IBA1⁺ cells in CT2A tumors treated with Cinobufagin.

: Cinobufagin purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Feb 3;44(1):35. [Abstract]; Flow cytometry of CD45⁺ cells in GL261 tumors treated with Cinobufagin (5 mg/kg, i.p.).

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Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	2.3 μM Compound: 12b	Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32526552]
A549	IC₅₀	6.5 μM Compound: 8	Cytotoxicity against human A549 cells after 24 hrs by MTT assay Cytotoxicity against human A549 cells after 24 hrs by MTT assay	[PMID: 24050254]
BEAS-2B	IC₅₀	22.3 μM Compound: 12b	Cytotoxicity against human BEAS-2B assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human BEAS-2B assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32526552]
BGC-823	IC₅₀	8.5 μM Compound: 4, cinobufagin	Cytotoxicity against human BGC823 cells Cytotoxicity against human BGC823 cells	[PMID: 17911017]
Bel-7402	IC₅₀	0.1 μM Compound: 1	Cytotoxicity against human Bel7402 cells by MTT assay Cytotoxicity against human Bel7402 cells by MTT assay	[PMID: 18558746]
Bel-7402	IC₅₀	4.9 x 10^-2 μM Compound: CB	Cytotoxicity against human Bel7402 cells assessed as againsthibition of cell growth after 72 hrs Cytotoxicity against human Bel7402 cells assessed as againsthibition of cell growth after 72 hrs	[PMID: 21205911]
CCRF S-180	IC₅₀	> 50 μM Compound: 2	Cytotoxicity against mouse S180 cells expressing mutated alpha-1 Na+/K+-ATPase assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against mouse S180 cells expressing mutated alpha-1 Na+/K+-ATPase assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 23799775]
CNE	IC₅₀	0.31 μM Compound: 2	Cytotoxicity against human CNE1 cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against human CNE1 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 23799775]
CNE2Z	IC₅₀	0.39 μM Compound: 2	Cytotoxicity against human CNE2Z cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against human CNE2Z cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 23799775]
Calu-3	IC₅₀	2.3 μM Compound: 12b	Antiproliferative activity against human Calu-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human Calu-3 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32526552]
H22	IC₅₀	> 50 μM Compound: 2	Cytotoxicity against mouse H22 cells expressing mutated alpha-1 Na+/K+-ATPase assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against mouse H22 cells expressing mutated alpha-1 Na+/K+-ATPase assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 23799775]
HCT-116	IC₅₀	0.782 μM Compound: 49	Cytotoxicity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Cytotoxicity against human HCT-116 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 38142509]
HL-60	IC₅₀	< 0.01 μg/mL Compound: 12	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 11575946]
HeLa	IC₅₀	0.76 μM Compound: 4, cinobufagin	Cytotoxicity against human HeLa cells Cytotoxicity against human HeLa cells	[PMID: 17911017]
HepG2	IC₅₀	1.706 μM Compound: 2	Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against adriamycin-resistant human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 23799775]
HepG2	IC₅₀	2.355 μM Compound: 2	Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay	[PMID: 23799775]
HepG2	IC₅₀	5.2 μM Compound: 4, cinobufagin	Cytotoxicity against human HepG2 cells Cytotoxicity against human HepG2 cells	[PMID: 17911017]
HepG2	IC₅₀	5.5 μM Compound: 8	Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay	[PMID: 24050254]
KB	IC₅₀	0.21 μg/mL Compound: 12	Cytotoxicity against human KB cells after 72 hrs by MTT assay Cytotoxicity against human KB cells after 72 hrs by MTT assay	[PMID: 11575946]
MH60	IC₅₀	> 25 μg/mL Compound: 12	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	> 56.3 μM Compound: 9	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	> 56.3 μM Compound: 9	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]
NCI-H1299	IC₅₀	2.3 μM Compound: 12b	Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32526552]
NCI-H460	IC₅₀	2.3 μM Compound: 12b	Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32526552]
RKO	IC₅₀	0.182 μM Compound: 49	Cytotoxicity against human RKO cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Cytotoxicity against human RKO cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 38142509]
SK-MES-1	IC₅₀	2.3 μM Compound: 12b	Antiproliferative activity against human SK-MES-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human SK-MES-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32526552]
SW-620	IC₅₀	0.364 μM Compound: 49	Cytotoxicity against human SW620 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay Cytotoxicity against human SW620 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay	[PMID: 38142509]

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.

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.

470-37-1

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

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

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
10 mM	0.2260 mL	1.1298 mL	2.2597 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)

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: ≥ 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% β-Cyclodextrin in Saline
Solubility: ≥ 0.97 mg/mL (2.19 mM); Clear solution

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: 99.8%

Select Batch:

Data Sheet (282 KB) SDS (420 KB)

COA (252 KB) Elemental Analysis Report (110 KB)

Handling Instructions (2659 KB)

References

[1]. Guangxin Zhang, et al. Cinobufagin inhibits tumor growth by inducing intrinsic apoptosis through AKT signaling pathway in human nonsmall cell lung cancer cells. Oncotarget. 2016 Mar 3. [Content Brief]

[2]. Yang Yu, et al. Immunomodulatory Effects of Cinobufagin on Murine Lymphocytes and Macrophages. Evid Based Complement Alternat Med. 2015;2015:835263. [Content Brief]

[3]. Baek SH, et al. Cinobufagin exerts anti-proliferative and pro-apoptotic effects through the modulation ROS-mediated MAPKs signaling pathway. Immunopharmacol Immunotoxicol. 2015 Jun;37(3):265-73. [Content Brief]

Complete Stock Solution Preparation Table

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

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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Cinobufagin (Synonyms: Cinobufagine)

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Other Forms of Cinobufagin:

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9 Publications Citing Use of MCE Cinobufagin

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Cinobufagin Related Antibodies

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Complete Stock Solution Preparation Table

Cinobufagin Related Classifications

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