Bufalin

Name: Bufalin
Brand: MedChemExpress
SKU: HY-N0877
Rating: 5.0 (7 reviews)

Cat. No.: HY-N0877 Purity: 99.86%: FAQs
Data Sheet SDS COA Handling Instructions

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Bufalin is an active component isolated from Chan Su, acts as a potent Na⁺/K⁺-ATPase inhibitor, binds to the subunit α1, α2 and α3, with K_d of 42.5, 45 and 40 nM, respectively. Anti-cancer activity.

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

Bufalin Chemical Structure

CAS No. : 465-21-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 77	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 77	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Based on 7 publication(s) in Google Scholar

Other Forms of Bufalin:

Bufalin (Standard) Get quote

6 Publications Citing Use of MCE Bufalin

Cell Viability Assay

: Bufalin purchased from MedChemExpress. Usage Cited in: Apoptosis. 2023 May 30. [Abstract]; Bufalin (12.5, 25, 50, 100, 200 nM; 24, 48, 72 h) significantly reduces the viability of MKN-45 and HGC-27 GC cells in a dose- and time-dependent manner.

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Biological Activity
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References
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Description

IC₅₀ & Target

Kd: 42.5 nM (Na,K-ATPase α1), 45 nM (Na,K-ATPase α2), 40 nM (Na,K-ATPase α3)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	EC₅₀	7.5 nM Compound: 4	Cytotoxicity against human 786-O cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human 786-O cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
A549	IC₅₀	0.6 μM Compound: 7	Cytotoxicity against human A549 cells after 24 hrs by MTT assay Cytotoxicity against human A549 cells after 24 hrs by MTT assay	[PMID: 24050254]
Bel-7402	IC₅₀	7 nM Compound: 1	Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay Cytotoxicity against human Bel7402 cells after 72 hrs by MTT assay	[PMID: 15844967]
BGC-823	IC₅₀	4.5 x 10^-2 μM Compound: 1	Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay Cytotoxicity against human BGC823 cells after 72 hrs by MTT assay	[PMID: 15844967]
BXPC-3	EC₅₀	11 nM Compound: 4	Cytotoxicity against human BxPC3 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human BxPC3 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
CCRF S-180	EC₅₀	> 20000 nM Compound: 4	Cytotoxicity against mouse S180 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against mouse S180 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
CCRF S-180	IC₅₀	> 50 μM Compound: 1	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	0.279 μM Compound: 1	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	0.46 μM Compound: 1	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]
H22	IC₅₀	> 50 μM Compound: 1	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	EC₅₀	11 nM Compound: 4	Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
HeLa	IC₅₀	2.8 x 10^-2 μM Compound: 1	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 15844967]
HeLa	IC₅₀	279.9 nM Compound: Bufalin	Cytotoxicity activity against human HeLa cells after 48 hrs by MTT assay Cytotoxicity activity against human HeLa cells after 48 hrs by MTT assay	[PMID: 30245398]
HeLa	IC₅₀	594.2 nM Compound: Bufalin	Cytotoxicity activity against human HeLa cells after 24 hrs by MTT assay Cytotoxicity activity against human HeLa cells after 24 hrs by MTT assay	[PMID: 30245398]
HepG2	IC₅₀	0.345 μM Compound: 1	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	0.589 μM Compound: 1	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	0.6 μM Compound: 7	Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay Cytotoxicity against human HepG2 cells after 24 hrs by MTT assay	[PMID: 24050254]
HepG2	EC₅₀	35 nM Compound: 4	Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
HL-60	IC₅₀	< 0.01 μg/mL Compound: 16	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay Cytotoxicity against human HL60 cells after 72 hrs by MTT assay	[PMID: 11575946]
HUVEC	EC₅₀	12 nM Compound: 4	Cytotoxicity against human HUVEC cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human HUVEC cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
KB	IC₅₀	0.67 μg/mL Compound: 16	Cytotoxicity against human KB cells after 72 hrs by MTT assay Cytotoxicity against human KB cells after 72 hrs by MTT assay	[PMID: 11575946]
MCF7	EC₅₀	42 nM Compound: 4	Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
MES-SA	EC₅₀	28 nM Compound: 4	Cytotoxicity against human MESSA cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human MESSA cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
MES-SA/Dx5	EC₅₀	18 nM Compound: 4	Cytotoxicity against human MES-SA/Dx5 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human MES-SA/Dx5 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
MH60	IC₅₀	> 25 μg/mL Compound: 16	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	> 64.8 μM Compound: 3	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	31.9 μM Compound: 3	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-H1975	EC₅₀	13 nM Compound: 4	Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
SK-OV-3	EC₅₀	10 nM Compound: 4	Cytotoxicity against human SKOV3 cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human SKOV3 cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]
U-87MG ATCC	EC₅₀	14 nM Compound: 4	Cytotoxicity against human U87MG cells assessed as decrease in cell viability after 72 hrs by MTS assay Cytotoxicity against human U87MG cells assessed as decrease in cell viability after 72 hrs by MTS assay	[PMID: 30369239]

In Vitro

Bufalin (0, 1, 2, 4 μM for 48 hours) decreases cell viability in NCI-H460 cells^[2].
Bufalin (2 μM) increases caspae-3, Endo G and GADD153 mRNA expression, but decreases the GRP78 mRNA expression^[2].

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

Cell Viability Assay^[2]

Cell Line:	NCI-H460 cells
Concentration:	0, 1, 2, 4 μM
Incubation Time:	48 hours
Result:	Decreased viability of NCI-H460 cells in a dose-dependent manner.

In Vivo

Bufalin (0.1, 0.2, or 0.4 mg/kg, i.p., daily for 14 days) shows significant anti-tumor activity in mice bearing NCI-H460 cells^[2].

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

Animal Model:	Forty male athymic BALB/c nu/nu mice (6-8 weeks old)^[2]
Dosage:	0.1, 0.2, or 0.4 mg/kg
Administration:	I.P. every day until 14 days
Result:	Dose-dependently suppressed tumor growth.

Molecular Weight

386.52

Formula

C₂₄H₃₄O₄

CAS No.

465-21-4

Appearance

Solid

Color

White to off-white

SMILES

O[C@]([C@@](CC[C@@]1([H])[C@@]2(CC[C@H](O)C1)C)([H])[C@]2([H])CC3)(CC[C@@H]4C(C=C5)=COC5=O)[C@]34C

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	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (258.72 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	2.5872 mL	12.9359 mL	25.8719 mL
5 mM	0.5174 mL	2.5872 mL	5.1744 mL
10 mM	0.2587 mL	1.2936 mL	2.5872 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.47 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 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.47 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.
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

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: 99.86%

Select Batch:

Data Sheet (279 KB) SDS (480 KB)

COA (253 KB) HNMR (167 KB) LCMS (112 KB)

Handling Instructions (2659 KB)

References

[1]. Katz A, et al. Selectivity of digitalis glycosides for isoforms of human Na,K-ATPase. J Biol Chem. 2010 Jun 18;285(25):19582-92. [Content Brief]

[2]. Wu SH, et al. Bufalin induces apoptosis in vitro and has Antitumor activity against human lung cancer xenografts in vivo. Environ Toxicol. 2017 Apr;32(4):1305-1317. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5872 mL	12.9359 mL	25.8719 mL	64.6797 mL
	5 mM	0.5174 mL	2.5872 mL	5.1744 mL	12.9359 mL
	10 mM	0.2587 mL	1.2936 mL	2.5872 mL	6.4680 mL
	15 mM	0.1725 mL	0.8624 mL	1.7248 mL	4.3120 mL
	20 mM	0.1294 mL	0.6468 mL	1.2936 mL	3.2340 mL
	25 mM	0.1035 mL	0.5174 mL	1.0349 mL	2.5872 mL
	30 mM	0.0862 mL	0.4312 mL	0.8624 mL	2.1560 mL
	40 mM	0.0647 mL	0.3234 mL	0.6468 mL	1.6170 mL
	50 mM	0.0517 mL	0.2587 mL	0.5174 mL	1.2936 mL
	60 mM	0.0431 mL	0.2156 mL	0.4312 mL	1.0780 mL
	80 mM	0.0323 mL	0.1617 mL	0.3234 mL	0.8085 mL
	100 mM	0.0259 mL	0.1294 mL	0.2587 mL	0.6468 mL

Bufalin 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:

Bufalin465-21-4Na+/K+ ATPaseSodium potassium pumpInhibitorinhibitorinhibit

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Bufalin

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Other Forms of Bufalin:

Bufalin Related Antibodies

6 Publications Citing Use of MCE Bufalin

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Bufalin Related Antibodies

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Complete Stock Solution Preparation Table

Bufalin Related Classifications

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