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Bufalin ATPase inhibitor

Name: Bufalin
Brand: Selleck Chemicals
SKU: S7821
Availability: InStock
Rating: 5 (10 reviews)

Cat.No.S7821

Bufalin (BF) is a potent inhibitor of steroid receptor coactivator SRC-3, SRC-1 and Na+/K+-ATPase. This compound binds to the subunit α1, α2 and α3 of Na+/K+-ATPase with Kd of 42.5 nM, 45 nM and 40 nM, respectively. It is a major immunoreactive component isolated from the Chinese medicine Chan Su with anti-cancer activity.

Chemical Structure

Molecular Weight: 386.52

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Quality Control

Batch: Purity: 99.98%

99.98

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel GluR
Other ATPase Inhibitors	(-)-Blebbistatin Thapsigargin Brefeldin A (BFA) CB-5083 Sodium orthovanadate Ouabain (NSC-25485) Golgicide A BTB06584 Ginsenoside Rb1 CDN1163

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (201.8 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 40 mg/mL

Water : ˂1 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	1%DMSO 1 5%Tween80 2 3%PEG300 3 91%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.400mg/ml (1.03mM)	Taking the 1 mL working solution as an example, add 10 μL 40 mg/ml clarified DMSO stock solution to 50 μL Tween80, mix evenly to clarify it; add 30 μL PEG300 to the above system, mix evenly to clarify it; then continue to add 910 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	386.52	Formula	C₂₄H₃₄O₄	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	465-21-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	SRC-3 SRC-1 Na+/K+-ATPase α3 (Cell-free assay) 40 nM Na+/K+-ATPase α1 (Cell-free assay) 42.5 nM Na+/K+-ATPase α2 (Cell-free assay) 45 nM
In vitro	Bufalin strongly promotes SRC-3 protein degradation and binds directly to the coactivator. This compound is able to block cancer cell growth at nanomolar concentrations.
In vivo	When incorporated into a nanoparticle delivery system, bufalin is able to reduce tumor growth in a mouse xenograft model of breast cancer. This compound sensitizes cancer cells to other targeted chemotherapeutic agents.
References	[1] https://pubmed.ncbi.nlm.nih.gov/20388710/ [2] https://pubmed.ncbi.nlm.nih.gov/24390736/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06360809	Recruiting	Breast Cancer	Institut Nacional d''Educacio Fisica de Catalunya\|ICFO - The Institute of Photonics Sciences\|Hospital Clinic of Barcelona\|Institut d''Investigacions Biomèdiques August Pi i Sunyer\|Universidad San Jorge	March 22 2024	Not Applicable
NCT06240078	Recruiting	Pulmonary Disease Chronic Obstructive\|Sexual Health\|Loneliness\|Well-Being Psychological	Vejle Hospital\|Region of Southern Denmark	February 20 2024	--

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