Bufalin

Catalog No.S7821 Synonyms: BF

For research use only.

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

Bufalin Chemical Structure

CAS No. 465-21-4

Selleck's Bufalin has been cited by 2 Publications

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Biological Activity

Description Bufalin (BF) is a potent inhibitor of steroid receptor coactivator SRC-3, SRC-1 and Na+/K+-ATPase. Bufalin binds to the subunit α1, α2 and α3 of Na+/K+-ATPase with Kd of 42.5 nM, 45 nM and 40 nM, respectively. Bufalin is a major digoxin-like immunoreactive component isolated from the Chinese medicine Chan Su with anti-cancer activity.
Targets
SRC-3 [2]
()
SRC-1 [2]
()
Na+/K+-ATPase α3 [1]
(Cell-free assay)
Na+/K+-ATPase α1 [1]
(Cell-free assay)
Na+/K+-ATPase α2 [1]
(Cell-free assay)
40 nM 42.5 nM 45 nM
In vitro

Bufalin strongly promotes SRC-3 protein degradation and binds directly to the coactivator. Bufalin is able to block cancer cell growth at nanomolar concentrations.[2]

In vivo

When incorporated into a nanoparticle delivery system, bufalin is able to reduce tumor growth in a mouse xenograft model of breast cancer. Bufalin sensitizes cancer cells to other targeted chemotherapeutic agents.[2]

Protocol (from reference)

Cell Research:

[2]

  • Cell lines: HeLa, MCF-7, A549 cells
  • Concentrations: 2 nM, 5 nM, 7.5 nM
  • Incubation Time: 24 h
  • Method:

    Luciferase assays are performed in HeLa cells transiently transfected with the reporter vector pG5-LUC in combination with expression vectors for pBIND, pBIND SRC-1, SRC-2 or SRC-3 prior to incubation with bufalin of different doses (0, 2, 5 and 7.5 nM) for 24 hours.

  • (Only for Reference)
Animal Research:

[2]

  • Animal Models: 6-7 week old SCID mice injected with MDA-MB-231-LM3.3 cells
  • Dosages: 1.5 mg/kg
  • Administration: IV
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 78 mg/mL
(201.8 mM)
Ethanol 40 mg/mL
(103.48 mM)
Water ˂1 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 386.52
Formula

C24H34O4

CAS No. 465-21-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC12CCC(CC1CCC3C2CCC4(C3(CCC4C5=COC(=O)C=C5)O)C)O

In vivo Formulation Calculator (Clear solution)

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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.
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05110456 Not yet recruiting Behavioral: Telephone support Depression Postpartum St. Justine''s Hospital|St. Justine Foundation|Canadian Medical Association|Hewitt Foundation November 2021 Not Applicable
NCT04901572 Not yet recruiting Diagnostic Test: QISI device Healthy QART Medical|Technostat June 2021 Not Applicable
NCT04849689 Completed Behavioral: Whole-food plant-based lifestyle Body Weight|Body Image|Body Weight Changes|Muscle Loss Barbara Jakše s.p. April 12 2021 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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