AZD9833

Catalog No.S8958

For research use only.

AZD9833 is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity.

AZD9833 Chemical Structure

CAS No. 2222844-89-3

Purity & Quality Control

Choose Selective Estrogen/progestogen Receptor Inhibitors

Other Estrogen/progestogen Receptor Products

Biological Activity

Description AZD9833 is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity.
Targets
ER [1]
()
In vitro

AZD9833 is demonstrated to be a highly potent selective estrogen receptor degraders (SERD) that shows a pharmacological profile comparable to fulvestrant in its ability to degrade ERα in both MCF-7 and CAMA-1 cell lines.[2]

In vivo

A stringent control of lipophilicity ensures that AZD9833 has favorable physicochemical and preclinical pharmacokinetic properties for oral administration. AZD9833 is potent in vivo activity in mouse xenograft models.[2]

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: MCF-7 cells
  • Concentrations: 100 nM
  • Incubation Time: 24 h
  • Method:

    MCF7 cells are treated with DMSO, 1 nM estradiol (E2), or 100 nM 4-OH tamoxifen, fulvestrant, or AZD9833 for 24 h. Expression of the ERα regulated genes PGR, TFF1, and GREB1 is assessed.

  • (Only for Reference)
Animal Research:

[1]

  • Animal Models: Male CB17 SCID mice, rats
  • Dosages: 0.5 mg/kg, 1 mg/kg, 2 mg/kg, 5 mg/kg
  • Administration: IV, Oral gavage
  • (Only for Reference)

Solubility (25°C)

In vitro

DMSO 95 mg/mL
(199.36 mM)
Water Insoluble
Ethanol ''''95 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 476.51
Formula

C24H28F4N6

CAS No. 2222844-89-3
Storage 3 years -20°C powder
2 years -80°C in solvent

In vivo Formulation Calculator (Clear solution)

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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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04588298 Recruiting Drug: AZD9833 HER2-negative Breast Cancer AstraZeneca November 2 2020 Phase 2
NCT04541433 Recruiting Drug: AZD9833 ER+ HER2- Advanced Breast Cancer AstraZeneca September 29 2020 Phase 1

(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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