Home Endocrinology & Hormones Estrogen/progestogen Receptor antagonist Camizestrant (AZD9833) For research use only.

Camizestrant (AZD9833)

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

Camizestrant (AZD9833) Chemical Structure

Camizestrant (AZD9833) Chemical Structure

CAS No. 2222844-89-3

Purity & Quality Control

Batch: S895801 DMSO]95 mg/mL]false]Ethanol]95 mg/mL]false]Water]Insoluble]false Purity: 99.38%
99.38

Camizestrant (AZD9833) Related Products

Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Signaling Pathway

Biological Activity

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

AZD9833 is demonstrated to be a highly potent selective estrogen receptor degraders (SERD) that shows a pharmacological profile comparable to ICI-182780;in its ability to degrade ERα in both MCF-7 and CAMA-1 cell lines.[2]
Cell Research 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 ICI 46474, ICI-182780, or AZD9833 for 24 h. Expression of the ERα regulated genes PGR, TFF1, and GREB1 is assessed.
In Vivo
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]
Animal Research 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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05551897 Completed
Healthy Subjects
AstraZeneca|Parexel
 October 4 2022 Phase 1
NCT05364255 Completed
ER-positive HER2-negative Breast Cancer
AstraZeneca|Quotient Sciences
 May 10 2022 Phase 1

Chemical Information & Solubility

Molecular Weight 476.51 Formula

C24H28F4N6
CAS No. 2222844-89-3 SDF --
Smiles CC1CC2=C(C=CC3=C2C=N[NH]3)C(N1CC(F)(F)F)C4=NC=C(NC5CN(CCCF)C5)C=C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 95 mg/mL ( (199.36 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 95 mg/mL

Water : Insoluble


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In vivo
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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. )

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

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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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