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Chemical Structure| 2222844-89-3 Chemical Structure| 2222844-89-3

Structure of Camizestrant
CAS No.: 2222844-89-3

Chemical Structure| 2222844-89-3

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AZD-9833 is a potent and orally active estrogen receptor (ER) antagonist. AZD-9833 is used for the study of ER+ HER2-advanced breast cancer[1].

Synonyms: AZD-9833

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Product Details of Camizestrant

CAS No. :2222844-89-3
Formula : C24H28F4N6
M.W : 476.51
SMILES Code : FC(F)(F)CN1[C@H](C2=CC=C(NC3CN(CCCF)C3)C=N2)C4=C(C5=C(NN=C5)C=C4)C[C@H]1C
Synonyms :
AZD-9833
MDL No. :N/A
InChI Key :WDHOIABIERMLGY-CMJOXMDJSA-N
Pubchem ID :134453496

Safety of Camizestrant

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

Description
Camizestrant (AZD-9833) is a highly potent and orally bioavailable antagonist of the estrogen receptor (ER). It is employed in the investigation of ER+ HER2-negative advanced breast cancer [1].

In Vitro:

Cell Line
Concentration Treated Time Description References
Ishikawa 100 nmol/L 48 h To evaluate the ability of Camizestrant to degrade ER and assess potential ER agonism in endometrial cancer cells, results showed Camizestrant effectively degraded ER with no evidence of agonism Cancer Res. 2023 Dec 1;83(23):3989-4004
CAMA-1 100 nmol/L 24 h To evaluate the ability of Camizestrant to degrade ER protein and modulate ER-regulated gene expression, results showed Camizestrant effectively degraded ER and completely antagonized ER transcriptional activity Cancer Res. 2023 Dec 1;83(23):3989-4004
MCF7 100 nmol/L 24 h To evaluate the ability of Camizestrant to degrade ER protein and modulate ER-regulated gene expression, results showed Camizestrant effectively degraded ER and completely antagonized ER transcriptional activity Cancer Res. 2023 Dec 1;83(23):3989-4004

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice ER+ breast cancer PDX models Oral 10 mg/kg daily Daily administration for 28 days To evaluate the antitumor activity of Camizestrant in ER+ breast cancer PDX models, results showed Camizestrant exhibited antitumor activity in 56% of ESR1 wild-type and mutant models, superior to fulvestrant Cancer Res. 2023 Dec 1;83(23):3989-4004

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05790304 Hepatic Impairment PHASE1 COMPLETED 2024-02-22 Research Site, San Antonio, Te... More >>xas, 78215, United States|Research Site, San Antonio, Texas, 78229, United States|Research Site, Sofia, 1612, Bulgaria|Research Site, Bratislava, 831 01, Slovakia Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.49mL

2.10mL

1.05mL

20.99mL

4.20mL

2.10mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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