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].
体内研究
Camizestrant (oral administration; 0.2-50 mg/kg; 20 days) demonstrates dose-dependent anti-tumor effectiveness in xenografts of human parental MCF7 mice [1].
Camizestrant (oral administration; 0.8-40 mg/kg; 30 days) reduces tumor growth in a dose-dependent manner. It achieves nearly complete inhibition of tumor growth at doses exceeding 10 mg/kg in mice [1].
体外研究
Camizestrant is sourced from example 17 of US patent US20180111931A1 [1].
Camizestrant 细胞实验
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
Camizestrant 动物实验
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
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