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Camizestrant

Chemical Structure : Camizestrant

CAS No.: 2222844-89-3

Camizestrant (AZD-9833, AZD9833)

Catalog No.: PC-72606Not For Human Use, Lab Use Only.

AZD9833 (Camizestrant) is an orally bioavailable, highly potent, next-generation selective estrogen receptor degrader (SERD) and antagonist with both EC50 of <1 nM (ERα receptor) in MCF7 cells.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

AZD9833 (Camizestrant) is an orally bioavailable, highly potent, next-generation selective estrogen receptor degrader (SERD) and antagonist with both EC50 of <1 nM (ERα receptor) in MCF7 cells.
AZD9833 demonstrated to be a highly potent SERD that showed a pharmacological profile comparable to fulvestrant in its ability to degrade ERα in both MCF-7 and CAMA-1 cell lines.
In contrast to AZD9496, AZD9833 does not cause ER agonism in the endometrial carcinoma cell line Ishikawa in vitro and does not cause an increase in the thickness of the endometrium in juvenile rats.
AZD9833 completely suppresses tumor growth in several patient-derived and cell line xenograft models, including models with clinically relevant ESR1 mutations.

Physicochemical Properties

M.Wt 476.524
Formula C24H28F4N6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

200 mM in DMSO (95.3 mg/mL)

Chemical Name/SMILES

N-[1-(3-fluoropropyl)azetidin-3-yl]-6-[(6S,8R)-8-methyl-7-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinolin-6-yl]pyridin-3-amine

References

1. Bamberg K, et al. PLoS One. 2018 Feb 23;13(2):e0193380.

2. Granberg KL, et al. J Med Chem. 2019 Feb 14;62(3):1385-1406.

3. Whittaker A, et al. Clin Transl Sci. 2020 Mar;13(2):275-283.

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