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SAR439859

Chemical Structure : SAR439859

CAS No.: 2114339-57-8

SAR439859 (Amcenestrant, SAR 439859)

Catalog No.: PC-73108Not For Human Use, Lab Use Only.

SAR439859 (Amcenestrant) is a potent, orally available, selective estrogen receptor degrader (SERD) with IC50 of 0.2 nM (ERα degradation).

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

Biological Activity

SAR439859 (Amcenestrant) is a potent, orally available, selective estrogen receptor degrader (SERD) with IC50 of 0.2 nM (ERα degradation).
SAR439859 showed an outstanding overall profile with high degradation efficacy (98%) comparable to the in vitro activity of fulvestrant combined with a remarkable metabolic stability.
SAR439859 displayed no off-target activity in a large Cerep panel for in vitro selectivity.
SAR439859 exhibited substantial tumor-growth inhibition, at a dose of 25 mg/kg/BID, SAR439859 displayed tumor regression in MCF-7 tamoxifen-sensitive xenograft, with no weight loss.

Physicochemical Properties

M.Wt 554.483
Formula C31H30Cl2FNO3
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

10 mM in DMSO

Chemical Name/SMILES

6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid

References

1. El-Ahmad Y, et al. J Med Chem. 2020 Jan 23;63(2):512-528.

2. Shomali M, et al. Mol Cancer Ther. 2021 Feb;20(2):250-262.

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