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Chemical Structure : SAR439859
CAS No.: 2114339-57-8
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).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $158 | In stock | |
| 10 mg | $228 | In stock | |
| 25 mg | $378 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 554.483 | |
| Formula | C31H30Cl2FNO3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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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