SAR439859 | SERD | Probechem Biochemicals

Chemical Structure : SAR439859

CAS No.: 2114339-57-8

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SAR439859 (Amcenestrant, SAR 439859)

货号: 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).

规格	价格	库存
5 mg	￥1580	In stock
10 mg	￥2280	In stock
25 mg	￥3780	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	554.483
分子式	C31H30Cl2FNO3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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.

SAR439859 (Amcenestrant, SAR 439859)

生物&药学活性

物理化学性质&存储条件

参考文献

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SAR439859 (Amcenestrant, SAR 439859)

生物&药学活性

物理化学性质&存储条件

参考文献

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