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Amcenestrant

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Products Details

Product Description

– SAR439859 (compound 43d) is an orally active, nonsteroidal and selective estrogen receptor degrader (SERD). SAR439859 is a potent ER antagonist and has ER degrading activity with an EC50 of 0.2 nM for ERα degradation[1]. SAR439859 demonstrates robust antitumor efficacy and limited cross-resistance in ER+ breast cancer[2].

Web ID

– HY-133017

Storage Temperature

– -20°C, 3 years; 4°C, 2 years (Powder)

Shipping

– Room Temperature

Applications

– Cancer-programmed cell death

Molecular Formula

– C31H30Cl2FNO3

References

– [1]El-Ahmad Y, et al. Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer. J Med Chem. 2019 Nov 27.|[2]Monsif Bouaboula, et al. Abstract 943: SAR439859, an orally bioavailable selective estrogen receptor degrader (SERD) that demonstrates robust antitumor efficacy and limited cross-resistance in ER<sup>+</sup> breast cancer.

CAS Number

– 2114339-57-8

Molecular Weight

– 554.48

Compound Purity

– 99.59

SMILES

– O=C(C1=CC=C(C(C2=CC=C(O[C@@H]3CN(CCCF)CC3)C=C2)=C(C4=CC=C(Cl)C=C4Cl)CCC5)C5=C1)O

Clinical Information

– Phase 3

Research Area

– Cancer

Solubility

– DMSO : 83.33 mg/mL (ultrasonic;warming;heat to 60°C)

Target

– Estrogen Receptor/ERR

Isoform

– ERα

Pathway

– Vitamin D Related/Nuclear Receptor

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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