Product Description: SAR439859 (compound 43d) is an orally active, non-steroidal, and selective estrogen receptor degrader (SERD). SAR439859 is an effective ER antagonist with ER degradation activity, an EC50 of 0.2 nM. SAR439859 can show potent anti-tumor effects and limited cross-resistance in ER+ breast cancer.
Applications: Cancer-programmed cell death
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: 99.79
Research Area: Cancer
Solubility: DMSO : 83.33 mg/mL (ultrasonic;warming;heat to 60°C)
Target: Estrogen Receptor/ERR
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