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SAR439859 (Synonyms: SAR439859)

Catalog No.GC61267

SAR439859 (compuesto 43d) es un degradador del receptor de estrÓgeno (SERD) selectivo, no esteroideo y activo por vÍa oral. SAR439859 es un potente antagonista de ER y tiene actividad degradante de ER con un EC50 de 0,2 nM para ERα degradaciÓn. SAR439859 demuestra una eficacia antitumoral robusta y una resistencia cruzada limitada en el cÁncer de mama ER+.

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SAR439859 Chemical Structure

Cas No.: 2114339-57-8

Tamaño Precio Disponibilidad Cantidad
5mg
243,00 $
Disponible
10mg
367,00 $
Disponible
50mg
1.055,00 $
Disponible
100mg
1.503,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

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].

SAR439859 (compound 43d) induces strong in vivo antitumor activity against a variety of BC cell lines and patient-derived xenografts, including models that harbor ERα mutations[1].

SAR439859 (compound 43d; orally; 2.5-25 mg/kg; twice daily for 30 days) exhibits substantial tumor-growth inhibition and displays tumor regression at the dose of 25 mg/kg/BID[1]. SAR439859 (3 mg/kg for iv and 10 mg/kg for po) shows a low to moderate clearance in the three animal species tested (0.03-1.92 L/h•kg), low to moderate volume of distribution (Vss=0.5-6.1 L/kg), and good bioavailability (54-76%) across species. It is noticed that T1/2 was variable across species (1.98 h in mouse, 4.13 h in rat and 9.80 h in dog)[1]. Animal Model: Nu/nu mouse with MCF7 tumor xenograft model[1]

[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+ breast cancer.

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Average Rating: 5 ★★★★★ (Based on Reviews and 38 reference(s) in Google Scholar.)

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