2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO Application
Biological activity
Description
CAS NO.：2114339-57-8 Product Name：Unii-tbf1nhy02O Synonyms：SAR439859;TBF1NHY02O;6-(2,4-dichlorophenyl)-5-[4-[(3~{S})-1-(3-fluoranylpropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7~{H}-benzo[7]annulene-2-carboxylic acid;Amcenestrant;Amcenestrant [INN];US9714221, Example 51;BDBM263716;Q66885452;8-(2,4-Dichlorophenyl)-9-(4-(((3S)-1-(3-fluoropropyl)-3-pyrrolidinyl)oxy)phenyl)-6,7-dihydro-5H-benzocycloheptene-3-carboxylic acid;L5B;6-(2,4-dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3;Unii-tbf1nhy02O EINEC: Molecular Formula：C31H30CL2FNO3 Molecular Weight：554.47921037674
Target:
ERα:0.2 nM (EC50)
In Vivo
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] Dosage: 2.5, 5, 12.5, 25 mg/kg Administration: Orally; twice daily for 30 days Result: Exhibited substantial tumor-growth inhibition and displayed tumor regression at the dose of 25 mg/kg/BID. Animal Model: Mouse, rat and dog[1] Dosage: 3 mg/kg (iv) and 10 mg/kg (po) (Pharmacokinetic Analysis) Administration: Iv or po Result: Showed 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.
In Vitro
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].
Kinase Assay
Cell Assay
Animal Administration
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+ breast cancer.
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