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SAR-439859

  Cat. No.:  DC60004   Featured
Chemical Structure
2114339-57-8
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More than 5000 active chemicals with high quality for research!
Field of application
SAR439859 is an orally available, nonsteroidal selective estrogen receptor degrader/downregulator (SERD), with potential antineoplastic activity. Upon oral administration, SERD SAR439859 specifically targets and binds to the estrogen receptor (ER) and induces a conformational change that promotes ER degradation. This prevents ER-mediated signaling and inhibits both the growth and survival of ER-expressing cancer cells
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2114339-57-8
Chemical 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
SMILES: ClC1C=C(C=CC=1C1CCCC2C=C(C(=O)O)C=CC=2C=1C1C=CC(=CC=1)O[C@H]1CCN(CCCF)C1)Cl
Formula: C31H30Cl2FNO3
M.Wt: 554.47921037674
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO Application
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].
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].
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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