Formulation: A solid
Formal Name: 8-(2,4-dichlorophenyl)-9-[4-[[(3S)-1-(3-fluoropropyl)-3-pyrrolidinyl]oxy]phenyl]-6,7-dihydro-5H-benzocycloheptene-3-carboxylic acid
Purity: ≥98%
Formula Markup: C31H30Cl2FNO3
Formula Weight: 554,5
Shelf life (days): 1460
CAS Number: 2114339-57-8
Notes: SAR439859 is a selective estrogen receptor degrader (SERD).{72354} It selectively induces degradation of estrogen receptor α (ERα) in MCF-7 breast cancer cells (EC50 = 0.2 nM) over ERβ, glucocorticoid, androgen, progesterone, and mineralocorticoid receptors at 5 µM but does activate ERβ signaling in reporter cells.{72355} SAR439859 decreases 17β-estradiol-induced proliferation of MCF-7 cells expressing wild-type ERα, MCF-7 cells expressing ERα containing a tyrosine-to-serine substitution at position 537 (ERαY537S), and MCF-7 cells expressing ERαD538G (EC50s = 20, 331, and 595 nM, respectively). In vivo, SAR439859 (100 mg/kg per day) reduces tumor volume to a greater extent than the ER degraders fulvestrant (Item No. 10011269) or GDC-0810 (ARN810; Item No. 29595) in a patient-derived xenograft (PDX) mouse model of breast cancer resistant to the ER antagonist tamoxifen (Item Nos. 13258 / 11629).
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