SAR439859, CAS 2114339-57-8

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).

• Artikelnummer: CAY40748-1
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 40748-1
• Verpackungseinheit: 1 mg
• Mengeneinheit: STK