Formulation: A solid
Formal Name: (7R,8R,9S,13S,14S,17S)-13-methyl-7-(9-((4,4,5,5,5-pentafluoropentyl)sulfinyl)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-16,16,17-d3-3,17-diol
Purity: ≥99% deuterated forms (d1-d3)
Formula Markup: C32H44D3F5O3S
Formula Weight: 609,8
Shelf life (days): 1460
Notes: Fulvestrant-d3 is intended for use as an internal standard for the quantification of fulvestrant (Item No. 10011269) by GC- or LC-MS. Fulvestrant is a selective estrogen receptor degrader (SERD) that downregulates and degrades estrogen receptor α (ERα).{16606,43228} It binds to rat uterine ER with an IC50 value of 44.8 nM and prevents uterine weight increases induced by estradiol in immature rats (ED50 = 0.06 mg/kg per day) but has no effect on uterine weight alone.{43229} It also decreases uterine weight in adult rats without affecting the production of luteinizing and follicle-stimulating hormones and prolactin. Fulvestrant inhibits the growth of ER-positive MCF-7 human breast cancer cells but not ER-negative BT-20 cells when used at a concentration of 1 µg/ml. It also prevents tumor growth in MCF-7 and Br10 breast cancer mouse xenograft models when used at a single dose of 5 mg per animal. Fulvestrant is neuroprotective in vitro against neurotoxicity induced by glutamate- and amyloid-β (1-42) (Aβ42) in primary rat hippocampal cells.{16605} Formulations containing fulvestrant have been used in the treatment of estrogen-sensitive breast cancer.
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