A selective estrogen receptor degrader; binds to rat uterine ER (IC50 = 44.8 nM); prevents increases in uterine weight induced by estradiol in immature rats (ED50 = 0.06 mg/kg per day); inhibits the growth of ER-positive MCF-7 human breast cancer cells at 1 µg/ml; prevents tumor growth in MCF-7 and Br10 breast cancer mouse xenograft models at 1 µg/ml; neuroprotective in vitro against neurotoxicity induced by glutamate- and Aβ42

Fulvestrant – 50 mg

Brand:
Cayman
CAS:
129453-61-8
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

A selective estrogen receptor degrader; binds to rat uterine ER (IC50 = 44.8 nM); prevents increases in uterine weight induced by estradiol in immature rats (ED50 = 0.06 mg/kg per day); inhibits the growth of ER-positive MCF-7 human breast cancer cells at 1 µg/ml; prevents tumor growth in MCF-7 and Br10 breast cancer mouse xenograft models at 1 µg/ml; neuroprotective in vitro against neurotoxicity induced by glutamate- and Aβ42

Formal name: 7α-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]-estra-1,3,5(10)-triene-3,17β-diol

Synonyms:  ICI 182780

Molecular weight: 606.8

CAS: 129453-61-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Lipids|Sterol Lipids||Product Type|Biochemicals|Receptor Pharmacology||Research Area|Cancer||Research Area|Endocrinology & Metabolism|Hormones & Receptors|Estrogens & Progestins

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