Fulvestrant-d3 (Synonyms: ICI 182780-d3; ZD 9238-d3; ZM 182780-d3) |
Katalog-Nr.GC40241 |
Fulvestrant-d3 (ICI 182780-d3) ist das als Fulvestrant bezeichnete Deuterium. Fulvestrant (ICI 182780) ist ein reines AntiÖstrogen und ein starker Antagonist des Östrogenrezeptors (ER) mit einem IC50 von 9,4 nM. Fulvestrant ist auch ein GPR30-Agonist. Fulvestrant hemmt wirksam das Wachstum von ER-positiven MCF-7-Zellen mit einer IC50 von 0,29 nM. Fulvestrant induziert auch Autophagie und hat eine Antitumorwirkung.
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Sample solution is provided at 25 µL, 10mM.
Fulvestrant-d3 is intended for use as an internal standard for the quantification of fulvestrant by GC- or LC-MS. Fulvestrant is a selective estrogen receptor degrader (SERD) that downregulates and degrades estrogen receptor α (ERα). 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. 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. Formulations containing fulvestrant have been used in the treatment of estrogen-sensitive breast cancer.
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