Fulvestrant-d3 (Synonyms: ICI 182780-d3; ZD 9238-d3; ZM 182780-d3) |
Catalog No.GC40241 |
풀베스트란트-d3(ICI 182780-d3)은 풀베스트란트로 표시된 중수소입니다. 풀베스트란트(ICI 182780)는 순수한 항에스트로겐이며 IC50이 9.4nM인 강력한 에스트로겐 수용체(ER) 길항제입니다. 풀베스트란트는 또한 GPR30 작용제입니다. 풀베스트란트는 0.29nM의 IC50으로 ER-양성 MCF-7 세포의 성장을 효과적으로 억제합니다. 풀베스트란트는 또한 자가포식을 유도하고 항종양 효능이 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
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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