Fulvestrant-d3 (ICI 182780-d3) 是标记为 Fulvestrant 的氘。 Fulvestrant (ICI 182780) 是一种纯抗雌激素和有效的雌激素受体 (ER) 拮抗剂，IC50 为 9.4 nM。 Fulvestrant 也是一种 GPR30 激动剂。 Fulvestrant 有效抑制 ER 阳性 MCF-7 细胞的生长，IC50 为 0.29 nM。 Fulvestrant 还诱导自噬并具有抗肿瘤功效。
货号:ajcx17546
CAS:N/A
分子式:C32H44D3F5O3S
分子量：609.8
溶解度:DMF: 25 mg/ml,DMSO: 20 mg/ml,Ethanol: 25 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.