Fulvestrant (ICI-182780) - Moligand™, 10mM in DMSO , Estrogen receptor antagonist, CAS No.129453-61-8, Estrogen receptor antagonist

CAS: 129453-61-8 Cat. No.: F408459 Peso molecular: 606.77 Número EC: 642-998-6

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

ZD 9238, ZM 182780 | 7-​[9-​[(4,​4,​5,​5,​5-​pentafluoropentyl)​sulfinyl]​nonyl]​-​ (7α,​17β)​-estra-​1,​3,​5(10)​-​triene-​3,​17-​diol

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Fulvestrant (ICI-182780, ZD 9238, ZM 182780) is anestrogen receptor (ER)antagonist withIC50of 0.94 nM in a cell-free assay. Fulvestrant also inducesautophagyandapoptosisand has antitumor activity.
In vitro

Fulvestrant is an effective inhibitor of the growth of ER-positive MCF-7 (with IC50 of 0.29 nM) but with no effect on the growth of ER-negative BT-20 human breast cancer cells. Fulvestrant causes accumulation of cells in G0/G1 and also reduces the proportion of cells capable of continued DNA synthesis. Fulvestrant competitively inhibits binding of oestradiol to the estrogen receptor. Fulvestrant blocks nuclear localization of the ER through impairing receptor dimerisation, and energy-dependent nucleo-cytoplasmic shuttling. Because of the instability of fulvestrant-ER complex, the binding of Fulvestrant with ER finally results in accelerated degradation of the ER protein. Fulvestrant (10 nM) not only decreases IGF-IR mRNA levels but also decreases the half-life. Treatment with 100 μM Fulvestrant leads to a time dependent increase of TNFR1 and TRADD steady-state mRNA levels in MCF-7 cells. Fulvestrant is capable of down-regulating androgen receptor expression and diminishes androgenic responses in LNCaP human prostate cancer cells. Fulvestrant also significantly attenuates R1881-stimulated growth by 70%. Fulvestrant is able to modulate mitosis and cell death in immature cerebellar neurons via rapid activation of MAPK.

In vivo

Fulvestrant is devoid of uterotropic activity, and when co-administered with estradiol, it effectively blocks the uterotropic action of estradiol with ED50 of 0.06 mg/kg/day s.c. in immature female rats. A single s.c. injection of 5 mg of Fulvestrant suspension blocks completely the growth of MCF-7 xenografts. The growth of transplants of the BrlO human breast tumor is also suppressed effectively by 10 μM Fulvestrant. Fulvestrant (10 mg/rat, s.c.) reduces the androgen receptor expression, ERK1/2 phosphorylation and cell proliferation in the rat ventral prostate. Fulvestrant also displays anti-angiogenesis in the chick egg chorioallantoic membrane.
Cell Data

cell lines：

Concentrations：2.9 nM

Incubation Time：5 days

Powder Purity:≥99%

Specifications

Sinónimos

ZD 9238, ZM 182780 | 7-​[9-​[(4, ​4, ​5, ​5, ​5-​pentafluoropentyl)​sulfinyl]​nonyl]​-​ (7α, ​17β)​-estra-​1, ​3, ​5(10)​-​triene-​3, ​17-​diol

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Fulvestrant (ICI-182780, ZD 9238, ZM 182780) is an estrogen receptor (ER) antagonist with IC50 of 0.94 nM in a cell-free assay. Fulvestrant also induces autophagy and apoptosis and has antitumor activity.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

AGONIST, ANTAGONIST

Mecanismo de acción

Estrogen receptor antagonist

Propiedades del producto

• ALogP: 9.2

Nombres e identificadores

• Isómeros SMILES: C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2O)[C@@H](CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F
• WGK Alemania: 3
• RTECS: KG7623000
• Peso molecular: 606.77
• Reaxy-Rn: 25807391
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=25807391&ln=

Objetivos asociados (humanos)

ESRRA Tchem Steroid hormone receptor ERR1 (1 Activities)

Discover Target: ESRRA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ESR1 Tclin Estrogen receptor (31 Activities)

Discover Target: ESR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ESR2 Tclin Estrogen receptor beta (8 Activities)

Discover Target: ESR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EPHX2 Tchem Bifunctional epoxide hydrolase 2 (2 Activities)

Discover Target: EPHX2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PGR Tclin Progesterone receptor (1 Activities)

Discover Target: PGR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GPER1 Tchem G-protein coupled estrogen receptor 1 (1 Activities)

Discover Target: GPER1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 30 mg/mL (194.6 mM)
• Punto de fusión (°C): 104 - 112 °C

Referencias

1. Hong Liu, Yang Huang, Jing Yang, Xuejiao Xu, Qiaomei Dai, Yuwei Zhang, Li Zhao, Mengdi Zhang, Jing Zhang, Tonghui Liu, Lili Zhong.  (2023)  Involvement of estrogen receptor activation in kaempferol-3-O-glucoside's protection against aging-related cognition impairment and microglial inflammation.  EXPERIMENTAL CELL RESEARCH,      [PMID:37926343] [10.1016/j.yexcr.2023.113849]

2. Xiu Yanghui, Su Yu, Gao Lihua, Yuan Hui, Xu Sennan, Liu Ying, Qiu Yan, Liu Zhen, Li Yuhang.  (2023)  Corylin accelerated wound healing through SIRT1 and PI3K/AKT signaling: a candidate remedy for chronic non-healing wounds.  Frontiers in Pharmacology,      [PMID:37266148] [10.3389/fphar.2023.1153810]

3. Yu Bi, Ziyi Xie, Xiang Cao, Huanyu Ni, Shengnan Xia, Xinyu Bao, Qinyue Huang, Yun Xu, Qingxiu Zhang.  (2024)  Cedrol attenuates acute ischemic injury through inhibition of microglia-associated neuroinflammation via ERβ-NF-κB signaling pathways.  BRAIN RESEARCH BULLETIN,      [PMID:39414157] [10.1016/j.brainresbull.2024.111102]

4. Su Qi, Chen Kun, Ren Jiayan, Zhang Yu, Han Xu, Leong Sze Wei, Wang Jingjing, Wu Qing, Tu Kaihui, Sarwar Ammar, Zhang Yanmin.  (2024)  Hypoxia drives estrogen receptor β-mediated cell growth via transcription activation in non-small cell lung cancer.  JOURNAL OF MOLECULAR MEDICINE-JMM,      [PMID:39420137] [10.1007/s00109-024-02496-8]

5. Xiaomin Su, Yang Wang, Xifeng Qin, Yaqiong Xiao, Boshu Ouyang, Lina Hu, Lin Kang, Ruizhe Xu, Ce Xu, Zanya Sun, Chenyu Sun, Huishu Guo, Zhiqing Pang, Shun Shen.  (2025)  HIFU-Driven Targeted Pyroptosis Therapy in Basal-Like Breast Cancer.  Advanced Science,      [PMID:40946176] [10.1002/advs.202503830]

6. Yawen Li, Yishan Li, Kunping Yang, Wanjie Liu, Ming Yang, Shuo Wang, Wei Feng, Guangfu Lv, Jiaming Sun.  (2025)  Screening of ERβ-Targeted Antipostmenopausal Osteoporosis Chemical Constituents From Cornus officinalis Based on Affinity Ultrafiltration and UHPLC-Q-Exactive Orbitrap MS.  BIOMEDICAL CHROMATOGRAPHY,  40  (1): (e70270).  [PMID:41311205] [10.1002/bmc.70270]

7. Yun Deng, Shujun Yi, Yu Zheng, Rouyi Wang, Fang Liu, Wenjue Zhong, Lingyan Zhu.  (2026)  Gestational Exposure to Tri-n-butyl Phosphate Induces Maternal Insulin Resistance and Glucose Intolerance by Antagonizing Estrogen Receptor Alpha.  ENVIRONMENTAL SCIENCE & TECHNOLOGY,      [PMID:] [10.1021/acs.est.5c14462]