Fulvestrant

SKU: orb1306347

特色

描述

Fulvestrant is a potent estrogen receptor antagonist (IC50=9.4 nM) and a GPR30 agonist. It exhibits antitumor activity by suppressing proliferation and promoting apoptosis and autophagy in breast cancer research, applicable in both in vitro and in vivo experimental models.

研究领域

Neuroscience

图片与验证

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关键属性

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CAS 号	129453-61-8
MW	606.8
纯度	>98%
分子式	C₃₂H₄₇F₅O₃S
SMILES	[H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@]1([H])c3ccc(O)cc3C[C@@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)[C@@]21[H]
靶点	Transcription factor
溶解性	Soluble in DMSO (up to 100 mg/ml) or in Ethanol (up to 50 mg/ml).

生物活性

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靶点 IC50	ER-positive MCF-7 cells:0.29 nM\|HEK293 cells:0.78 nM\|LNCaP cells:18 nM\|MDA-MB-231 cells:196.3 μM\|MDA-MB-231 cells:> 1 µM\|MCF-7 cells:0.8 nM\|MCF-7 cells:0.044 μM\|MCF-7 cells:< 0.1 nM\|COS-7 cells:3.8 nM\|T47D cells:0.0012 μM\|ERR:9.4 nM (cell free)\|MCF-7 cells/TAMR-1 cells:1.8 nM
体内	METHODS: To assay anti-tumor activity in vivo, Fulvestrant (25-200 mg/kg, 5% DMSO/95% corn oil) was injected subcutaneously four times per week for four weeks into Nu/J mice bearing tamoxifen-resistant (TamR) tumors. RESULTS: Significant inhibition of tumor growth was observed at all doses of Fulvestrant, and no significant differences were detected between doses. METHODS: To assay anti-tumor activity in vivo, Fulvestrant (5 mg/mouse) was injected subcutaneously into nude mice with in situ established ER+ mammary carcinomas twice weekly for twenty-four days. RESULTS: Fulvestrant treatment resulted in a significant reduction in tumor growth.
体外	METHODS: ER-positive MCF-7 and ER-negative MDA-MB-231 cells were treated with Fulvestrant (0.01-10000 nM) for 6 days, and the cell growth rate was measured by crystal violet staining. RESULTS: Fulvestrant inhibited the growth of MCF-7 cells with an IC50 of 0.8 nM. Fulvestrant did not inhibit the growth of MDA-MB-231 cells with an IC50 greater than 1 µM. METHODS: Human breast cancer cells MCF-7 were treated with Fulvestrant (100 nM) for 0.25-6 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: ERα protein expression was reduced in a time-dependent manner when MCF-7 cells were exposed to Fulvestrant.
细胞研究	In brief, hippocampi were dissected from the brains of embryonic day 18 Sprague-Dawley rat fetuses, treated with 0.02% trypsin in Hanks' balanced salt solution (137 mM NaCl, 5.4 mM KCl, 0.4 mM KH2PO4, 0.34 mM Na2HPO4·7H2O, 10.0 mM glucose, and 10.0 mM HEPES) at 37°C for 5 min and dissociated by repeated passage through a series of fire-polished constricted Pasteur pipettes. For intracellular Ca2+ imaging analyses, approximately 10^4 cells were seeded onto poly-D-lysine (10 μg/ml)-coated 22-mm coverslips in covered 35-mm Petri dishes. For neuroprotection and Western immunoblotting analyses, approximately 10^6 cells/ml were seeded onto poly-D-lysine-coated solid black and clear bottom 96-well culture plates and 60-mm Petri dishes, respectively. Cells were grown in phenol-red free neurobasal medium supplemented with B27, 5 U/ml penicillin, 5 μg/ml streptomycin, 0.5 mM glutamine, and 25 μM glutamate at 37°C in 10% CO2 for the first 3 days and NBM without glutamate afterward. Cultures grown in serum-free NBM yields approximately 99.5% neurons and 0.5% glial cells .
动物研究	MCF-7 cells were suspended in culture medium (no serum) and inoculated s.c. into the flank of adult female nude mice (0.1 ml/approximately 5 x 10^6 cells). Mice were maintained in a clean environment and were given sterile food and water. Estrogen supplementation was provided by ethynyl estradiol at 1 μg/ml in the water. Antiestrogen treatment was initiated when tumor diameter attained a minimum of 0.5 cm. The Br10 tumor at passage 49 was established by implantation of 1-2-mm^3 tumor fragments into the flank of anesthetized intact adult female nude mice. After 3 passages a reproducible pattern of growth was established without additional estrogen supplementation. Approximately two-thirds of animals established progressively growing tumors which attained measurable size (area, ≥70 mm2) after 6-7 weeks. Antiestrogen treatment was initiated at the time of transplantation. Tamoxifen was administered once daily p.o. at a dose of 10 mg/kg (1 ml/100 g body weight of aqueous dispersion in 0.5% Tween 80) and ICI 182,780 as a single s.c. injection of 5 mg/mouse (50 mg/ml in arachis oil). Tumor size was assessed weekly as the product of caliper measurements of the largest diameter and the axis perpendicular to it .

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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ICI 182780; ZD-9238

相似产品

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ZB716 (Fulvestrant-3 Boronic Acid) [orb573459]
纯度：
>98%
CAS 号：
1853279-29-4
MW:
634.59
分子式：
C₃₂H₄₈BF₅O₄S
可选规格： 5 mg
BY13 [orb3135175]
可选规格： 50 mg, 10 mg
Fulvestrant impurity 5 [orb3215957]
CAS 号：
2170200-14-1
MW:
604.76
分子式：
C₃₂H₄₅F₅O₃S
可选规格： 10 mg, 50 mg
Fulvestrant 3-β-D-Glucuronide [orb3137139]
CAS 号：
261506-27-8
MW:
782.9
分子式：
C₃₈H₅₅F₅O₉S
可选规格： 5 mg, 50 mg
Fulvestrant (S enantiomer) [orb1709659]
CAS 号：
1316849-17-8
MW:
606.77
分子式：
C₃₂H₄₇F₅O₃S
可选规格： 25 mg, 100 mg, 50 mg

质量保证

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化合物标识

PubChem CID

104741 ↗

关键属性

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暂无计算属性。

实验方案信息

查看更多实验方案

纯度：	>98%
CAS 号：	1853279-29-4
MW:	634.59
分子式：	C₃₂H₄₈BF₅O₄S

CAS 号：	2170200-14-1
MW:	604.76
分子式：	C₃₂H₄₅F₅O₃S

CAS 号：	261506-27-8
MW:	782.9
分子式：	C₃₈H₅₅F₅O₉S

CAS 号：	1316849-17-8
MW:	606.77
分子式：	C₃₂H₄₇F₅O₃S

Fulvestrant

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

ZB716 (Fulvestrant-3 Boronic Acid) [orb573459]

BY13 [orb3135175]

Fulvestrant impurity 5 [orb3215957]

Fulvestrant 3-β-D-Glucuronide [orb3137139]

Fulvestrant (S enantiomer) [orb1709659]

质量保证

化合物标识

关键属性

实验方案信息

可选规格