Fulvestrant

SKU: orb1306347

Description

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.

Research Area

Cell Biology, Metabolism Research

Images & Validation

−

Key Properties

−

CAS Number	129453-61-8
MW	606.77
Purity	99.77%
Formula	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]
Target	Estrogen Receptor/ERR,Autophagy,Estrogen/progestogen Receptor,Apoptosis
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:6.07 mg/mL (10 mM);Ethanol:30.3 mg/mL (49.94 mM);DMSO:260 mg/mL (428.5 mM)

Bioactivity

−

Target 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 Read more...
In Vivo	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. Read more...
In Vitro	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. Read more...
Cell Research	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 . Read more...
Animal Research	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 . Read more...

Storage & Handling

−

Storage	keep away from direct sunlight,keep away from moisture,store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

−

progestogenReceptor, progestogen Receptor, ZD9238, ZD-9238, ZD 9238, ZM 182780, ZM182780, ZM-182780, inhibit, Fulvestrant, Estrogen Receptor, Estrogen Receptor/ERR, EstrogenReceptor, ERR, ER, ICI 182780, ICI182780, ICI-182780, Inhibitor, Autophagy, Apoptosis

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID

104741 ↗

Key Properties

−

No computed properties available.

Documents Download

Datasheet

Product Information

Download

Request a Document

Protocol Information

Find More Protocols

Fulvestrant (orb1306347)

Based on 0 reviews

Participating in our Biorbyt product reviews program enables you to support fellow scientists by sharing your firsthand experience with our products.

No reviews yet

Purity:	>98%
CAS Number:	1853279-29-4
MW:	634.59
Formula:	C₃₂H₄₈BF₅O₄S

CAS Number:	1807900-80-6
MW:	606.77
Formula:	C₃₂H₄₇F₅O₃S

CAS Number:	98008-06-1
MW:	622.77
Formula:	C₃₂H₄₇F₅O₄S

CAS Number:	1316849-17-8
MW:	606.77
Formula:	C₃₂H₄₇F₅O₃S

MW:	609.79
Formula:	C₃₂H₄₇F₅O₃S

Fulvestrant

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Similar Products

ZB716 (Fulvestrant-3 Boronic Acid) [orb573459]

Fulvestrant (R enantiomer) [orb1709660]

Fulvestrant sulfone [orb1737784]

Fulvestrant (S enantiomer) [orb1709659]

Fulvestrant-d3 [orb2299767]

Quality Guarantee

Compound Identifiers

Key Properties

Documents Download

Request a Document

Protocol Information

Fulvestrant (orb1306347)

Step 1: Enter information below

Step 2: Enter the in vivo formulation

Available Sizes

Email

UK Office

US Office

CN Office

Distributors