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Fulvestrant

Cayman Chemical Item Number 10011269

ICI 182,780; Faslodex® (CAS 129453-61-8)

Fulvestrant (CAS 129453-61-8)

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Description

Fulvestrant is a potent estrogen receptor (ER) antagonist that works by down-regulating and degrading the estrogen receptor, ERα.1 The prescription drug, Faslodex®, is efficacious in the treatment of estrogen-sensitive breast cancer, in part because it largely lacks agonist activity in relevant tissues.2 However, fulvestrant was found to fully activate ER on rat hippocampal neurons,3 suggesting it might afford protective neurological benefits with aging.

1 Kansra, S., Yamagata, S., Sneade, L., et al. Differential effects of estrogen receptor antagonists on pituitary lactotroph proliferation and prolactin release. Mol Cell Endocrinol 239 27-36 (2005).

2 Addo, S., Yates, R.A., and Laight, A. A phase I trial to assess the pharmacology of the new oestrogen receptor antagonist fulvestrant on the endometrium in healthy postmenopausal volunteers. Br J Cancer 87 1354-1359 (2002).

3 Zhao, L., O'Neill, K., and Brinton, R.D. Estrogenic agonist activity of ICI 182,780 (Faslodex) in hippocampal neurons: Implications for basic science understanding of estrogen signaling and development of estrogen modulators with a dual therapeutic profile. J Pharmacol Exp Ther 319(3) 1124-1132 (2006).

Synonyms
  • ICI 182,780
  • Faslodex®
Formal Name 7α-​[9-​[(4,​4,​5,​5,​5-​pentafluoropentyl)sulfinyl]nonyl]-​estra-​1,​3,​5(10)-​triene-​3,​17β-​diol
CAS Number 129453-61-8
Molecular Formula C32H47F5O3S
Formula Weight 606.8
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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O=S(CCCCCCCCCC1Cc2cc(O)​ccc2C2CC[C@]​3(C)​[C@@H]​(O)​CCC3C12)​CCCC(F)​(F)​C(F)​(F)​F

Background Reading

Kansra, S., Yamagata, S., Sneade, L., et al. Differential effects of estrogen receptor antagonists on pituitary lactotroph proliferation and prolactin release. Mol Cell Endocrinol 239 27-36 (2005).

Addo, S., Yates, R.A., and Laight, A. A phase I trial to assess the pharmacology of the new oestrogen receptor antagonist fulvestrant on the endometrium in healthy postmenopausal volunteers. Br J Cancer 87 1354-1359 (2002).

Zhao, L., O'Neill, K., and Brinton, R.D. Estrogenic agonist activity of ICI 182,780 (Faslodex) in hippocampal neurons: Implications for basic science understanding of estrogen signaling and development of estrogen modulators with a dual therapeutic profile. J Pharmacol Exp Ther 319(3) 1124-1132 (2006).
Size Price Quantity Subtotal
1 mg $15.00 $0.00
5 mg $68.00 $0.00
10 mg $120.00 $0.00
50 mg $525.00 $0.00
Bulk Contact
Cart Total $0.00

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Pricing updated 2012-05-25. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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