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Fulvestrant

Indications and Usage Mechanisms of Action Pharmacokinetics Adverse reactions
Fulvestrant
Fulvestrant
CAS No.
129453-61-8
Chemical Name:
Fulvestrant
Synonyms
ZD 9238;FASLODEX;zd182780;zm182780;Fulvtrant;Fulvestran;ICH-182780;ICI-187280;Fulvstrant;ICI 182,780
CBNumber:
CB0698542
Molecular Formula:
C32H47F5O3S
Formula Weight:
606.77
MOL File:
129453-61-8.mol

Fulvestrant Properties

Melting point:
104-106°C
storage temp. 
2-8°C
solubility 
DMSO: >5mg/mL
form 
powder
InChIKey
VWUXBMIQPBEWFH-WCCTWKNTSA-N
CAS DataBase Reference
129453-61-8(CAS DataBase Reference)

SAFETY

WGK Germany  3
RTECS  KG7623000
Hazardous Substances Data 129453-61-8(Hazardous Substances Data)

Fulvestrant price More Price(8)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich I4409 Fulvestrant >98% (HPLC) 129453-61-8 25mg $143 2018-11-20 Buy
Sigma-Aldrich 1286650 Fulvestrant United States Pharmacopeia (USP) Reference Standard 129453-61-8 200mg $863 2018-11-20 Buy
Cayman Chemical 10011269 Fulvestrant ≥98% 129453-61-8 1mg $15 2018-11-19 Buy
Cayman Chemical 10011269 Fulvestrant ≥98% 129453-61-8 5mg $68 2018-11-19 Buy
Sigma-Aldrich Y0001399 Fulvestrant European Pharmacopoeia (EP) Reference Standard 129453-61-8 y0001399 $179 2018-11-23 Buy

Fulvestrant Chemical Properties,Uses,Production

Indications and Usage

Fulvestrant is a muscle injection drug developed by the company AstraZeneca and is suitable for treating postmenopausal women with estrogen receptor-positive metastasized breast cancer whose condition continued to worsen despite antiestrogen treatment. Fulvestrant is the only antiestrogen drug that can be widely clinically used following unsuccessful tamoxifen treatment. This drug is a type of endocrine therapy, so it will not cause any adverse effects commonly seen in chemotherapy, giving it relatively good patient compliance. Multiple clinical trials have found that 250mg Fulvestrant is effective and consistently safe as a second line of treatment for advanced breast cancer.

Mechanisms of Action

Many breast cancer cells contain estrogen receptors (ER), so estrogen stimulates breast cancer growth. Fulvestrant is a steroid estrogen receptor antagonist, and its chemical structure is similar to estradiol, except that its 7α position contains a linking group. Fulvestrant is a 17β-estradiol alkylamine analogue, and it binds with, prevents, and decreases ER to inhibit the estrogen signal transduction pathway. It binds competitively with ER, has a similar affinity with ER as estrogen, and inhibits gene activation stimulated by estrogen, thus affecting necessary estrogen-related processes in cell circulation. Its fulvastans have a similar affinity with ER as estrogen and is 100 times that of tamoxifen.

Pharmacokinetics

Fulvestrant has a relatively poor oral bioavailability, so it is commonly injected into the muscle with lipids as excipients. In an open, random and multicenter study on postmenopausal women with advanced breast cancer, one 5ml or 2 2.5ml dosages containing 250mg were injected, and their pharmacokinetics and poisonous side effects did not differ greatly, while its blood concentration was dose-dependent and had individual differences. In the 7-day treatment period, serum LH, FSH or SBHG levels did not change significantly. This drug does not pass through the blood-brain barrier and will not cause side effects such as vasomotor symptoms.

Adverse reactions

Fulvestrant causes relatively fewer side effects, including brief vaginal bleeding, body odor change, and sleepwalking. There have not been any reports of effects such as vaginal dryness, weight gain, blood clotting abnormalities, thrombus formation and libido change, and characteristics such as facial flushing and sweating are not affected. A small-scale stage III clinical trial on 19 women with metastasized breast cancer who used this drug showed that its clinical efficacy was 67% and there were no serious safety issues. It showed that continuous monthly injections were crucial and that it was well-tolerated, with only slight swelling and paint at injection site, while facial flushing, uterine lining thickness, sex hormone binding globulin levels, follicle stimulating hormones levels, and luteinizing hormone levels all showed no change.

Chemical Properties

White or almost white powder.

Uses

A novel steroidal estrogen antagonist reported to lack any partial agonist activity. Antineoplastic (hormonal).

Uses

antiestrogen

Definition

ChEBI: A 3-hydroxy steroid that is 17beta-estradiol in which the 7alpha hydrogen has been replaced by a nonyl group in which one of the hydrogens of the terminal methyl has been replaced by a (4,4,5,5,5-pentafluoropentyl)sulfinyl group. An estrogen receptor antagonist, it is used in the treatment of breast cancer.

brand name

Faslodex (AstraZeneca).

Biological Activity

A high affinity estrogen receptor antagonist (IC 50 = 0.29 nM), devoid of any partial agonism both in vitro and in vivo . Also high affinity agonist at the membrane estrogen receptor GPR30.

Fulvestrant Preparation Products And Raw materials

Raw materials

Preparation Products


Fulvestrant Suppliers

Global( 238)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Lianyungang happen teng technology co., LTD
15950718863
wang666xt@163.com CHINA 305 58
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853
+86-755-23284190 sales@tianpharm.com CHINA 308 58
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19953 60
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3217 55
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 22049 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20786 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32651 55
Hangzhou FandaChem Co.,Ltd.
0086 158 5814 5714 (Mobile; WhatsApp; Telegram)
+86-571-56059825 fandachem@gmail.com CHINA 2097 55
PI & PI BIOTECH INC.
020-81716320
020-81716319 Sales@pipitech.com CHINA 2548 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 E-mail:sales03@shyrchem.com
+86-21-34979012 sales03@shyrchem.com CHINA 663 60

View Lastest Price from Fulvestrant manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-03-19 Fulvestrant 129453-61-8
129453-61-8
US $10.00 / KG 10G 99.5% 10MT Hubei XinRunde Chemical Co., Ltd.
2018-12-19 Irsogladine maleate
129453-61-8
US $1.00 / kg 1kg 95%-99% 100kg career henan chemical co
2018-12-19 Fulvestrant
129453-61-8
US $1.00 / kg 1kg 95%-99% 100kg career henan chemical co

129453-61-8(Fulvestrant)Related Search:


  • (7a,17b)-7-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol
  • 7A,17B-[9[(4,4,5,5,5-PENTAFLUOROPENTYL)SULFINYL]NONYL]ESTRA-1,3,5(10)-TRIENE-3,17-DIOL
  • (7alpha,17beta)-nonyl)
  • estra-1,3,5(10)-triene-3,17-diol,7-(9-((4,4,5,5,5-pentafluoropentyl)sulfinyl)
  • Fulvtrant
  • 7-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]- (7α,17β)-estra-1,3,5(10)-triene-3,17-diol
  • (7a,17b)-7-[9-[(4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol Fulvestrant ICI 182,780
  • Fulvestrant for system suitability
  • Fulvestran
  • (7R,8R,9S,13S,14S,17S)-13-methyl-7-(9-((4,4,5,5,5-pentafluoropentyl)sulfinyl)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol
  • Fulvestrant Impurity
  • Fulvestrant Vetec(TM) reagent grade, >98%
  • Fulvestrant, >=98%
  • Fulvestrant (Steroids)
  • Fulvestrant IMP
  • ICI 182,780
  • FULVESTRANT
  • FULVESTRANT-13C1-D2
  • FASLODEX
  • Fulvestrant 129453-61-8
  • Astrazeneca
  • BioChemical
  • Cell Biology
  • Cell Signaling and Neuroscience
  • Hormones
  • Steroid Hormones
  • 129453-61-8
  • 129435-61-8
  • C32H47F5O3S
  • zd182780
  • zm182780
  • (717b)- 7-[9-[4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol
  • ICH-182780
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  • ICI-187280
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  • (7,17)-7-[9-[4,4,5,5,5-Pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol
  • Faslodex, ICI 182,780, ZD 182780, ZD 9238, ZM 182780, (7a,17b)-7-[9-[(4,4,5,5,5pentafluoropentyl)Sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol
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  • Fulvestrant Estra-1,3,5(10)-triene-3,17-diol, 7-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]-, (7 ,17 )-
  • Fulvestrant (Faslodex)
  • ZD 9238
  • Fulvestrant(ICI 182,780)
  • (1S,9R,10R,11S,14S,15S)-15-Methyl-9-{9-[(R)-(4,4,5,5,5-pentafluoropentane)sulfinyl]nonyl}tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-2,4,6-triene-5,14-diol
  • FASLODEX
  • Anti-cancer&immunity
  • Inhibitors
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Nuclear Receptors
  • Chiral Reagents
  • Steroids
  • Sulfur & Selenium Compounds
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  • Estrogen
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