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Fulvestrant is white powder, while it's Molecular Formula is C32H47F5O3S. antiestrogen
The CAS number of Fulvestrant is 129453-61-8.
More information of Fulvestrant 129453-61-8 are:
Synonyms |
Faslodex;Estra-1,3,5(10)-triene-3,17-diol,7-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]-, (7a,17b)-;ICI 182780;ZD 182780;ZD 9238;ZM 182780; |
CAS Number |
129453-61-8 |
Molecular Formula |
C32H47F5O3S |
Molecular Weight |
606.781 |
Density |
1.201 g/cm3 |
Melting Point |
104-106°C |
Boiling Point |
674.8 °C at 760 mmHg |
Flash Point |
361.9 °C |
HS CODE |
2937230000 |
PSA |
76.74000 |
LogP |
9.54830 |
Pka |
10.27±0.70(Predicted) |
Fulvestrant was launched in the US as a novel once monthly injectable steroidal estrogen antagonist for the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following estrogen therapy. This 7a-alkylsulphinyl derivative of estradiol can be prepared in 10 steps from 6,7- didehydro-19-nor-testosterone by successive conjugate addition of the organocuprate derived from O-protected 9-bromononan-l-o1 followed by aromatization of the resulting enone, then activation of the protected primary alcohol, substitution with 4,4,5,5,5- pentafluoropentanthiol and oxidation to the sulfoxide. Fulvestrant is the first “pure” estrogen antagonist from a novel class known as selective estrogen receptor down regulators (SERDs). It binds to the estrogen receptor (ER), with affinity close to that of estradiol and 100 fold greater than that of tamoxifen (a partial estrogen antagonist), preventing estrogen-stimulated gene activation, thereby interfering with the estrogenrelated processes essential for cell-cycle completion. Fulvestrant also appears to downregulate the ER by 80-90% often to non detectable level both in vitro and in vivo. In comparison to tamoxifen, fulvestrant is devoid of systemic estrogenic activity, it displays no uterotrophic activity and is able to block the uterine stimulation of estradiol or tamoxifen. Furthermore, fulvestrant completely blocks the cell growth in tamoxifen-resistant breast cancer cell-lines and prevents growth of tamoxifen resistant tumor in mice. In clinical trials, it was also shown that fulvestrant is comparable to anastrozole (a third generation aromatase inhibitor) both in efficacy and tolerability in postmenopausal women with tamoxifen-resistant advanced breast cancers.
InChI:InChI=1/C32H47F5O3S/c1-30-17-15-26-25-12-11-24(38)21-23(25)20-22(29(26)27(30)13-14-28(30)39)10-7-5-3-2-4-6-8-18-41(40)19-9-16-31(33,34)32(35,36)37/h11-12,21-22,26-29,38-39H,2-10,13-20H2,1H3/t22?,26-,27+,28+,29-,30+,41?/m1/s1
Articles related to Fulvestrant:
Article |
Source |
An Efficient Regioselective Preparation of Fulvestrant |
Pichandi Mohanraj, Senthil Kumar,Tulasi, Ramachar,Chidambaram Subramanian, Venkatesan , p. 362 - 368 (2021) |
Impurity control method of fulvestrant |
- Paragraph 0061-0063, (2020/09/23) |
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