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Chemical compound
FERb 033
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2-Chloro-3′-fluoro-3,4′-dihydroxy-[1,1-biphenyl]-4-carboxaldehyde oxime
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CAS Number | |
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ChemSpider | |
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UNII | |
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Formula | C13H9ClFNO3 |
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Molar mass | 281.67 g·mol−1 |
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3D model (
JSmol) | |
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c1cc(c(cc1c2ccc(c(c2Cl)O)/C=N/O)F)O
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InChI=1S/C13H9ClFNO3/c14-12-9(3-1-8(6-16-19)13(12)18)7-2-4-11(17)10(15)5-7/h1-6,17-19H/b16-6+ Key:LRRMQNGSYOUANY-OMCISZLKSA-N
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FERb 033 is a
synthetic,
nonsteroidal
estrogen that was
synthesized in 2009 and is used in
scientific research.
[1]
[2] It is a
potent and
selective
ERβ
agonist (Ki = 7.1 nM,
EC50 = 4.8 nM), with 62-fold selectivity for the ERβ over the
ERα.
[1]
[2]
See also
References
- ^
a
b Minutolo F, Bertini S, Granchi C, Marchitiello T, Prota G, Rapposelli S, Tuccinardi T, Martinelli A, Gunther JR, Carlson KE, Katzenellenbogen JA, Macchia M (2009). "Structural evolutions of salicylaldoximes as selective agonists for estrogen receptor beta". J. Med. Chem. 52 (3): 858–67.
doi:
10.1021/jm801458t.
PMID
19128016.
- ^
a
b Reese JM, Suman VJ, Subramaniam M, Wu X, Negron V, Gingery A, Pitel KS, Shah SS, Cunliffe HE, McCullough AE, Pockaj BA, Couch FJ, Olson JE, Reynolds C, Lingle WL, Spelsberg TC, Goetz MP, Ingle JN, Hawse JR (2014).
"ERβ1: characterization, prognosis, and evaluation of treatment strategies in ERα-positive and -negative breast cancer". BMC Cancer. 14: 749.
doi:
10.1186/1471-2407-14-749.
PMC
4196114.
PMID
25288324.
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ERTooltip Estrogen receptor | Agonists |
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2-Hydroxyestradiol
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2-Hydroxyestrone
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3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol
-
3α-Androstanediol
-
3α,5α-Dihydrolevonorgestrel
-
3β,5α-Dihydrolevonorgestrel
-
3α-Hydroxytibolone
-
3β-Hydroxytibolone
-
3β-Androstanediol
-
4-Androstenediol
-
4-Androstenedione
-
4-Fluoroestradiol
-
4-Hydroxyestradiol
-
4-Hydroxyestrone
-
4-Methoxyestradiol
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4-Methoxyestrone
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5-Androstenediol
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7-Oxo-DHEA
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7α-Hydroxy-DHEA
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7α-Methylestradiol
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7β-Hydroxyepiandrosterone
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8,9-Dehydroestradiol
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8,9-Dehydroestrone
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8β-VE2
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10β,17β-Dihydroxyestra-1,4-dien-3-one (DHED)
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11β-Chloromethylestradiol
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17α-Dihydroequilenin
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17α-Dihydroequilin
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17α-Epiestriol (16α-hydroxy-17α-estradiol)
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17α-Ethynyl-3α-androstanediol
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17α-Ethynyl-3β-androstanediol
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17β-Dihydroequilenin
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17β-Methyl-17α-dihydroequilenin
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RU-16117
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- Others (e.g.,
agnuside,
rotundifuran)
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Mixed (
SERMsTooltip Selective estrogen receptor modulators) | |
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Antagonists |
- Coregulator-binding modulators:
ERX-11
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GPERTooltip G protein-coupled estrogen receptor | Agonists | |
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Antagonists | |
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Unknown | |
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