151533-34-5

151533-34-5 structure

Name: rac-Acolbifene
Chemical Name: 2-[4-[2-(1-piperidino)ethoxy]phenyl]-3-(4-hydroxyphenyl)-4-methyl-7-hydroxy-2H-1-benzopyran
CAS Number: 151533-34-5
Molecular Formula: C₂₉H₃₁NO₄
Molecular Weight: 457.56100
Catalog: Research Areas Cancer
Create Date: 2017-11-07 09:18:02
Modify Date: 2024-01-12 11:39:35
(Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380[1].

Name	2-[4-[2-(1-piperidino)ethoxy]phenyl]-3-(4-hydroxyphenyl)-4-methyl-7-hydroxy-2H-1-benzopyran
Synonyms	7-hydroxy-3-(4'-hydroxyphenyl)-4-methyl-2-(4"-(2"'-piperidinoethoxy)phenyl)-2H-benzopyran rac-Acolbifene 2-[4-[2-(1-piperidino)ethoxy]phenyl]-3-(4-hydroxyphenyl) -4-methyl-7-hydroxy-2H-1-benzopyran

Description	(Rac)-Acolbifene (EM-343; (Rac)-EM-652) is the racemic form of EM652 (estrogen receptor antagonist), has anti-estrogenic and estrogenic activities. (Rac)-Acolbifene (EM-343; (Rac)-EM-652) contains a piperidine ring, shows good pharmacological profile,relative binding affinity (RBA)=380[1].
Related Catalog	Signaling Pathways >> Others >> Estrogen Receptor/ERR Research Areas >> Cancer
In Vitro	(Rac)-Acolbifene (EM-343; (Rac)-EM-652) shows a inhibitory effect in T-47D cells with an IC50 value of 0.110 nM[1]. Cell Viability Assay[1] Cell Line: T-47D cells Concentration: 0.110 nM Incubation Time: 72 hours Result: Inhibited T-47D cells growth.
In Vivo	(Rac)-Acolbifene (orally adminstration; 7.5 nM, 75 nM; 9 days; once daily) shows a good pharmacological profile in ovariectomized mice, shows 63% and 84% antiuterotrophic inhibitions at the 7.5 and 75 nM doses, respectively (PK study, ovariectomized mice)[1].
References	[1]. Gauthier S1,et al.Synthesis and structure-activity relationships of analogs of EM-652 (acolbifene), a pure selective estrogen receptor modulator. Study of nitrogen substitution.J Enzyme Inhib Med Chem. 2005 Apr;20(2):165-77.

Precursor 0
DownStream 1
182167-02-8