851107-28-3

851107-28-3 structure

Name: CMP8
Chemical Name: 9a-(4-Chlorobenzyl)-7-hydroxy-4-{4-[2-(1-piperidinyl)ethoxy]phenyl}-1,2,9,9a-tetrahydro-3H-fluoren-3-one
CAS Number: 851107-28-3
Molecular Formula: C₃₃H₃₄ClNO₃
Molecular Weight: 528.081
Catalog: Research Areas Cancer
Create Date: 2018-07-13 18:41:17
Modify Date: 2024-01-13 19:38:55
CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively[1][2].

Name	9a-(4-Chlorobenzyl)-7-hydroxy-4-{4-[2-(1-piperidinyl)ethoxy]phenyl}-1,2,9,9a-tetrahydro-3H-fluoren-3-one
Synonyms	9a-(4-Chlorobenzyl)-7-hydroxy-4-{4-[2-(1-piperidinyl)ethoxy]phenyl}-1,2,9,9a-tetrahydro-3H-fluoren-3-one 3H-Fluoren-3-one, 9a-[(4-chlorophenyl)methyl]-1,2,9,9a-tetrahydro-7-hydroxy-4-[4-[2-(1-piperidinyl)ethoxy]phenyl]- 9a-(4-chlorobenzyl)-7-hydroxy-4-{4-[2-(piperidin-1-yl)ethoxy]phenyl}-1,2,9,9a-tetrahydro-3H-fluoren-3-one CMP8

Description	CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively[1][2].
Related Catalog	Signaling Pathways >> Others >> Estrogen Receptor/ERR Research Areas >> Cancer
Target	MGERα:29 nM (IC50) MGRERα:41 nM (IC50) hERα:1100 nM (IC50) hERβ:2200 nM (IC50)
In Vivo	CMP8 (Compound 20h) is dosed in male Balb-c mice (4 mg/kg, ip). The plasma concentration after 4 h was 1.5-fold its EC50 in mammalian cells with a Cmax of 0.5 µM after 30 min[1][2].
References	[1]. Miyazaki Y, et al. Destabilizing domains derived from the human estrogen receptor. J Am Chem Soc. 2012 Mar 7;134(9):3942-5. [2]. Kinzel O, et al. A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies. J Med Chem. 2006 Sep 7;49(18):5404-7.