CMP8

Names

[ Name ]:
CMP8

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
703.5±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₃₃H₃₄ClNO₃

[ Molecular Weight ]:
528.081

[ Flash Point ]:
379.3±32.9 °C

[ Exact Mass ]:
527.222717

[ LogP ]:
8.38

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.667

Related Compounds

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