Estrogen receptor modulator 1

Names

[ Name ]:
Estrogen receptor modulator 1

[Synonym ]:
2-(4-hydroxyphenyl)-6-hydroxybenzo[b]thiophene
2-(4-Hydroxyphenyl)benzo[b]thiophen-6-ol
2-(4-Hydroxyphenyl)benzo[b]thiophene-6-ol
6-hydroxy-2-(4-hydroxyphenyl)benzo<b>thiophene
ZTW
RALOXIFENE CORE
benzthiophene compound,3

Biological Activity

[Description]:

Estrogen receptor modulator 1 (compound 18) is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. Estrogen receptor modulator 1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors[1][2].

[Related Catalog]:

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Cancer

[In Vitro]

Estrogen receptor modulator 1 (compound 18) (100 nM; 10 days) inhibits T47D:A18/PKCα and T47D:A18-TAM1 colony formation[2]. Estrogen receptor modulator 1 (100 nM; 9 days) significantly inhibits the growth of MCF-7:5C cell, and induces apoptosis in these cells 6 days[2]. Cell Proliferation Assay[2] Cell Line: T47D:A18/PKCα and T47D:A18-TAM1 cells Concentration: 100 nM Incubation Time: 10 days Result: Inhibit T47D:A18/PKCα and T47D:A18-TAM1 colony formation. Cell Viability Assay[2] Cell Line: MCF-7:5C cells Concentration: 100 nM Incubation Time: 9 days Result: Significantly inhibited the growth of MCF-7:5C cells.

[In Vivo]

Estrogen receptor modulator 1 (1.5 mg/animal; p.o. ; daily for 2 weeks) results in regression of T47D:A18/PKCα tumors[2]. Animal Model: 4-6 week old athymic mice (Harlan-Sprague-Dawley)[2] Dosage: 1.5 mg/animal Administration: p.o. ; daily for 2 weeks Result: Significantly reduced tumor volume.

[References]

[1]. Brogi S, et al. 3D-QSAR using pharmacophore-based alignment and virtual screening for discovery of novel MCF-7 cell line inhibitors. Eur J Med Chem. 2013 Sep;67:344-51.

[2]. Molloy ME, et al. Novel selective estrogen mimics for the treatment of tamoxifen-resistant breast cancer. Mol Cancer Ther. 2014 Nov;13(11):2515-26.

Chemical & Physical Properties

[ Density]:
1.383

[ Boiling Point ]:
477ºC at 760 mmHg

[ Melting Point ]:
295 °C(dec.)

[ Molecular Formula ]:
C₁₄H₁₀O₂S

[ Molecular Weight ]:
242.29300

[ Flash Point ]:
242.3ºC

[ Exact Mass ]:
242.04000

[ PSA ]:
68.70000

[ LogP ]:
3.97950

[ Index of Refraction ]:
1.742

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

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