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Estrogen receptor modulator 1

  Cat. No.:  DC28269   Featured
Chemical Structure
63676-22-2
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More than 5000 active chemicals with high quality for research!
Field of application
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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 63676-22-2
SMILES: OC1C=C2SC(C3C=CC(O)=CC=3)=CC2=CC=1
Formula: C14H10O2S
M.Wt: 242.29
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [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.
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].
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.
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.
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.
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