Estrogen receptor modulator 1

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Estrogen receptor modulator 1 

Estrogen receptor modulator 1 (compound 18) 是一种口服活性选择性雌激素受体 (estrogen receptor) 调节剂 (SERM)，pIC50 为 0.46。Estrogen receptor modulator 1 诱导 Tamoxifen 耐药、激素非依赖性异种移植瘤的消退。

Estrogen receptor modulator 1

Estrogen receptor modulator 1 Chemical Structure

CAS No. : 63676-22-2

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生物活性

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].

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

242.29

Formula

C14H10O2S
CAS 号

63676-22-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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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