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CAS No.: 63676-22-2

Estrogen receptor modulator 1 Catalog No. CSN25302

Synonyms: RALOXIFENE CORE;BTC

Estrogen receptor modulator 1 is an orally active and selective estrogen receptor modulator (SERM), with a pIC50 of 0.46. It has been found to be both estrogenic and antiproliferative in ER-positive endocrine-resistant breast cancer cell lines that overexpress protein kinase C alpha (PKCα).

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技术信息

生物活性

描述A large proportion of breast cancer patients have a tumor expressing estrogen receptor (ER). Compounds that block the effects of estrogen in tumor tissues are considered as promising therapeutic options for breast cancer patients. Estrogen receptor modulator 1 is a selective and orally active estrogen receptor modulator with a pIC50 of 0.46^[1]. Estrogen receptor modulator 1 at a concentration of 100 nM stimulated the proliferation of T47D:A18/neo cells compared to the control group. The incubation with 100 nM estrogen receptor modulator 1 also increased colony formation in T47D:A18/neo cells, but prevented T47D:A18/PKCα and T47D:A18-TAM1 colony formation. Estrogen receptor modulator 1 at 100 nM also induced apoptosis and inhibited growth of MCF-7:5C cells. In athymic mice inoculated with T47D:A18/PKCα cells, oral administration with estrogen receptor modulator 1 (1.5 mg/day) for two weeks significantly reduced tumor volume compared to the non-treated group. Daily administration of estrogen receptor modulator 1 (1.5 mg/day) for two weeks also resulted in significant tumor regression in mice with T47D:A18-TAM1 xenograft^[2].
参考文献

[1] Brogi S, Papazafiri P, Roussis V, Tafi A. 3D-QSAR using pharmacophore-based alignment and virtual screening for discovery of novel MCF-7 cell line inhibitors. Eur J Med Chem. 2013;67:344-351. doi:10.1016/j.ejmech.2013.06.048
[2] Molloy ME, White BE, Gherezghiher T, et al. Novel selective estrogen mimics for the treatment of tamoxifen-resistant breast cancer. Mol Cancer Ther. 2014;13(11):2515-2526. doi:10.1158/1535-7163.MCT-14-0319

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.1272 mL
- 20.6362 mL
- 41.2723 mL
- 5 mM
- 0.8254 mL
- 4.1272 mL
- 8.2545 mL
- 10 mM
- 0.4127 mL
- 2.0636 mL
- 4.1272 mL

技术信息

CAS号

63676-22-2

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H10O2S

运输

蓝冰

分子量

242.29

别名

RALOXIFENE CORE;BTC

溶解度

DMSO	48.0 mg/mL (198.1 mM)
Water	Insoluble
Ethanol	35.0 mg/mL (144.5 mM)

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Estrogen receptor modulator 1 Catalog No. CSN25302

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