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Estrogen receptor modulator 1

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Chemical Structure| 63676-22-2 同义名 : -
CAS号 : 63676-22-2
货号 : A251043
分子式 : C14H10O2S
纯度 : 99%+
分子量 : 242.293
MDL号 : MFCD16619490
存储条件:

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

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(433.36 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.13mL

0.83mL

0.41mL

20.64mL

4.13mL

2.06mL

41.27mL

8.25mL

4.13mL

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