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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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]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 63676-22-2 |
分子式 | C14H10O2S |
分子量 | 242.293 |
别名 | |
运输 | 蓝冰 |
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 |