Estrogen receptor modulator 1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。已发现它在ER阳性内分泌抗药性乳腺癌细胞系中具有雌激素样和抗增殖作用,且这些细胞系过度表达蛋白激酶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 | 242.29 |
| SMILES Code | OC1=CC=C(C=C(C2=CC=C(O)C=C2)S3)C3=C1 |
| MDL No. | MFCD16619490 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | MDGWZLQPNOETLH-UHFFFAOYSA-N |
| Pubchem ID | 445920 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
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 |
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