1443752-76-8
1443752-76-8 結構式
基本信息
中文別名
化合物 T12312 英文別名
OP-1074OP 1074,OP1074
2H-1-Benzopyran-7-ol, 3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-[(3R)-3-methyl-1-pyrrolidinyl]ethoxy]phenyl]-, (2S)-
物理化學性質(zhì)
沸點643.9±55.0 °C(Predicted)
密度1.210±0.06 g/cm3(Predicted)
酸度系數(shù)(pKa)9.70±0.40(Predicted)
形態(tài)Solid
顏色White to off-white
常見問題列表
生物活性
OP-1074，純抗雌激素藥，是一種選擇性 ER 降解劑 (PA-SERD)，對 ERα 和 ERβ 具有特異性抗雌激素活性，可抑制 17β-estradiol (E2)-刺激的轉錄活性，IC50 分別為 1.6 和 3.2 nM。靶點
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ERα
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ERβ
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體外研究
OP-1074 (0-100?nM; 24 hours) inhibits ?MCF-7 cells? and CAMA-1 cells proliferation?with IC50 values of 6.3 and 9.2 nM, respectively. OP-1074 (100?nM; 24 hours) destabilizatizes ERα protein expression in MCF-7 and CAMA-1 cells.
Cell Viability Assay
| Cell Line: | MCF-7 cells, CAMA-1 cells |
| Concentration: | 0 nM, 10 nM,100 nM |
| Incubation Time: | 24 hours |
| Result: | Inhibited breast cancer cell proliferation. |
Western Blot Analysis
| Cell Line: | MCF-7 cells, CAMA-1 cells |
| Concentration: | 100 nM |
| Incubation Time: | 24 hours |
| Result: | Downregulated ERα protein expression. |