1. Vitamin D Related/Nuclear Receptor
  2. Estrogen Receptor/ERR
  3. ER degrader 5

ER degrader 5 是一种有效的 estrogen receptor (ER) 降解剂。ER degrader 5 具有抗增殖活性。ER degrader 5 可以用于乳腺癌研究。

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ER degrader 5 Chemical Structure

ER degrader 5 Chemical Structure

CAS No. : 2913192-47-7

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查看 Estrogen Receptor/ERR 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ER degrader 5 is a potent estrogen receptor (ER) degrader. ER degrader 5 shows anti-proliferation activity. ER degrader 5 can be used for the research of breast cancer[1].

体外研究
(In Vitro)

ER degrader 5 (compound 27d) (5 days) 抑制 MCF-7 细胞的增殖,IC50 值为 55 nM[1]
ER degrader 5 阻断 MCF-7 细胞 G0/G1 期细胞周期[1]
ER degrader 5 (1 nM-10 μM; 24 h) 降解 MCF-7 细胞中的雌激素受体 (ER)[1]
ER degrader 5 (1-10 μM; 24 h) 显着降低 MCF-7 细胞中GREB1PGRTFF1 的表达水平[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1, 10, 100, 1000, 10000 nM
Incubation Time: 24 hours
Result: Degraded ER in a dose-dependent manner.

Real Time qPCR[1]

Cell Line: MCF-7 cells
Concentration: 1, 5, 10 μM
Incubation Time: 24 hours
Result: Decreased the expression levels of GREB1, PGR, and TFF1 in a dose-dependent manner.
体内研究
(In Vivo)

ER degrader 5 (compound 27d) (30 mg/kg; i.p. daily for 30 days) 显着抑制 MCF-7 异种移植模型中的肿瘤生长[1]
ER degrader 5 (3 mg/kg; i.v.) 的半衰期为 1.23 小时,Cmax 为 4497 ng/mL[1]
ER degrader 5 (30 mg/kg; p.o.) 产生 62.9% 的口服生物利用度[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice injected with MCF-7 cells[1]
Dosage: 30 mg/kg
Administration: I.p. daily for 30 days
Result: Inhibited tumor growth and observed no significant body weight loss.
分子量

464.48

Formula

C26H18F2O4S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
ER degrader 5
目录号:
HY-149970
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