1. Vitamin D Related/Nuclear Receptor
  2. Estrogen Receptor/ERR
  3. Etacstil

Etacstil (GW5638) 是一种雌激素受体 (estrogen receptor) 拮抗剂,在去卵巢大鼠中显示出极少的子宫促性活性,并抑制 Estradiol (HY-B0141), Tamoxifen (HY-13757A) 和 Raloxifene (HY-13738) 的激动剂活性。Etacstil 有望用于乳腺癌和骨骼保护方面的研究。

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Etacstil Chemical Structure

Etacstil Chemical Structure

CAS No. : 155701-61-4

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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

Etacstil (GW5638) is a estrogen receptor antagonist that displays minimal uterotropic activity in ovariectomized rats and inhibits the agonist activity of Estradiol (HY-B0141), Tamoxifen (HY-13757A) and Raloxifene (HY-13738) in the environment. Etacstil is promising for research of breast cancer and bone protection[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MCF7 IC50
> 1.27 μM
Compound: 3a, GW5638
Suppression of ER alpha in human MCF7 cells after 24 hrs by immunostaining analysis
Suppression of ER alpha in human MCF7 cells after 24 hrs by immunostaining analysis
[PMID: 25790336]
MCF7 IC50
> 100 μM
Compound: 3a, GW5638
Agonist activity at ER alpha in human MCF7 cells assessed as PR gene expression after 24 hrs by laser scanning imaging cytometer analysis
Agonist activity at ER alpha in human MCF7 cells assessed as PR gene expression after 24 hrs by laser scanning imaging cytometer analysis
[PMID: 25790336]
MCF7 EC50
0.3 μM
Compound: 3a, GW5638
Inhibition of cell proliferation in human MCF7 cells after 7 days by laser scanning imaging cytometer analysis
Inhibition of cell proliferation in human MCF7 cells after 7 days by laser scanning imaging cytometer analysis
[PMID: 25790336]
MCF7 EC50
0.39 μM
Compound: 4, GW-5638
Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay
Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay
[PMID: 25879485]
MCF7 IC50
0.985 μM
Compound: 4, GW-5638
Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay
Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay
[PMID: 25879485]
MCF7 EC50
390 nM
Compound: GW-5638; 2
Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS incubated for 4 hrs by IRDye 800CW/DRAQ5 dye based in-cell Western assay
Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS incubated for 4 hrs by IRDye 800CW/DRAQ5 dye based in-cell Western assay
[PMID: 30587451]
MCF7 IC50
4 μM
Compound: 3a, GW5638
Antagonist activity at ER alpha in human MCF7 cells assessed as inhibition of estradiol-induced PR expression treated for 24 hrs after incubation with estradiol for 30 mins by laser scanning imaging cytometer analysis
Antagonist activity at ER alpha in human MCF7 cells assessed as inhibition of estradiol-induced PR expression treated for 24 hrs after incubation with estradiol for 30 mins by laser scanning imaging cytometer analysis
[PMID: 25790336]
分子量

354.44

Formula

C25H22O2

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:
Etacstil
目录号:
HY-112746
需求量: