1. Vitamin D Related/Nuclear Receptor
  2. Estrogen Receptor/ERR
  3. (E)-GW7604

(E)-GW7604 是 GW7604 的 (E)-异构体,GW7604 是一种抗雌激素,同时也是高亲和力雌激素受体 (ER) 拮抗剂 GW5638 (HY-112746) 的活性代谢产物。

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(E)-GW7604 Chemical Structure

(E)-GW7604 Chemical Structure

CAS No. : 195611-82-6

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Other Forms of (E)-GW7604:

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

(E)-GW7604 is the (E)-isomer of GW7604, an antiestrogen and a metabolite of GW5638 (HY-112746), which is a high-affinity estrogen receptor (ER) antagonist[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MCF7 IC50
> 30 μM
Compound: 3b, GW7604
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
0.0017 μM
Compound: 5, GW-7604
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
0.005 μM
Compound: 5, GW-7604
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 IC50
0.007 μM
Compound: 3b, GW7604
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
0.012 μM
Compound: 3b, GW7604
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]
MCF7 EC50
1.7 nM
Compound: GW-7604; 1
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
18 nM
Compound: 5, GW-7604
Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay
Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay
[PMID: 25879485]
MCF7 IC50
4.6 nM
Compound: GW-7604; 1
Antiproliferative activity against human MCF7 cells assessed as reduction in cell proliferation measured after 5 days by Cell-titer-Glo assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell proliferation measured after 5 days by Cell-titer-Glo assay
[PMID: 30587451]
分子量

370.44

Formula

C25H22O3

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:
(E)-GW7604
目录号:
HY-W926789
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