1. Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  2. Androgen Receptor Reactive Oxygen Species (ROS)
  3. Androgen receptor-IN-7

Androgen receptor-IN-7 是一种强效的雄激素受体 (AR) 抑制剂。Androgen receptor-IN-7 通过 AR- 依赖性和非依赖性双重途径,对 PC-3 (IC50 = 370.37 nM) 和 LNCaP 细胞均表现强效抗癌活性。Androgen receptor-IN-7 在 PC-3 细胞中诱导活性氧 (ROS) 的产生。Androgen receptor-IN-7 可用于前列腺癌的相关研究。

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Androgen receptor-IN-7

Androgen receptor-IN-7 Chemical Structure

CAS No. : 401580-43-6

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Androgen receptor-IN-7 is a potent androgen receptor (AR) inhibitor. Androgen receptor-IN-7 exhibits potent anticancer activity against PC-3 cells (IC50 =370.37 nM) and LNCaP cells via both AR-dependent and AR-independent pathways. Androgen receptor-IN-7 induces ROS production in PC-3 cells. Androgen receptor-IN-7 can be used for prostate cancer research[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
DU-145 IC50
> 1 x 10-3 μM
Compound: 3a
Anticancer activity against human DU145 cells after 24 hrs by MTT assay
Anticancer activity against human DU145 cells after 24 hrs by MTT assay
[PMID: 19376704]
HCT-116 IC50
> 1 x 10-3 μM
Compound: 3a
Anticancer activity against human HCT116 cells after 24 hrs by MTT assay
Anticancer activity against human HCT116 cells after 24 hrs by MTT assay
[PMID: 19376704]
LNCaP IC50
23.7 μM
Compound: 3a
Anticancer activity against human LNCAP cells after 24 hrs by MTT assay
Anticancer activity against human LNCAP cells after 24 hrs by MTT assay
[PMID: 19376704]
MCF7 IC50
> 1 x 10-3 μM
Compound: 3a
Anticancer activity against human MCF7 cells after 24 hrs by MTT assay
Anticancer activity against human MCF7 cells after 24 hrs by MTT assay
[PMID: 19376704]
MDA-MB-231 IC50
> 1 x 10-3 μM
Compound: 3a
Anticancer activity against human MDA231 cells after 24 hrs by MTT assay
Anticancer activity against human MDA231 cells after 24 hrs by MTT assay
[PMID: 19376704]
MIA PaCa-2 IC50
> 1 x 10-3 μM
Compound: 3a
Anticancer activity against human MIAPaCa2 cells after 24 hrs by MTT assay
Anticancer activity against human MIAPaCa2 cells after 24 hrs by MTT assay
[PMID: 19376704]
PC-3 IC50
> 1 x 10-3 μM
Compound: 3a
Anticancer activity against human PC3 cells after 24 hrs by MTT assay
Anticancer activity against human PC3 cells after 24 hrs by MTT assay
[PMID: 19376704]
体外研究
(In Vitro)

Androgen receptor-IN-7 (MS14) (0-300 nM,24 小时) 可剂量依赖性地增加 PC-3 细胞中的 ROS 水平,与对照组相比,150 nM 时 ROS 相对水平增加 19.8%,300 nM 时增加 49%[1]
Androgen receptor-IN-7 (150-300 nM,24 小时) 可剂量依赖性地降低 PC-3 细胞中雄激素受体的表达[1]
Androgen receptor-IN-7 与雄激素受体结合口袋紧密结合,并通过与 Arg752 和 Gln711 的关键氢键相互作用而稳定[1]
Androgen receptor-IN-7 (0-1000 nM,24 小时) 在 LNCaP 细胞中表现出剂量依赖性的抗增殖作用 (在 1000 nM 时达到 78.2% 的抑制率),表明它在 AR 阳性模型中保留了显著的活性,通过 AR 依赖性和非 AR 依赖性途径发挥作用[1]

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

Immunofluorescence[1]

Cell Line: PC-3 cells
Concentration: 150 and 300 nM
Incubation Time: 24 h
Result: Resulted in a dose-dependent decrease in androgen receptor expression compared to the control group.
分子量

240.23

Formula

C14H9FN2O

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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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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