1. Epigenetics Apoptosis
  2. Histone Methyltransferase Bcl-2 Family
  3. AS 1411

AS 1411 (AGRO-100) 是一种靶向核蛋白的寡核苷酸适配体。AS 1411 通过影响含核蛋白复合物的活性抑制肿瘤细胞增殖,并可作为载体将纳米颗粒、寡核苷酸及小分子精准递送至癌细胞。AS 1411 在 DU145 前列腺癌细胞中,减少 PRMT5 表达以抑制肿瘤生长。AS 1411 在 MCF-7 乳腺癌细胞中,则通过阻断核蛋白与 bcl-2 mRNA 的结合发挥作用。AS 1411 偶联金纳球能在体外抑制乳腺癌细胞增殖,也可以在小鼠模型中抑制乳腺癌细胞增殖,具备穿越血脑屏障的能力且组织毒性低。

该游离形式化合物不稳定,推荐具有相同生物学活性的稳定盐形式 AS 1411 sodium

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DNA, d(G-G-T-G-G-T-G-G-T-G-G-T-T-G-T-G-G-T-G-G-T-G-G-T-G-G)

AS 1411 Chemical Structure

CAS No. : 301636-59-9

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Other Forms of AS 1411:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AS 1411 (AGRO-100) is an oligonucleotide aptamer targeting nucleoproteins. AS 1411 inhibits tumor cell proliferation by affecting the activity of nucleoprotein-containing complexes and can be used as a carrier to precisely deliver nanoparticles, oligonucleotides and small molecules to cancer cells. AS 1411 reduces PRMT5 expression to inhibit tumor growth in DU145 prostate cancer cells. AS 1411 works by blocking the binding of nucleoproteins to bcl-2 mRNA in MCF-7 breast cancer cells. AS 1411-coupled Jin nanospheres can inhibit breast cancer cell proliferation in vitro and in mouse models, has the ability to cross the blood-brain barrier with low tissue toxicity[1][2][3].

IC50 & Target

Bcl-2

 

体外研究
(In Vitro)

AS 1411 (10 μM, 0-48 h) 改变了 DU145 细胞中 PRMT5 的核定位[1]
AS 1411 (10 μM, 24 h) 通过降低 PRMT5 表达,增加 cyclin E2 和 ST7 的表达[1]
AS 1411 (0-20 μM, 0-96 h) 抑制 MCF-7 细胞增殖,但不影响 MCF-10A 细胞[2]
AS 1411 (2 μM, 1 h) 在 MCF-7 和 MCF-10A 细胞核中均有分布,但在 MCF-7 细胞质中的分布更高[2]
AS 1411 (10 μM, 72 h) 抑制 MCF-7 和 MDA-MB-231 细胞中 Bcl-2 mRNA 的稳定性,对 MCF-10A 无影响[2]
AS 1411 (0-10 μM, 72 h) 抑制 MCF-7 细胞中核蛋白与 bcl-2 mRNA 的结合[2]
AS 1411 偶联金纳米球 (0-800 nM, 72 h) 对 MCF-7 和 MDA-MB-231 细胞的抗增殖作用强于单独使用 AS 1411,且不对 MCF-10A 细胞产生抗增殖作用[3]

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

Cell Cycle Analysis[1]

Cell Line: DU145
Concentration: 10 μM
Incubation Time: 24 h
Result: Increased the proportion of cells in S phase and decreased G2-M cells.

Cell Viability Assay[2]

Cell Line: MCF-7, MCF-10A
Concentration: 0, 5, 10, 20 μM
Incubation Time: 0, 24, 48, 72, 96 h
Result: Inhibited the proliferation of MCF-7 and lost mitochondrial activity after 72 hours, but had no effect on MCF-10A.

Cell Proliferation Assay[3]

Cell Line: MCF-7; MDA-MB-231; MCF-10A
Concentration: 0, 200, 400, 600, 800 nM,
Incubation Time: 72 h
Result: Inhibited MCF-7 cell survival by more than 80% at 200 nM, whereas neither AS1411 alone nor control GNS had a significant effect under these conditions. AS1411GNS (88% cell death at 200 nM) was significantly increased in MDA-MB-231 cells compared to AS1411 (27% cell death at 10 μM).

RT-PCR[1]

Cell Line: DU145
Concentration: 10 μM
Incubation Time: 24 h
Result: Increased the mRNA expressions of cyclin E2 and ST7.

RT-PCR[2]

Cell Line: MCF-7, MCF-10A
Concentration: 10 μM
Incubation Time: 72 h
Result: Reduced the stability of bcl-2 mRNA, reducing the half-life of bcl-2 from 10h to 1h in MCF-7 cells and from 11h to 1.2h in MDA-MB-231 cells, but had no effect on MCF-10A cells.

Western Blot Analysis[1]

Cell Line: DU145; DU145 cells transfected with siRNA; NM23
Concentration: 10 μM
Incubation Time: 0, 1, 4, 24, 48 h
Result: Reduced nucleolar protein-associated PRMT5 in the nucleus of DU145 cells and increased nucleolar protein-associated PRMT5 in the cytoplasm, which was related to time and dose.
Reduced the expression of PRMT5 in DU145 cells, upregulated the expression of PRMT5 cyclin2 and ST7 and inhibited tumor proliferation.

Immunofluorescence[2]

Cell Line: MCF-7, MCF-10A
Concentration: 2 μM
Incubation Time: 1 h
Result: Distributed in the cell nucleus, and its distribution in the cytoplasm of MCF-7 is higher than that of MCF-10A and it is more sensitive to MCF-7.

Real Time qPCR[2]

Cell Line: MCF-7
Concentration: 0, 5, 10 μM
Incubation Time: 72 h
Result: Reduced the enrichment of bcl-2 mRNA in the immunoprecipitate.
体内研究
(In Vivo)

AS 1411 与金纳米球 (GNS) 偶联在乳腺癌细胞异种移植的小鼠模型中有抗肿瘤活性[3]

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

Animal Model: Female nude mice bearing MDA-MB-231 xenografts[3]
Dosage: 22 μg; once a day; 12 days
Administration: Intravenous injection (i.v.)
Result: Took up and retained in tumors and cleared in normal tissues.
分子量

8272.31

CAS 号
性状

固体

颜色

White to off-white

Sequence

DNA, d(G-G-T-G-G-T-G-G-T-G-G-T-T-G-T-G-G-T-G-G-T-G-G-T-G-G)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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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AS 1411
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