AS 1411 (Synonyms: AGRO-100)

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Data Sheet SDS Handling Instructions

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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.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (AS 1411 sodium) that retains the same biological activity.

For research use only. We do not sell to patients.

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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This product is a controlled substance and not for sale in your territory.

Other Forms of AS 1411:

AS 1411 sodium Get quote
AS 1411 triethylamine Get quote

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EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Bcl-2

In Vitro

AS 1411 (10 μM, 0-48 h) alters the nuclear localization of PRMT5 in DU145 cells^[1].
AS 1411 (10 μM, 24 h) reduces PRMT5 expression and increases the expression of cyclin E2 and ST7^[1].
AS 1411 (0-20 μM, 0-96 h) inhibits MCF-7 cell proliferation without affecting MCF-10A cells^[2].
AS 1411 (2 μM, 1 h) distributes in the nuclei of both MCF-7 and MCF-10A cells, but its cytoplasmic distribution is higher in MCF-7 cells^[2].
AS 1411 (10 μM, 72 h) inhibits the stability of Bcl-2 mRNA in MCF-7 and MDA-MB-231 cells, with no effect on MCF-10A cells^[2].
AS 1411 (0-10 μM, 72 h) inhibits the binding of nucleoproteins to bcl-2 mRNA in MCF-7 cells^[2].
AS 1411 conjugated with gold nanoparticles (0-800 nM, 72 h) exerts a stronger antiproliferative effect on MCF-7 and MDA-MB-231 cells compared to AS 1411 alone, without affecting MCF-10A cells^[3].

MedChemExpress (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.

In Vivo

AS 1411 coupled with gold nanospheres (GNS) shows antitumor activity in a mouse model of breast cancer cell xenografts^[3].

MedChemExpress (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.

Molecular Weight

8272.31

CAS No.

301636-59-9

Appearance

Solid

Color

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)

SMILES

[AS 1411]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

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

Purity & Documentation

Data Sheet (276 KB) SDS (251 KB) Handling Instructions (2659 KB)

References

[1]. Teng Y, et al. AS1411 alters the localization of a complex containing protein arginine methyltransferase 5 and nucleolin. Cancer Res. 2007;67(21):10491-10500. [Content Brief]

[2]. Soundararajan S, et al. The nucleolin targeting aptamer AS1411 destabilizes Bcl-2 messenger RNA in human breast cancer cells. Cancer Res. 2008;68(7):2358-2365. [Content Brief]

[3]. Mohammad T Malik, et al. AS1411-conjugated gold nanospheres and their potential for breast cancer therapy. Oncotarget. 2015 Sep 8;6(26):22270-81. [Content Brief]

AS 1411 Related Classifications

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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.

Keywords:

AS 1411301636-59-9AGRO-100AS1411AS-1411AGRO100AGRO 100Histone MethyltransferaseBcl-2 FamilyNanoparticlesOligonucleotidesCancersTumor suppressionMCF-7DeliveryNuclear proteinInhibitorinhibitorinhibit

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