ATN-161

Catalog No.S8454 Batch:S845402

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Technical Data

Formula

C23H35N9O8S
Molecular Weight 597.64 CAS No. 262438-43-7
Solubility (25°C)* In vitro Water 13 mg/mL (21.75 mM)
 
 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description ATN-161 is a novel small peptide antagonist of integrin α5β1. It binds to several integrins, including α5β1 and αvβ3, that play a role in angiogenesis and tumor progression.
Targets
integrin α5β1 [1] αvβ3 [1]
In vitro ATN-161 interacts with the N-terminus of the β1-domain of integrin α5β1, which may lock this integrin in an inactive conformation[2]. ATN-161 treatment up to 100 μmol/L shows no significant effect on tumor cell proliferation compared with the vehicle-treated control group of cells. However, ATN-161 significantly inhibits MAPK phosphorylation with maximal effects observed at 20 μmol/L of ATN-161 after 30 minutes of treatment[1].
In vivo ATN-161 (Ac-PHSCN-NH2), a 5-mer capped peptide derived from the synergy region of fibronectin that binds to α5β1 and αvβ3 in vitro, blocks breast cancer growth and metastasis. Treatment with ATN-161 causes a significant dose-dependent decrease in tumor volume and either completely blocked or caused a marked decrease in the incidence and number of skeletal as well as soft tissue metastases. Treatment with ATN-161 results in a significant decrease in the expression of phosphorylated mitogen-activated protein kinase, microvessel density, and cell proliferation in tumors grown in vivo[1]. ATN-161 is a peptide with a fairly short plasma half-life. compared with the plasma pharmacokinetics of ATN-161, It is cleared from the tumor with much slower kinetics supporting the hypothesis that this peptide exerts its effects through a durable interaction with its target(s)in the tumor[3].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    MDA-MB-231 cells

  • Concentrations

    1-100 μmol/L

  • Incubation Time

    15-60 minutes

  • Method

    MDA-MB-231 (1 × 106) cells are plated in 100 mm Petri dishes for 24 hours, then serum-starved overnight before treatment with vehicle or ATN-161 (1-100 μmol/L) for different time periods (15-60 minutes). Western blot analyses are carried out using antibodies against focal adhesion kinase, phosphorylated FAK, mitogen-activated protein kinase (MAPK), phosphorylated MAPK, and β-tubulin as previously described. Western blots are detected using enhanced chemiluminescence detection reagents.
Animal Study:

[1]
  • Animal Models

    BALB/c nu/nu mice

  • Dosages

    0.05-1 mg/kg/d

  • Administration

    i.v.

Selleck's ATN-161 has been cited by 17 publications

Ion elemental-optimized layered double hydroxide nanoparticles promote chondrogenic differentiation and intervertebral disc regeneration of mesenchymal stem cells through focal adhesion signaling pathway [ Bioact Mater, 2023, 22:75-90] PubMed: 36203960
Tumor-derived insulin-like growth factor-binding protein-1 contributes to resistance of hepatocellular carcinoma to tyrosine kinase inhibitors [ Cancer Commun (Lond), 2023, 10.1002/cac2.12411] PubMed: 36825684
Stromal-induced epithelial-mesenchymal transition induces targetable drug resistance in acute lymphoblastic leukemia [ Cell Rep, 2023, 42(7):112804] PubMed: 37453060
Targeting NADPH Oxidase and Integrin α5β1 to Inhibit Neutrophil Extracellular Traps-Mediated Metastasis in Colorectal Cancer [ Int J Mol Sci, 2023, 10.3390/ijms242116001] PubMed: 37958984
SHARPIN Enhances Ferroptosis in Synovial Sarcoma Cells via NF-κB- and PRMT5-Mediated PGC1α Reduction [ Cancers (Basel), 2023, 15(13)3484] PubMed: 37444594
The natural compound atraric acid suppresses androgen-regulated neo-angiogenesis of castration-resistant prostate cancer through angiopoietin 2 [ Oncogene, 2022, 10.1038/s41388-022-02333-7] PubMed: 35513564
EXOC4 Promotes Diffuse-Type Gastric Cancer Metastasis via Activating FAK Signal [ Mol Cancer Res, 2022, 20(7):1021-1034] PubMed: 35471457
EXOC4 Promotes Diffuse-Type Gastric Cancer Metastasis via Activating FAK Signal [ Mol Cancer Res, 2022, 20(7):1021-1034] PubMed: 35471457
ITGA5 and ITGB1 contribute to Sorafenib resistance by promoting vasculogenic mimicry formation in hepatocellular carcinoma [ Cancer Med, 2022, 10.1002/cam4.5110] PubMed: 35946175
Phosphorylation inhibition of protein-tyrosine phosphatase 1B tyrosine-152 induces bone regeneration coupled with angiogenesis for bone tissue engineering [ Bioact Mater, 2021, 6(7):2039-2057] PubMed: 33511306

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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