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    ATN-161 TFA
    ATN-161 TFA

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0434
    CAS #: 904763-27-5Purity ≥98%

    Description: ATN-161 TFA, the trifluoroacetic acid salt of ATN161, is a novel and potent small peptide inhibitor of the integrin α5β1 with potential anticancer activity. It inhibits the angiogenesis and growth of liver metastases in a murine model. ATN-161 acts by interacting with the N-terminus of the β1-domain of integrin α5β1, which may lock this integrin in an inactive conformation. Integrin α5β1 is expressed on activated endothelial cells and plays a critical role in tumor angiogenesis. Therefore, ATN-161 has potential anticancer activities.The combination of ATN-161 with 5-fluorouracil (5-FU) chemotherapy has shown enhanced antineoplastic effect. 

    References:  2003 Apr 20;104(4):496-503.

    Related CAS: 262438-43-7 (free base)

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    Molecular Weight (MW) 711.67
    FormulaC25H36F3N9O10S 
    CAS No.  904763-27-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: > 10 mM
    Water: N/A
    Ethanol: N/A
    Chemical Name(S)-2-((R)-2-((S)-2-((S)-2-((S)-1-acetylpyrrolidine-2-carboxamido)-3-(1H-imidazol-5-yl)propanamido)-3-hydroxypropanamido)-3-mercaptopropanamido)succinamide trifluoroacetic acid
    SynonymsAcPHSCNNH2; ATN161; ATN 161; ATN-161
    SMILES CodO=C(N)[[email protected]@H](NC([[email protected]@H](NC([[email protected]@H](NC([[email protected]@H](NC([[email protected]]1N(C(C)=O)CCC1)=O)CC2=CN= CN2)=O)CO)=O)CS)=O)CC(N)=O.O=C(O)C(F)(F)F


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    In Vitro

    In vitro activity:  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.


    Kinase Assay: Binding to purified integrins and localization of ATN-453 to a particular integrin subunit was carried out as follows. α5β1-integrin (Chemicon; 0.2 μmol/L), ATN-453 (10 μmol/L), and 2 mmol/L Mn2+ in 50 mmol/L HBS were incubated at room temperature for 2 h Samples were then resolved under nonreducing conditions on a 4% to 12% NuPAGE Bis-Tris gel, then transferred to a polyvinylidene difluoride membrane by Western blot, and probed with Streptavidin–horseradish peroxidase to identify the ATN-453–bound band. Separate blots were also probed with either an anti-α5, an anti-β1, or an anti-β3 antibody followed by the appropriate secondary antibody to identify the subunit that interacts with ATN-453. Alternatively, purified α5β1 was incubated with anti-β1 antibodies followed by incubation with ATN-453, as previously described. Under nonreducing conditions, the α5subunit runs at ∼160 kDa and β1 at ∼110 kDa.


    Cell Assay: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. 

    In Vivo 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 tumo. 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.
    Animal modelBALB/c nu/nu mice
    Formulation & Dosagesaline; 0.05-1 mg/kg/d;  i.v.
    References  2003 Apr 20;104(4):496-503;  2006 Sep;5(9):2271-80;  2008 Apr 1;14(7):2137-44


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    ATN-161 TFA


    ATN-453 binding to HUVECs can be competed by ATN-161.  2008 Apr 1;14(7):2137-44.

    ATN-161 TFA

    ATN-161 inhibits angiogenesis in a Matrigel plug model.  2008 Apr 1;14(7):2137-44.

     

    ATN-161 TFA

    ATN-453 localizes to neovessels in 3LL tumors grown in Matrigel in vivo.  2008 Apr 1;14(7):2137-44.

    ATN-161 TFA

    Radiographic and histologic analysis of MDA-MB-231-GFP tumor-bearing animals receiving vehicle alone or ATN-161.  2006 Sep;5(9):2271-80.

    ATN-161 TFA

    Effect of ATN-161 on MDA-MB-231 tumor growth in vivo.  2006 Sep;5(9):2271-80.
     ATN-161 TFA


    Effect of ATN-161 on MDA-MB 231-GFP breast cancer micrometastases.  2006 Sep;5(9):2271-80


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