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    Pyridostatin Trifluoroacetate (RR82)
    Pyridostatin Trifluoroacetate (RR82)

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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 #: V1433
    CAS #: 1472611-44-1 Purity ≥98%

    Description: Pyridostatin Trifluoroacetate (RR82; RR 82; RR-82; PDS; Pyridostatin TFA), the Trifluoroacetate (TFA) salt of Pyridostatin, is a G-quadruplexe stabilizer with potential antineoplastic activity. It stabilizes G-quadruplexe with a Kd of 490 nM in a cell-free assay. Pyridostatin targets a series of proto-oncogenes including c-kit, K-ras and Bcl-2. Pyridostatinshows potent anti-proliferative activity in vitro against various cancer cell lines such as MRC-5–SV40 cells and various cancer cell lines, and induces cell-cycle arrest by DNA-damage checkpoint activation. Pyridostatin also reduces SRC-dependent cell motility in MDA-MB-231 cells by interacting with G-quadruplex motifs in SRC. 

    References: Nat Chem Biol. 2012 Feb 5;8(3):301-10; Nat Chem Biol. 2014 May;10(5):358-64.

    Related CAS#: 1085412-37-8 (free base); 1472611-44-1 (TFA); 1629261-49-9 (HCl)    

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    Molecular Weight (MW)938.72
    FormulaC37H35F9N8O11
    CAS No.1472611-44-1 TFA salt
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL 
    Water: 100 mg/mL 
    Ethanol: 30 mg/mL
    Other info

    Chemical Name: 4-(2-aminoethoxy)-N2,N6-bis(4-(2-aminoethoxy)quinolin-2-yl)pyridine-2,6-dicarboxamide tris(2,2,2-trifluoroacetate)

    InChi Key: CYYZQGUDHAKBIQ-UHFFFAOYSA-N

    InChi Code: InChI=1S/C31H32N8O5.3C2HF3O2/c32-9-12-42-19-15-24(30(40)38-28-17-26(43-13-10-33)20-5-1-3-7-22(20)36-28)35-25(16-19)31(41)39-29-18-27(44-14-11-34)21-6-2-4-8-23(21)37-29;3*3-2(4,5)1(6)7/h1-8,15-18H,9-14,32-34H2,(H,36,38,40)(H,37,39,41);3*(H,6,7)

    SMILES Code: O=C(C1=NC(C(NC2=NC3=CC=CC=C3C(OCCN)=C2)=O)=CC(OCCN)=C1)NC4=NC5=CC=CC=C5C(OCCN)=C4.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F

    Synonyms

    RR-82; PDS; RR 82; RR82; Pyridostatin TFA salt


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    In Vitro

    In vitro activity: Pyridostatin decreases the proliferation of MRC-5–SV40 cells and various cancer cell lines, and induces cell-cycle arrest by DNA-damage checkpoint activation. Pyridostatin also reduces SRC-dependent cell motility in MDA-MB-231 cells by interacting with G-quadruplex motifs in SRC. Pyridostatin decreases EBNA1 synthesis via inhibition of G-quadruplexes.


    Cell Assay: Cells (MRC-5–SV40 cells and various cancer cell lines) are plated at equal confluence and are left either untreated or were treated with 2 μM pyridostatin continually during the indicated time before harvesting the cells. Cells from individual plates are trypsinized and counted in a Coulter counter. Graphs represent the total cell numbers at each time interval, and the error bars represent the s.e.m. Data represent three independent experiments.

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    References

    Nat Chem Biol. 2012 Feb 5;8(3):301-10; Nat Chem Biol. 2014 May;10(5):358-64. 


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

    Pyridostatin Trifluoroacetate

    The small molecule PDS stabilizes g4-EBNA1 G-quadruplex structure and inhibits EBNA1 translation. Nat Chem Biol. 2014 May;10(5):358-64.



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