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    TH287
    TH287

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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 #: V1893
    CAS #: 1609960-30-6Purity ≥98%

    Description: TH287 is a potent and selective MTH1 (NUDT1) inhibitor with IC50 of 0.8 nM. TH287 selectively and effectively kill U2OS and other cancer cell lines with less toxic to several primary or immortalized cells, and induces oxidative DNA damage. In U2OS and other cancer cell lines, TH287 treatment selectively and effectively kill cancer cells with less toxic to some primary or immortalized cells. U2OS cells treated with TH287 shows increase of 8-oxodG in DNA. The MTH1 inhibitor TH287 induces DNA damage and activates an ATM-p53-mediated death response and DNA repair in U2OS cells. 

    References: Nature. 2014 Apr 10;508(7495):215-21; J Pharm Biomed Anal. 2015 Feb;104:1-11.

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    Molecular Weight (MW)269.13 
    FormulaC11H10Cl2N4 
    CAS No.1609960-30-6 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 53 mg/mL (196.9 mM) 
    Water: <1 mg/mL
    Ethanol: 10 mg/mL (37.2 mM) 
    Other info

    Chemical Name: 6-(2,3-dichlorophenyl)-N4-methylpyrimidine-2,4-diamine

    InChi Key: URWCXPXBBITYLR-UHFFFAOYSA-N

    InChi Code: InChI=1S/C11H10Cl2N4/c1-15-9-5-8(16-11(14)17-9)6-3-2-4-7(12)10(6)13/h2-5H,1H3,(H3,14,15,16,17)

    SMILES Code: NC1=NC(C2=CC=CC(Cl)=C2Cl)=CC(NC)=N1

    SynonymsTH287; TH 287; TH-287.


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    In Vitro

    In vitro activity: TH287 selectively and effectively kill U2OS and other cancer cell lines with less toxic to several primary or immortalized cells, and induces oxidative DNA damage.


    Cell Assay: In U2OS and other cancer cell lines, TH287 treatment selectively and effectively kill cancer cells with less toxic to some primary or immortalized cells. U2OS cells treated with TH287 shows increase of 8-oxodG in DNA. The MTH1 inhibitor TH287 induces DNA damage and activates an ATM-p53-mediated death response and DNA repair in U2OS cells. 

    In VivoIn C57Bl/6 mice, TH287 (5 mk/kg, i.p.) causes a peak time and maximum concentration of 0.5 h and 0.82μM.  
    Animal modelC57Bl/6 mice 
    Formulation & DosageDissolved in 1% DMSO, 10% ethanol, 10% Chremophore EL and 10% Tween-80 and diluted with PBS; 5 mg/kg; i.p. injection.
    References

    Nature. 2014 Apr 10;508(7495):215-21; J Pharm Biomed Anal. 2015 Feb;104:1-11. 


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

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