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TH-287

CAS No. 1609960-30-6

TH-287( TH287 )

Catalog No. M12321 CAS No. 1609960-30-6

A potent and selective inhibitor of MTH1 protein with IC50 of 0.8 nM.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    TH-287
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent and selective inhibitor of MTH1 protein with IC50 of 0.8 nM.
  • Description
    A potent and selective inhibitor of MTH1 protein with IC50 of 0.8 nM; shows no relevant inhibition for MTH2,NUDT5, NUDT12,NUDT14,NUDT16 and other proteinswith known nucleoside triphosphate pyrophosphatase activity; causees incorporation of oxidized dNTPs in cancer cells, leading to DNA damage, cytotoxicity and therapeutic responses in patient-derived mouse xenografts.
  • In Vitro
    TH287 (1-10 μM; 24 h) selectively and effectively kills U2OS and other cancer cell lines, but is considerably less toxic to several primary or immortalized cells.
  • In Vivo
    TH287 (5 mg/kg; i.p.) exhibits Cmax of 0.82 μM and tmax of 0.5 h in mice.
  • Synonyms
    TH287
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    DNA/RNA Synthesis
  • Recptor
    MTH1
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    1609960-30-6
  • Formula Weight
    269.1299
  • Molecular Formula
    C11H10Cl2N4
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 2.6 mg/mL
  • SMILES
    NC1=NC(C2=CC=CC(Cl)=C2Cl)=CC(NC)=N1
  • Chemical Name
    2,4-Pyrimidinediamine, 6-(2,3-dichlorophenyl)-N4-methyl-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Gad H, et al. Nature. 2014 Apr 10;508(7495):215-21. 2. Wang M, et al. Sci Rep. 2017 Jan 11;7:40557. 3. Kawamura T, et al. Sci Rep. 2016 May 23;6:26521.
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