TH588

TH588

Catalog Number:
L002371284APE
Mfr. No.:
APE-B5845
Price:
$196
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      • Overview
        • Please contact us at for specific academic pricing.

          Background

          TH588 is a potent and selective MTH1 inhibitor (IC50 = 5 nM).
          MTH1 (human MutT homolog 1) is an antimutagenic purine nucleoside triphosphatase that sanitize oxidized nucleotide pools. It’s a new cancer therapeutic target as it protects the cancer cell from DNA damages such as oxidative stress-induced cell dysfunction or death.
          In U2OS and other cancer cell lines, TH588 treatment selectively and effectively kill cancer cells with less toxic to some primary or immortalized cells. U2OS cells treated with TH588 shows increase of 8-oxodG in DNA. The MTH1 inhibitor TH588 induces DNA damage and activates an ATM-p53-mediated death response and DNA repair in U2OS cells. [1]
          Mice were transplanted with BRAFV600E-mutated melanoma, resistant to carboplatin, dacarbazine and vemurafenib. Ten of the tumor mice were randomized to receive TH588 once daily or vehicle control treatment. All TH588-treated mice had a reduced tumor growth rate, although the serum amount of TH588 decreased below IC50 concentrations during 24 hours treatment. [1]

      • Properties
        • Alternative Name
          (Z)-N-(6-(2,3-dichlorophenyl)-2-imino-2,3-dihydropyrimidin-4(1H)-ylidene)cyclopropanamine
          CAS Number
          1609960-31-7
          Molecular Formula
          C13H12Cl2N4
          Molecular Weight
          295.17
          Appearance
          A solid
          Purity
          98.09%
          Solubility
          insoluble in H2O; insoluble in EtOH; ≥7.38 mg/mL in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

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