| Hazard Information | Back Directory | [Description]
TH287 hydrochloride is a potent inhibitor of MTH1 (NUDT1) with an IC50 value of 0.8 nM, less potent for MTH2, NUDT5, NUDT12, NUDT14, and NUDT16.IC50 value: 0.8 nM [1]Target: MTH1 inhibitorTH287 is considered a new target for cancer therapy. TH287 is highly selective towards MTH1, with no relevant inhibition of other members of the nudix protein family. TH287 has been shown to selectively kill a variety of cancer cell lines, but is rapidly metablized, so not as useful for in vivo studies.
| [Uses]
TH287 hydrochloride is a potent and selective inhibitor of MTH1, with an IC50 of 0.8 nM. TH287 hydrochloride is highly selective towards MTH1, with no relevant inhibition of MTH2, NUDT5, NUDT12, NUDT14, NUDT16, dCTPase, dUTPase and ITPA at 100 μM. TH287 hydrochloride could act as a chemotherapeutic agent for cancer research[1]. | [in vivo]
TH287 (5 mg/kg; i.p.) exhibits Cmax of 0.82 μM and tmax of 0.5 h in mice[2].
| [storage]
Store at -20°C | [References]
[1]. Gad H, et al. MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool. Nature. 2014 Apr 10;508(7495):215-21. |
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