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TH588 hydrochloride is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).

TH588 (2-10μM; 7-10 days) selectively and effectively kills U2OS, HeLa, MDA-MB-231, MCF-7, SW480, and SW620 cells with IC50s of 1.38, 0.83, 1.03, 1.08, 1.72, 0.8 μM [1]. Cell Viability Assay[1] Cell Line: U2OS, HeLa, MDA-MB-231, MCF-7, SW480, SW620, VH10, HDFn cells

TH588 (30 mg/kg; s.c.; once daily for 35 days) reduces tumour growth in SW480 xenograft cancer model[1]. Animal Model: 5-6 weeks female SCID mice (SW480 xenograft cancer model)[1]

[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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