Biological Activity |
TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM). IC50 & Target: IC50: 5 nM (MTH1)[1] In Vitro: TH588 (2-10uM; 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 uM[1]. In Vivo: TH588 (30 mg/kg; s.c.; once daily for 35 days) reduces tumour growth in SW480 xenograft cancer model[1]. |