TH588 盐酸盐是MTH1 (NUDT1)高效选择性抑制剂，IC50值 5 nM。

TH588 hydrochloride is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 ( IC 50 = 5 nM).

TH588 (2-10μM; 7-10 days) selectively and effectively kills U2OS, HeLa, MDA-MB-231, MCF-7, SW480, and SW620 cells with IC 50 s 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 Concentration: 2, 4, 6, 8, 10 μM Incubation Time: 7–10 days Result: Selectively and effectively killed U2OS, HeLa, MDA-MB-231, MCF-7, SW480, and SW620 cells with IC 50 s of 1.38, 0.83, 1.03, 1.08, 1.72, 0.8 μM, respectively, but was less toxic to several primary or immortalized 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] Dosage: 30 mg/kg Administration: Subcutaneous injection (s.c.); once daily for 35 days Result: Reduced tumour growth in SW480 xenograft cancer model.

1640282-30-9

C13H13Cl3N4

331.63

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years