TH-588

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 MTH1 蛋白抑制剂，IC50 为 5 nM。

A potent and selective inhibitor of MTH1 protein with IC50 of 5 nM; shows no relevant inhibition for MTH2,NUDT5, NUDT12,NUDT14,NUDT16 and other proteinswith known nucleoside triphosphate pyrophosphatase activity; causees incorporation of oxidized dNTPs in cancer cells, leading to DNA damage, cytotoxicity and therapeutic responses in patient-derived mouse xenografts.

Cell Viability Assay 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 IC50s of 1.38, 0.83, 1.03, 1.08, 1.72, 0.8 μM, but was less toxic to several primary or immortalized cells.

Animal Model:5-6 weeks female SCID mice (SW480 xenograft cancer model)Dosage:30 mg/kg Administration:Subcutaneous injection; once daily for 35 days Result:Reduced tumour growth in SW480 xenograft cancer model.

TH588

Cell Cycle/DNA Damage

DNA/RNA Synthesis

MTH1

Cancer

——

1609960-31-7

295.1672

C13H12Cl2N4

>98% (HPLC)

DMSO: 16 mg/mL

NC1=NC(C2=CC=CC(Cl)=C2Cl)=CC(NC3CC3)=N1

2,4-Pyrimidinediamine, N4-cyclopropyl-6-(2,3-dichlorophenyl)-

(-20℃)

With Ice Pack

≥ 2 years