TH-287

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 0.8 nM。

A potent and selective inhibitor of MTH1 protein with IC50 of 0.8 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.

TH287 (1-10 μM; 24 h) selectively and effectively kills U2OS and other cancer cell lines, but is considerably less toxic to several primary or immortalized cells.

TH287 (5 mg/kg; i.p.) exhibits Cmax of 0.82 μM and tmax of 0.5 h in mice.

TH287

Cell Cycle/DNA Damage

DNA/RNA Synthesis

MTH1

Cancer

——

1609960-30-6

269.1299

C11H10Cl2N4

>98% (HPLC)

DMSO: ≥ 2.6 mg/mL

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

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

(-20℃)

With Ice Pack

≥ 2 years