TH-287 hydrochloride

Research use only, not for human use.

A potent and selective inhibitor of MTH1 protein with IC50 of 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 hydrochloride

Cell Cycle/DNA Damage

DNA/RNA Synthesis

DNA/RNA Synthesis

Cancer

——

1638211-05-8

305.5909

C11H11Cl3N4

>98% (HPLC)

10 mM in DMSO

CNC1=NC(=NC(=C1)C2=C(C(=CC=C2)Cl)Cl)N.Cl

2,4-Pyrimidinediamine, 6-(2,3-dichlorophenyl)-N4-methyl-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years