TH-588 hydrochloride

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.

TH588 (2-10μM; 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 μM . 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, 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. Animal Model:5-6 weeks female SCID mice (SW480 xenograft cancer model) Dosage:30 mg/kg Administration: Subcutaneous injection (s.c.); once daily for 35 days Result:Reduced tumour growth in SW480 xenograft cancer model.

TH588 hydrochloride

Cell Cycle/DNA Damage

DNA/RNA Synthesis

DNA/RNA Synthesis

Cancer

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1640282-30-9

331.6281

C13H13Cl3N4

>98% (HPLC)

10 mM in DMSO

C1CC1NC2=NC(=NC(=C2)C3=C(C(=CC=C3)Cl)Cl)N.Cl

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

(-20℃)

With Ice Pack

≥ 2 years