CAS:1609960-30-6TH287

TH287 is a selective MTH1 inhibitor with IC50 value of 0.8 nM.

规格	价格	促销价格	库存

18817579266

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咨询

18817579266

立即询价

实验数据

技术信息

CAS号

1609960-30-6

储存条件

分子式

C11H10Cl2N4

运输

蓝冰

分子量

269.13

别名

溶解度

DMSO	50.0 mg/mL (185.8 mM)
Water	insoluble

动物实验配方

生物活性

描述The nucleotide-sanitizing enzyme MutT homolog 1 (MTH1) can hydrolyze oxidized nucleotides and is required for cancer survival. TH287 is a potent inhibitor of MTH1 with an IC50 value of 0.8 nM and causes incorporation of oxidized dNTPs in cancer cells, leading to DNA damage, cytotoxicity and therapeutic responses. TH287 at 10uM significantly induced 3.2-fold increases in apoptosis level in human non-small cell lung cancer cell line H23 but showed no affect on A549 cells. TH287 alone showed no obvious effect on the human tongue squamous cell carcinoma cell line CAL27 cancer suppression in the xenograft model.
作用机制TH287 inhibits MTH1 by occupying the recognition site of 8-oxodGTP in MTH1.

动物研究

剂量

Mice: 10 mg/kg^[2] (s.c.); 5 mg/kg^[1] (i.p.)

给药途径

s.c.

动物药代数据