您好，欢迎来到试剂仪器网！ [登录] [免费注册]
试剂仪器网
发布求购
位置：首页 > 产品库 > TH287
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
TH287
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
TH287图片
CAS NO:1609960-30-6
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
100mg电议

产品介绍
TH287 是一种有效的选择性 MTH1 抑制剂，IC50 为 0.8 nM。 TH287 对 MTH1 具有高度选择性，在 100 μM 时对 MTH2、NUDT5、NUDT12、NUDT14、NUDT16、dCTPase、dUTPase 和 ITPA 没有相关抑制作用。 TH287 可以作为癌症研究的化学治疗剂。
Cas No.1609960-30-6
化学名6-(2,3-dichlorophenyl)-N4-methylpyrimidine-2,4-diamine
Canonical SMILESClC1=C(Cl)C(C2=CC(NC)=NC(N)=N2)=CC=C1
分子式C11H10Cl2N4
分子量269.13
溶解度≥ 55.6mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

TH287 is a potent MTH1 inhibitor with IC50 of 0.8±0.1 nM. [1]

MTH1 (human MutT homolog 1) is an antimutagenic purine nucleoside triphosphatase that sanitize oxidized nucleotide pools. It’s a new cancer therapeutic target as it protects the cancer cell from DNA damages such as oxidative stress-induced cell dysfunction or death.

In U2OS and other cancer cell lines, TH287 treatment selectively and effectively kill cancer cells with less toxic to some primary or immortalized cells. U2OS cells treated with TH287 shows increase of 8-oxodG in DNA. The MTH1 inhibitor TH287 induces DNA damage and activates an ATM-p53-mediated death response and DNA repair in U2OS cells. [1]

Reference:
1.  Gad H, Koolmeister T, Jemth AS et al. MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool. Nature. 2014 Apr 10;508(7495):215-21.