TH287

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Chemical Structure| 1609960-30-6 同义名 : -
CAS号 : 1609960-30-6
货号 : A600790
分子式 : C11H10Cl2N4
纯度 : 99%
分子量 : 269.13
MDL号 : MFCD29035111
存储条件：

Pure form Keep in dark place,Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(390.15 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • MTH1

    MTH1, IC50:0.8 nM
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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.72mL

0.74mL

0.37mL

18.58mL

3.72mL

1.86mL

37.16mL

7.43mL

3.72mL
参考文献

[1]Saleh A, Gokturk C, et al. Development and validation of method for TH588 and TH287, potent MTH1 inhibitors and new anti-cancer agents, for pharmacokinetic studies in mice plasma. J Pharm Biomed Anal. 2015 Feb;104:1-11.

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