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TH287 hydrochloride

Names

[ CAS No. ]:
1638211-05-8

[ Name ]:
TH287 hydrochloride

[Synonym ]:
2,4-Pyrimidinediamine, 6-(2,3-dichlorophenyl)-N4-methyl-, hydrochloride (1:1)
6-(2,3-Dichlorophenyl)-N4-methyl-2,4-pyrimidinediamine hydrochloride (1:1)
TH287 (hydrochloride)

Biological Activity

[Description]:

TH287 hydrochloride is a potent inhibitor of MTH1 (NUDT1) with an IC50 value of 0.8 nM, less potent for MTH2, NUDT5, NUDT12, NUDT14, and NUDT16.IC50 value: 0.8 nM [1]Target: MTH1 inhibitorTH287 is considered a new target for cancer therapy. TH287 is highly selective towards MTH1, with no relevant inhibition of other members of the nudix protein family. TH287 has been shown to selectively kill a variety of cancer cell lines, but is rapidly metablized, so not as useful for in vivo studies.

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> DNA/RNA Synthesis
Research Areas >> Cancer

[References]

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


[Related Small Molecules]

Cycloheximide | Actinomycin D | alpha-Amanitin | Anisomycin | SCR7 | CX-5461 | LMI070 | COH29 | Triciribine | Folic Acid | Halofuginone | RG7800 | ML216 | Adenine | Nedaplatin

Chemical & Physical Properties

[ Molecular Formula ]:
C11H11Cl3N4

[ Molecular Weight ]:
305.591

[ Exact Mass ]:
304.004944

[ Storage condition ]:
2-8℃

Related Compounds