TH287

Names

[ Name ]:
TH287

[Synonym ]:
6-(2,3-dichlorophenyl)-N4-methylpyrimidine-2,4-diamine
2,4-Pyrimidinediamine, 6-(2,3-dichlorophenyl)-N-methyl-
6-(2,3-Dichlorophenyl)-N-methyl-2,4-pyrimidinediamine

Biological Activity

[Description]:

TH287 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]

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
512.2±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₁H₁₀Cl₂N₄

[ Molecular Weight ]:
269.130

[ Flash Point ]:
263.5±32.9 °C

[ Exact Mass ]:
268.028259

[ PSA ]:
37.81000

[ LogP ]:
3.48

[ Appearance of Characters ]:
white solid

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.681

[ Storage condition ]:
2-8℃

Related Compounds

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