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TH 588

Names

[ CAS No. ]:
1609960-31-7

[ Name ]:
TH 588

[Synonym ]:
2,4-Pyrimidinediamine, N-cyclopropyl-6-(2,3-dichlorophenyl)-
N-Cyclopropyl-6-(2,3-dichlorophenyl)-2,4-pyrimidinediamine
TH588

Biological Activity

[Description]:

TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1(IC50= 5 nM) in cells.IC50 value: 5 nM [1]Target: MTH1 inhibitorTH588 is highly selective towards MTH1, with no relevant inhibition of other members of the nudix protein family or a panel of 87 enzymes, GPCRs, kinases, ion channels and transporter. TH588 has been shown to selectively kill a variety of cancer cell lines and with in vivo activity shown for TH588 in SW480 colorectal and MCF7 breast tumour xenografts.

[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

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
545.7±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C13H12Cl2N4

[ Molecular Weight ]:
295.167

[ Flash Point ]:
283.9±32.9 °C

[ Exact Mass ]:
294.043915

[ LogP ]:
3.85

[ Appearance of Characters ]:
white solid

[ Vapour Pressure ]:
0.0±1.5 mmHg at 25°C

[ Index of Refraction ]:
1.725

[ Storage condition ]:
-20℃

Related Compounds