TH588 hydrochloride

Names

[ Name ]:
TH588 hydrochloride

[Synonym ]:
2,4-Pyrimidinediamine, N4-cyclopropyl-6-(2,3-dichlorophenyl)-, hydrochloride (1:1)
N4-Cyclopropyl-6-(2,3-dichlorophenyl)-2,4-pyrimidinediamine hydrochloride (1:1)
TH588 (hydrochloride)

Biological Activity

[Description]:

TH588 hydrochloride 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]

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₃H₁₃Cl₃N₄

[ Molecular Weight ]:
331.628

[ Exact Mass ]:
330.020569

[ Storage condition ]:
2-8℃

Related Compounds

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