TH287 Chemical Properties

Boiling point:

512.2±60.0 °C(Predicted)

Density 

1.440±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

DMSO: soluble5mg/mL, clear (warmed)

pka

5.91±0.10(Predicted)

form 

powder

color 

white to beige

Safety Information

Hazard Codes 

Xn

Risk Statements 

22-41

Safety Statements 

26-39

WGK Germany 

3

TH287 Usage And Synthesis

Description

Human mutT homolog (MTH1) is a nucleotide pool sanitizing enzyme that cleaves oxidized nucleotides (dNTPs) to prevent incorporation of damaged bases during DNA replication. Cancer cells rely on MTH1 activity in order to avoid cell death. TH287 is an MTH1 inhibitor (IC₅₀ = 0.8 nM) that selectively kills cancer cell lines (IC₅₀s = 0.8-3.06 μM) without significant cytotoxicity towards primary or immortalized cells (IC₅₀s = ≥20 μM). At up to 100 μM it does not show significant effect towards the related nudix hydrolase protein family members MTH2, NUDT5, NUDT12, NUDT14, and NUDT16, as well as other proteins with known nucleoside triphosphate pyrophosphatase activity (dCTPase, dUTPase, and ITPA).

Uses

6-(2,3-Dichlorophenyl)-N4-methyl-2,4-pyrimidinediamine is known to possess antitumor effects and nanomolar MTH1-inhibitory activity in vitro for cancer cell survival.

References

1. gad h, koolmeister t, jemth as et al. mth1 inhibition eradicates cancer by preventing sanitation of the dntp pool. nature. 2014 apr 10;508(7495):215-21.

TH287(1609960-30-6)Related Product Information

• N,N'-Bis(2-bromoethyl)phosphorodiamidic acid (1-methyl-2-nitro-1H-imidazol-5-yl)methyl ester
• TH588