TH287 盐酸盐

C₁₁H₁₀Cl₂N₄ · HCl

305.59

MFCD28127273

329825648

NA.77

TH287 is a potent inhibitor of human 7,8-Dihydro-8-oxoguaninetriphosphatase MTH1 (NUDT1) with an IC₅₀ value of 0.8 nM. MTH1 hydrolyzes oxidized purine nucleoside triphosphates that might otherwise be incorporated into DNA/RNA and contribute to DNA damage. MTH1 removal of oxidized nucleotides that result from increased levels of reactive oxygen species (ROS) in fast-proliferating cancer cells helps protect cancer cells from proliferative stress and prevent cancer cell death. TH287 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.

100

≥98% (HPLC)

powder

white to beige

DMSO: 5 mg/mL, clear (warmed)

2-8℃

ClC1=CC=CC(C2=NC(N)=NC(NC)=C2)=C1Cl.Cl

1S/C11H10Cl2N4.ClH/c1-15-9-5-8(16-11(14)17-9)6-3-2-4-7(12)10(6)13;/h2-5H,1H3,(H3,14,15,16,17);1H

YBLIJWDQSUDCJU-UHFFFAOYSA-N

5, 25 mg in glass bottle

GHS05,GHS07

Danger

H302 - H318

P280 - P301 + P312 + P330 - P305 + P351 + P338 + P310

Acute Tox. 4 Oral - Eye Dam. 1

11 - Combustible Solids

WGK 3