TH287 hydrochloride

SKU: orb1306566

Description

TH287 is a potent and selective MTH1 inhibitor with an IC50 of 0.8 nM. It induces cytotoxicity in cancer cells by promoting the incorporation of oxidized dNTPs into DNA, causing DNA damage. This mechanism has demonstrated therapeutic efficacy in patient-derived xenograft (PDX) mouse models, supporting its use in oncology research.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 1638211-05-8
• MW: 305.59
• Purity: 99.50% (May vary between batches)
• Formula: C₁₁H₁₁Cl₃N₄
• SMILES: NC1=NC(C2=CC=CC(Cl)=C2Cl)=CC(NC)=N1.[H]Cl
• Target: MTH1,DNA/RNA Synthesis
• Solubility: DMSO:27.5 mg/mL (89.99 mM)

Bioactivity

• Target IC50:
  MTH1:0.8 nM
• In Vitro:
  TH287 as first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 protein in cells. Protein co-crystal structures demonstrate that the inhibitors bind in the active site of MTH1. The inhibitors cause incorporation of oxidized dNTPs in cancer cells, leading to DNA damage, cytotoxicity and therapeutic responses in patient-derived mouse xenografts.
  Read more...

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DNA/RNA Synthesis, DNA Synthesis, DNASynthesis, inhibit, MTH1, Inhibitor, TH 287, TH 287 Hydrochloride, TH287, TH-287, TH287 Hydrochloride, TH287 hydrochloride, TH-287 Hydrochloride, TH-287 hydrochloride, RNASynthesis, RNA Synthesis

Compound Identifiers

PubChem CID

91826506