TH-287

SKU: orb1226062

Description

A potent and selective inhibitor of MTH1 protein with IC50 of 0.8 nM; shows no relevant inhibition for MTH2,NUDT5, NUDT12,NUDT14,NUDT16 and other proteinswith known nucleoside triphosphate pyrophosphatase activity; causees incorporation of oxidized dNTPs in cancer cells, leading to DNA damage, cytotoxicity and therapeutic responses in patient-derived mouse xenografts.

Key Properties

• CAS Number: 1609960-30-6
• MW: 269.1299
• Purity: >98% (HPLC)
• Formula: C₁₁H₁₀Cl₂N₄
• SMILES: NC1=NC(C2=CC=CC(Cl)=C2Cl)=CC(NC)=N1
• Target: DNA/RNA Synthesis
• Solubility: DMSO: ≥ 2.6 mg/mL

Bioactivity

• In Vivo:
  TH287 (5 mg/kg; i.p.) exhibits Cmax of 0.82 μM and tmax of 0.5 h in mice.
• In Vitro:
  TH287 (1-10 μM; 24 h) selectively and effectively kills U2OS and other cancer cell lines, but is considerably less toxic to several primary or immortalized cells.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

TH287

Quick Database Links

Gene Symbol

DNA/RNA Synthesis