TH-588

SKU: orb1226061

Description

A potent and selective inhibitor of MTH1 protein with IC50 of 5 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: 1609960-31-7
• MW: 295.1672
• Purity: >98% (HPLC)
• Formula: C₁₃H₁₂Cl₂N₄
• SMILES: NC1=NC(C2=CC=CC(Cl)=C2Cl)=CC(NC3CC3)=N1
• Target: DNA/RNA Synthesis
• Solubility: DMSO: 16 mg/mL

Bioactivity

• In Vivo:
  Animal model: 5-6 weeks female SCID mice (SW480 xenograft cancer model). Dosage: 30 mg/kg. Administration: Subcutaneous injection; once daily for 35 days. Result: Reduced tumour growth in SW480 xenograft cancer model.
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• In Vitro:
  Cell Viability Assay Cell line: U2OS, HeLa, MDA-MB-231, MCF-7, SW480, SW620, VH10, HDFn cells. Concentration: 2, 4, 6, 8, 10 μM. Incubation time: 7-10 days. Result: Selectively and effectively killed U2OS, HeLa, MDA-MB-231, MCF-7, SW480, and SW620 cells with IC50s of 1.38, 0.83, 1.03, 1.08, 1.72, 0.8 μM, but was 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

TH588

Quick Database Links

Gene Symbol

DNA/RNA Synthesis