DI-87

SKU: orb1691229

Description

DI-87 (TRE-515) is a potent, orally bioavailable small molecule inhibitor of deoxycytidine kinase (dCK). By blocking dCK-mediated phosphorylation, it reduces dNTP pools, induces S-phase arrest, and demonstrates synergistic antitumor activity with thymidine in preclinical models. This inhibitor is a valuable research tool for investigating nucleotide metabolism and combination therapies in oncology.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 2107280-55-5
• MW: 502.65
• Formula: C₂₃H₃₀N₆O₃S₂
• SMILES: COc1ccc(cc1OCCN1CCOCC1)-c1nc([C@@H](C)Sc2nc(N)cc(N)n2)c(C)s1
• Target: Others
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.96 mM);DMSO:120 mg/mL (238.73 mM)

Bioactivity

• Target IC50:
  DCK:10.2 nM (EC50)
• In Vivo:
  Methods: Female NSG mice bearing CEM tumors were treated with DI-87 (10, 25, or 50 mg/kg, orally) and DI-87 plasma and tumor concentrations were assessed. Results: Plasma DI-87 concentrations peaked between 1 and 3 hours; tumor concentrations were lower than plasma and had a later, more sustained peak at 3-9 hours.
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• In Vitro:
  Methods: CEM cells were seeded at 1 × 10 3 cells/well in white opaque 384-well plates at 50 μl/well and treated as indicated. After incubation with increasing concentrations (2 nM-10 μM) of gemcitabine and 1 μM DI-87 for 72 h, 50 μl of CellTiter-Glo reagent (diluted 1:5 in dH2O) was added to each well, the plates were incubated at room temperature for 5 m, and luminescence was measured using a BioTek microplate luminometer. Results: The cytotoxic effect of gemcitabine requires dCK, and administration of DI-87 completely blocked cytotoxicity after gemcitabine treatment, demonstrating dCK inhibition by DI-87.
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Storage & Handling

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

Alternative Names

TRE515, TRE-515, DI87, DI-87, DI 87

Compound Identifiers

PubChem CID

122491414