NU7026

SKU: orb1226119

Description

NU7026 is a potent DNA-PK inhibitor with IC50 of 0.23 μM in cell-free assays, 60-fold selective for DNA-PK than PI3K and inactive against both ATM and ATR.

Key Properties

• CAS Number: 154447-35-5
• MW: 281.31
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₅NO₃
• SMILES: O=C1C=C(N2CCOCC2)OC3=C1C=CC4=CC=CC=C43
• Target: ATM/ATR
• Solubility: DMSO: 1 mg/mL (3.55 mM)

Bioactivity

• In Vivo:
  NU7026, a novel inhibitor of the DNA repair enzyme DNA-dependent protein kinase (DNA-PK). Following intravenous administration to mice at 5 mg/kg, NU7026 underwent rapid plasma clearance (0.108 L/h) and this is largely attributed to extensive metabolism. Bioavailability following interperitoneal (i.p.) and p.o. administration at 20 mg/kg is 20 and 15%, respectively. Solution In vivo: NU7026 is formulated in 10% DMSO and 5% Tween 20 in saline (i.p. and p.o.) (Mice). NU7026 is formulated in 10% ethanol, 25% PEG 200 and 5% Tween 20 in saline (i. v.).
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• In Vitro:
  NU7026 (10 μM) potentiates ionizing radiation (IR) cytotoxicity [potentiation factor at 90% cell kill (PF90)=1.51±0.04] in exponentially growing DNA-PK proficient but not deficient cells. NU7026 synergistically sensitizes I83 cells to Chlorambucil (CLB) 3.5-fold. NU7026, a novel inhibitor of the DNA repair enzyme DNA-dependent protein kinase (DNA-PK). At a dose of 10 μM, which is nontoxic to cells per se, a minimum NU7026 exposure of 4 h in combination with 3 Gy radiation is required for a significant radiosensitisation effect in CH1 human ovarian cancer cells. Solution in vitro: NU7026 is dissolved in anhydrous DMSO. NU7026 is added to cells to a final concentration of 0.25% DMSO (v/v).
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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

DNA-PK Inhibitor II | LY293646

Quick Database Links

Gene Symbol

ATM/ATR