Cas No.: | 154447-35-5 |
Chemical Name: | NU 7026, NU-7026 |
Synonyms: | NU 7026, NU-7026 |
SMILES: | C1COCCN1C2=CC(=O)C3=C(O2)C4=CC=CC=C4C=C3 |
Formula: | C17H15NO3 |
M.Wt: | 281.31 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | NU 7026 is a novel specific DNA-PK inhibitor with IC50 of 0.23±0.01 μM, also inhibits PI3K with IC50 of 13±3 μM. |
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[3]. |
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[1]. NU7026 synergistically sensitizes I83 cells to Chlorambucil (CLB) 3.5-fold[2].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[3]. |