NU 7026

NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC₅₀ of 0.23 μM, also inhibits PI3K with IC₅₀ of 13 μM. IC50 & Target: IC50: 0.23±0.01 μM (DNA-PK), 13±3 μM (PI3K)^[1] 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].
Solution in vitro: NU7026 is dissolved in anhydrous DMSO. NU7026 is added to cells to a final concentration of 0.25% DMSO (v/v)^[4]. 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].
Solution in vivo:
NU7026 is formulated in 10% DMSO and 5% Tween 20 in saline (i.p. and p.o.) (Mice)^[3].
NU7026 is formulated in 10% ethanol, 25% PEG 200 and 5% Tween 20 in saline (i.v.)^[3].