MDL | MFCD06798345 |
---|---|
Molecular Weight | 281.31 |
Molecular Formula | C17H15NO3 |
SMILES | O=C1C2=CC=C3C=CC=CC3=C2OC(N4CCOCC4)=C1 |
DNA-PK 0.23 μM (IC 50 ) |
PI3K 13 μM (IC 50 ) |
NU7026 (10 μM) potentiates ionizing radiation (IR) cytotoxicity [potentiation factor at 90% cell kill (PF
90
)=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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 2.5 mg/mL ( 8.89 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 3.5548 mL | 17.7740 mL | 35.5480 mL |
5 mM | 0.7110 mL | 3.5548 mL | 7.1096 mL |
10 mM | --- | --- | --- |