NU7026

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NU7026 是一种有效的 DNA-PK 抑制剂，在无细胞测定中 IC50 为 0.23 μM。

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.

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).

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.).

DNA-PK Inhibitor II | LY293646

Cell Cycle/DNA Damage

ATM/ATR

ATM| ATR| DNA-PK| PI3K

Cancer

——

154447-35-5

281.31

C17H15NO3

>98% (HPLC)

DMSO: 1 mg/mL (3.55 mM)

O=C1C=C(N2CCOCC2)OC3=C1C=CC4=CC=CC=C43

2-morpholino-4H-benzo[h]chromen-4-one

(-20℃)

With Ice Pack

≥ 2 years