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[CAS NO. 154447-35-5] NU7026
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15719 |
| Brand: | MCE |
| CAS: | 154447-35-5 |
Overview
| MDL | MFCD06798345 |
|---|---|
| Molecular Weight | 281.31 |
| Molecular Formula | C17H15NO3 |
| SMILES | O=C1C2=CC=C3C=CC=CC3=C2OC(N4CCOCC4)=C1 |
11 Publications Citing Use of MCE
- [1]Mol Cell. 2022 Apr 14:S1097-2765(22)00290-8.
- [2]Nat Commun. 2020 Dec 3;11(1):6182.
- [3]Nucleic Acids Res. 2023 Jan 18;gkac1269.
- [4]Genome Res. 2021 Mar;31(3):461-471.
- [5]Cell Syst. 2020 Jan 22;10(1):66-81.e11.
- [6]Cell Mol Life Sci. 2019 May;76(10):2015-2030.
- [7]Cell Death Dis. 2022 Apr 25;13(4):404.
- [8]Int J Mol Sci. 2022, 23(14), 7518.
- [9]Sci Rep. 2019 Oct 3;9(1):14257.
- [10]Technische Universität Darmstadt. Department of Biology. 2022 Aug.
- [11]Harvard Medical School LINCS LIBRARY
Summary
IC50 & Target
|
DNA-PK 0.23 μM (IC 50 ) |
PI3K 13 μM (IC 50 ) |
In Vitro
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.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 2.5 mg/mL ( 8.89 mM ; Need ultrasonic)
Stock Solutions
| 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 | --- | --- | --- |
References
- [1] Veuger SJ, et al. Radiosensitization and DNA repair inhibition by the combined use of novel inhibitors of DNA-dependent protein kinase and poly(ADP-ribose) polymerase-1. Cancer Res. 2003 Sep 15;63(18):6008-15.
- [2] Amrein L, et al. Chlorambucil cytotoxicity in malignant B lymphocytes is synergistically increased by 2-(morpholin-4-yl)-benzo[h]chomen-4-one (NU7026)-mediated inhibition of DNA double-strand break repair via inhibition of DNA-dependent protein kinase. J
- [3] Nutley BP, et al. Preclinical pharmacokinetics and metabolism of a novel prototype DNA-PK inhibitor NU7026. Br J Cancer. 2005 Oct 31;93(9):1011-8.
- [4] Ciszewski WM, et al. Interleukin-4 enhances PARP-dependent DNA repair activity in vitro. J Interferon Cytokine Res. 2014 Sep;34(9):734-40.
Synonyms
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