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| 25mg |
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Purity: ≥98%
NU7441 (also called KU-57788) is a highly potent, selective and ATP-competitive inhibitor of DNA-PK (DNA-dependent protein kinase) with IC50 of 14 nM, has anticancer activity. Additionally, it inhibits PI3K in cell-free assays with an IC50 value of 5 M. At a concentration of 100 μM, the DNA-PK-related enzymes ATM and ATR were not inhibited by NU7441. With IC50 values for mTOR and PI3K that were 1.7 and 5 M, respectively—roughly 100 times higher than the IC50 value for DNA-PK—NU7441 demonstrated inhibition activities. In vitro, NU7441 made HeLa cells more sensitive to ionizing radiation, with dose modification factors of 2.5 at 10% survival being seen at 0.5 microM.
| Targets |
DNA-PK (IC50 = 14 nM); mTOR (IC50 = 1.7 μM); PI3K (IC50 = 5.0 μM); CRISPR/Cas9
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| ln Vitro |
NU7441 increases the persistence of γH2AX foci after ionizing radiation–induced or etoposide-induced DNA damage. In both SW620 and LoVo cells, NU7441 (0.5 μM or 1 μM) significantly increases G2-M accumulation brought on by ionizing radiation, etoposide, and doxorubicin. [2] In addition to making DNA double-strand breaks more persistent, NU7441 also slightly reduces the activity of homologous recombination in DNA-PK-sufficient M059-Fus-1 and DNA-PK-sufficient M059 J human tumor cells.[3] In cells that express polymerase as well as those that lack it, NU7441 inhibits UV-induced RPA p34 hyperphosphorylation in a dose-dependent manner. [4] In chronic lymphocytic leukemia cells, NU7441 causes fludarabine-induced H2AX foci to accumulate and, in turn, reduces fludarabine-induced cell death. [5] In addition, DNA-PKcs autophosphorylation and repair brought on by mitoxantrone in cells of chronic lymphocytic leukemia are inhibited by NU7441.[6] In the aftermath of Cas9-mediated DNA cleavage, it decreases the frequency of NHEJ while increasing the rate of HDR[7].
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| ln Vivo |
In mice bearing SW620 xenografts, administration of NU7441 intraperitoneally at a dose of 10 mg/kg for at least 4 hours demonstrates nontoxicity and increases etoposide-induced tumor growth delay by a factor of two.[2]
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| Enzyme Assay |
NU7441 (also called KU-57788) is a highly potent, selective and ATP-competitive DNA-PK inhibitor with IC50 of 14 nM. It also inhibits PI3K with IC50 value of 5 μM in cell-free assays.
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| Cell Assay |
HepG2 cells (4000 per well) are cultured in a 96-well plate for 24 h. The culture media are then supplemented with concentrations of 0.1 µM, 1 µM, 5 µM, and 10 µM of KU-57788 once the cells have finished adhering. 10% CCK-8 solution is added to the culture media after KU-57788 treatment has been going on for 12 hours.Incubation is then continued for another 2 hours. A spectrometer is used to calculate the OD450 values, and the results are then analyzed to calculate the rate of cell growth.
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| Animal Protocol |
Female rude mice bearing SW620 xenografts
10 mg/kg Intraperitoneally administrated |
| References |
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| Additional Infomation |
8-(4-dibenzothiophenyl)-2-(4-morpholinyl)-1-benzopyran-4-one is a member of dibenzothiophenes.
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| Molecular Formula |
C25H19NO3S
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|---|---|---|
| Molecular Weight |
413.49
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| Exact Mass |
413.108
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| Elemental Analysis |
C, 72.62; H, 4.63; N, 3.39; O, 11.61; S, 7.75
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| CAS # |
503468-95-9
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| Related CAS # |
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| PubChem CID |
11327430
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| Appearance |
Off-white to beige solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
646.9±55.0 °C at 760 mmHg
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| Melting Point |
246.28° C
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| Flash Point |
345.0±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
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| Index of Refraction |
1.732
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| LogP |
5.98
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
30
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| Complexity |
690
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C2=C([H])C([H])=C([H])C([H])=C2C2C([H])=C([H])C([H])=C(C1=2)C1=C([H])C([H])=C([H])C2C(C([H])=C(N3C([H])([H])C([H])([H])OC([H])([H])C3([H])[H])OC1=2)=O
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| InChi Key |
JAMULYFATHSZJM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H19NO3S/c27-21-15-23(26-11-13-28-14-12-26)29-24-17(6-3-9-20(21)24)19-8-4-7-18-16-5-1-2-10-22(16)30-25(18)19/h1-10,15H,11-14H2
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| Chemical Name |
8-dibenzothiophen-4-yl-2-morpholin-4-ylchromen-4-one
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| Synonyms |
NU7441; NU 7441; NU-7441; KU 57788; KU57788; KU-57788
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~4 mg/mL warming (~9.7 mM)
Water: <1 mg/mL (slightly soluble or insoluble) Ethanol: <1 mg/mL (slightly soluble or insoluble) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.43 mg/mL (3.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. AO:AO 4%DMSO+30%PEG 300+5%Tween 80+ddH2O: 1.0mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4184 mL | 12.0922 mL | 24.1844 mL | |
| 5 mM | 0.4837 mL | 2.4184 mL | 4.8369 mL | |
| 10 mM | 0.2418 mL | 1.2092 mL | 2.4184 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NU7441 (0.3 μM) enhances cellular senescence in irradiated H1299 cells.Cancer Sci.2016 Sep;107(9):1250-5. |
Both X‐rays and carbon ions induce radio‐sensitization in non‐small cell lung cancer (NSCLC) cells with nontoxic conce ntrations of NU7441 treatment.Cancer Sci.2016 Sep;107(9):1250-5. |
Non‐small cell lung cancer (NSCLC) cells treated with NU7441 (0.3 μM) and radiation show significant G2/M arrest.Cancer Sci.2016 Sep;107(9):1250-5. |
Low concentration of NU7441 does not seem to show double strand break (DSB) repair inhibition in X‐ray‐irradiated and carbon‐irradiated non‐small cell lung cancer (NSCLC) cells.Cancer Sci.2016 Sep;107(9):1250-5. |
NU7441 (0.3 μM) causes a remarkable increase of DNA fragmentation in irradiated H1299 cells.Cancer Sci.2016 Sep;107(9):1250-5. |
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