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NU7441 (KU-57788) Europäischer Partner

Hersteller Selleckchem
Kategorie
Typ Inhibitors
Specific against other
Menge 50 mg
ArtNr S2638-50
CAS-Nr. 503468-95-9
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
Administration
Intraperitoneally administrated
Animal Models
Female rude mice bearing SW620 xenografts
Cell lines
SW620, LoVo, V3-YAC and V3 cells
Chemical Name
4H-1-Benzopyran-4-one, 8-(4-dibenzothienyl)-2-(4-morpholinyl)-
Concentrations
0.5 uM or 1 uM
Description
NU7441 is a highly potent and selective DNA-PK inhibitor with IC50 of 14 nM and also inhibits PI3K with IC50 of 5 uM.
Dosages
10 mg/kg
Formulation
Sterile 0.9% sodium chloride solution
IC50
14 nM [1], 14 nM [1], 14 nM [1], 14 nM [1], 14 nM [1], 14 nM [1]
In vitro
NU7441 increases the persistence of gammaH2AX foci after ionizing radiation–induced or etoposide-induced DNA damage. NU7441 (0.5 uM or 1 uM) appreciably increases G2-M accumulation induced by ionizing radiation, etoposide, and doxorubicin in both SW620 and LoVo cells. [2] NU7441 causes persistence of doxorubicin- and ionising radiation-induced DNA double-strand break and also slightly decreases homologous recombination activity DNA-PK-proficient M059-Fus-1 and DNA-PK-deficient M059 J human tumour cells. [3] NU7441 inhibits UV-induced RPA p34 hyperphosphorylation in a dose-dependent manner both in cells lacking and cells expressing polymerase eta. [4] NU7441 increases levels of fludarabine-induced gammaH2AX foci and correspondingly decreased fludarabine-induced cell death in chronic lymphocytic leukemia cells. [5] NU7441 also inhibits mitoxantrone-induced DNA-PKcs autophosphorylation and repair in chronic lymphocytic leukemia cells. [6]
In vivo
NU7441 intraperitoneally administrated at dose of 10 mg/kg maintains for at least 4 hours shows nontoxic and increases etoposide-induced tumor growth delay 2-fold in mice bearing SW620 xenografts. [2]
Incubation Time
17 hours
Method
The effect of NU7441 on cellular survival following exposure to etoposide, doxorubicin, and ionizing radiation is measured in SW620, LoVo, V3, and V3-YAC cells by clonogenic assays. Briefly, growing cells in six-well plates or 6-cm dishes are exposed to etoposide or doxorubicin with or without NU7441 (0.5 or 1.0 uM) for 16 hours. For radiosensitization studies, NU7441 is added to the cells 1 hour before irradiation. V3 and V3-YAC cells are exposed to gamma-irradiation (3.1 Gy/min 137Cesium). SW620 and LoVo are exposed to X-irradiation (2.9 Gy/min at 230 kV, 10 mA) due to the equipment available. After irradiation, the cells are incubated with or without NU7441 for a further 16 hours. Cells are then harvested by trypsinization, counted, and seeded into 10-cm diameter Petri dishes at densities varying from 100 to 105 per dish in drug-free medium for colony formation. Colonies are stained with crystal violet after 10 to 14 days and counted with an automated colony counter. The survival reduction factor (SRF) is calculated as the surviving fraction of cells in the absence of NU7441 divided by the surviving fraction of cells in the presence of NU7441 for any given dose or concentration of cytotoxic agent. The dose modification ratio (DMR90) is calculated as the concentration/dose of cytotoxic agent required to kill 90% of the cells in the absence of NU7441 divided by the concentration/dose of cytotoxic agent required to kill 90% of the cells in the presence of NU7441.
Molecular Weight (MW)
413, 49
Picture ChemicalStructure Description
NU7441 (KU-57788) Chemical Structure
Picture Description 1
Data independently produced by Dr. Zhang of Tianjin Medical University, , NU7441 (KU-57788)purchased from Selleck, After starved in serum-free medium for 24h, A549 cells incubated with the indicated concentrations of NU-7441 for 3h, followed by 20-minute stimolation of 100ng/ml EGF.
Solubility (25C)
DMSO 3 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Storage
2 years -20CPowder, 2 weeks4Cin DMSO, 2 months-80Cin DMSO

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Alle Produkte sind nur für Forschungszwecke bestimmt. Nicht für den menschlichen, tierärztlichen oder therapeutischen Gebrauch.

Menge: 50 mg
Lieferbar: In stock
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Lieferung vsl. bis 16.05.2024 

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