dA-NHbenzylOCF3
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dA-NHbenzylOCF3 is a DNA-targeted radiosensitizer that enhances the sensitivity of tumor cells to X-rays via the dissociative electron attachment (DEA) mechanism. dA-NHbenzylOCF3 shows low cytotoxicity to normal cells and mainly localizes to the cytoplasm and nucleus after entering cells. dA-NHbenzylOCF3 exerts its radiosensitizing effect by inducing cell cycle arrest at the radiation-sensitive G2/M phase. dA-NHbenzylOCF3 can be used for radiosensitization research on malignant tumors such as prostate cancer and breast cancer.
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- Reinheit: 98.04%
- Formel: C18H19F3N6O4
- Molecular Weight:440.38
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
dA-NHbenzylOCF3 (0.001-100 µM; 48-72 h) exhibits low cytotoxicity against PC3, MCF-7 and HaCaT cells, with statistically significant decreases in cell viability observed only at 20 µM (PC3, 72 h) and 100 µM (all cell lines, 48/72 h)[1].
dA-NHbenzylOCF3 (20 µM; administered 48 h prior to irradiation with 1, 3, 4 Gy) significantly enhances the radiosensitivity of PC3 and MCF-7 cells to X-rays at a statistical level, with stronger activity against PC3 cells (an α elevation factor of 2.1 versus 1.5 for MCF-7 cells), and the dose enhancement factors are 1.30 (PC3) and 1.21 (MCF-7), respectively[1].
When combined with X-ray irradiation, dA-NHbenzylOCF3 (20 µM; treated for 48 h before 8 Gy irradiation; incubated for 24 h after irradiation) regulates the cell cycle progression of PC3 and MCF-7 cells, increases the proportion of cells in the radiation-sensitive G2/M phase, and this effect is more pronounced in PC3 cells[1].
dA-NHbenzylOCF3 (20-100 µM; 48 h) penetrates PC3 cells, localizes primarily in the cytoplasm (with a cytoplasm-to-nucleus ratio ranging from 26:1 to 22:1), and exists exclusively in the non-phosphorylated form[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3 (human prostate cancer), MCF-7 (human breast cancer), HaCaT (immortalized human keratinocyte)
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Concentration:0.001, 0.01, 0.1, 1, 10, 20, 100 µM
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Incubation Time:48 h; 72 h
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Result:Reduced PC3 cell viability to 86.3% (48 h) and 80.8% (72 h,) at 100 µM; reduced viability to 88.5% (72 h) at 20 µM.
Reduced MCF-7 cell viability to 91.9% (48 h) and 87.5% (72 h) at 100 µM.
Reduced HaCaT cell viability to 84.2% (48 h) and 76.3% (72 h) at 100 µM.
Caused no statistically significant viability reduction at lower tested concentrations for any cell line.
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Cell Line:PC3 (human prostate cancer), MCF-7 (human breast cancer)
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Concentration:20 µM
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Incubation Time:48 h prior to irradiation with 8 Gy; 24 h incubation post-irradiation
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Result:Reduced PC3 cell G0/G1 phase fraction from 47.8% to 36.3% and increased G2/M phase fraction from 46.1% to 56.8% when combined with 8 Gy irradiation compared to irradiation alone.
Reduced MCF-7 cell G0/G1 phase fraction from 43.3% to 41.7% and increased G2/M phase fraction from 43.8% to 48.4% when combined with 8 Gy irradiation compared to irradiation alone.
Had no significant effect on cell cycle distribution compared to control when used alone in either cell line.
Chemical Information
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Appearance Solid
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Molecular Weight 440.38
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Formel C18H19F3N6O4
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Color White to off-white
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SMILES
O[C@H]1C[C@@H](O[C@@H]1CO)N2C(NCC3=CC=C(OC(F)(F)F)C=C3)=NC4=C(N=CN=C42)N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)