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  3. dA-NHbenzylOCF3

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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dA-NHbenzylOCF3

dA-NHbenzylOCF3 Chemical Structure

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Description

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[1].

In Vitro

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.

Cell Cytotoxicity Assay[1]

Cell Line: PC3 (human prostate cancer), MCF-7 (human breast cancer), HaCaT (immortalized human keratinocyte)
Concentration: 0.001, 0.01, 0.1, 1, 10, 20, 100 µM
Incubation Time: 48 h; 72 h
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.

Cell Cycle Analysis[1]

Cell Line: PC3 (human prostate cancer), MCF-7 (human breast cancer)
Concentration: 20 µM
Incubation Time: 48 h prior to irradiation with 8 Gy; 24 h incubation post-irradiation
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.
Molecular Weight

440.38

Formula

C18H19F3N6O4

Appearance

Solid

Color

White to off-white

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

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
Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
dA-NHbenzylOCF3
Cat. No.:
HY-176217
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