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122405-33-8

中文名稱 ETOPOSIDE PHOSPHATE DISODIUM
英文名稱 Etoposide phosphate disodium
CAS 122405-33-8
分子式 C29H34NaO16P
分子量 692.54
MOL 文件 122405-33-8.mol
122405-33-8 結(jié)構(gòu)式 122405-33-8 結(jié)構(gòu)式

基本信息

英文別名
BMY-40481 disodium
Etoposide phosphate disodium

常見問題列表

生物活性
Etoposide phosphate disodium (BMY-40481 disodium) 是一種有效的抗癌 (anti-cancer) 化療試劑和一種選擇性拓撲異構(gòu)酶 II (topoisomerase II) 抑制劑,可以防止 DNA 鏈的重新連接。Etoposide phosphate disodium 是依托泊苷的磷酸酯前藥,被認為與 Etoposide 活性相當。Etoposide phosphate disodium 誘導細胞周期阻滯、凋亡 (apoptosis) 和自噬 (autophagy)。
靶點

Topoisomerase II

體外研究

Etoposide phosphate disodium is a water-soluble derivative and probable prodrug of etoposide characterized by the presence of a phosphate group in position 4' of the E ring of the etoposide molecule.Etoposide phosphate disodium (0-1 μM; 72 hours) inhibits HCT116 FBXW +/+ , FBXW -/- and p53 -/- as a dose-dependent manner, exhibits IC 50 values of 0.945 μM; 0.375 μM; and 1.437 μM, respectively.Etoposide phosphate disodium (25 μM; 6 hours) delays p53 recover in FBXW7-deficient cells. In addition, FBXW7 expression is disappeared in FBXW7 -/- cells.

Cell Viability Assay

Cell Line: FBXW +/+ , FBXW -/- and p53 -/- cell
Concentration: 0.025 μM, 0.05 μM, 0.075 μM, 0.1 μM, 0.2 μM, 0.4 μM, 0.6 μM, 0.8 μM, 1 μM
Incubation Time: 72 hours
Result: Inhibited HCT116 FBXW +/+ , FBXW -/- and p53 -/- cell growth as a concentration manner.

Western Blot Analysis

Cell Line: HCT116 FBXW7 +/+ or FBXW7 -/- cells
Concentration: 25 μM
Incubation Time: 6 hours
Result: Exhibited that the recovery of p53 levels after DNA damage is mediated by FBXW7.
體內(nèi)研究

Etoposide phosphate (intravenous injection; 50, 100, or 150 mg/kg; single dose) has clinical symptomology of progressive ataxia, impaired righting reflex, and splaying and paresis of fore- and hindlimbs at day 8?in female CD-1 mice.

Animal Model: Female CD-1 mice
Dosage: 50, 100, or 150 mg/kg
Administration: Intravenous injection; single dose
Result: Observed degeneration of dorsal root ganglion cells and axonal degeneration of their distal and proximal processes in peripheral nerves, dorsal spinal roots, and dorsal funiculi of the spinal cord at all doses under light microscopy (LM).
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