ETOPOSIDE PHOSPHATE DISODIUM

ETOPOSIDE PHOSPHATE DISODIUM

中文名称ETOPOSIDE PHOSPHATE DISODIUM
中文同义词
英文名称Etoposide phosphate disodium
英文同义词Etoposide phosphate disodium;BMY-40481 disodium
CAS号122405-33-8
分子式C29H34NaO16P
分子量692.54
EINECS号
相关类别
Mol文件122405-33-8.mol
结构式ETOPOSIDE PHOSPHATE DISODIUM 结构式

ETOPOSIDE PHOSPHATE DISODIUM 性质

ETOPOSIDE PHOSPHATE DISODIUM 用途与合成方法

Etoposide phosphate disodium (BMY-40481 disodium) 是一种有效的抗癌 (anti-cancer) 化疗试剂和一种选择性拓扑异构酶 II (topoisomerase II) 抑制剂,可以防止 DNA 链的重新连接。Etoposide phosphate disodium 是依托泊苷的磷酸酯前药,被认为与 Etoposide 活性相当。Etoposide phosphate disodium 诱导细胞周期阻滞、凋亡 (apoptosis) 和自噬 (autophagy)。

Topoisomerase II

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.

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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