标签归档：泊苷

Etoposide phosphate(Synonyms: 磷酸依托泊苷; BMY-40481)

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Etoposide phosphate (Synonyms: 磷酸依托泊苷; BMY-40481) 纯度: 98.40%

Etoposide phosphate (BMY-40481) 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 是依托泊苷的磷酸酯前药，被认为与 Etoposide 活性相当。Etoposide phosphate 诱导细胞周期阻滞、凋亡 (apoptosis) 和自噬 (autophagy)。

Etoposide phosphate(Synonyms: 磷酸依托泊苷; BMY-40481)

Etoposide phosphate Chemical Structure

CAS No. : 117091-64-2

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10 mg ￥1300 In-stock
25 mg ￥2600 In-stock
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生物活性

Etoposide phosphate (BMY-40481) is a potent anti-cancer chemotherapy agent and a selective topoisomerase II inhibitor to prevent re-ligation of DNA strands. Etoposide phosphate is the phosphate ester prodrug of etoposide and is considered as active equivalent to Etoposide. Etoposide phosphate induces cell cycle arrest, apoptosis, and autophagy[1][2].

IC50 & Target[1]

Topoisomerase II

 

体外研究
(In Vitro)

Etoposide phosphate 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[1].
Etoposide phosphate (0-1 μM; 72 hours) inhibits HCT116 FBXW+/+, FBXW-/- and p53-/- as a dose-dependent manner, exhibits IC50 values of 0.945 μM; 0.375 μM; and 1.437 μM, respectively[2].
Etoposide phosphate (25 μM; 6 hours) delays p53 recover in FBXW7-deficient cells. In addition, FBXW7 expression is disappeared in FBXW7-/- cells[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

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[2]

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.

体内研究
(In Vivo)

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[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female CD-1 mice[3]
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).

Clinical Trial

分子量

668.54

Formula

C29H33O16P
CAS 号

117091-64-2
中文名称

磷酸依托泊苷
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O : 125 mg/mL (186.97 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4958 mL 7.4790 mL 14.9580 mL
5 mM 0.2992 mL 1.4958 mL 2.9916 mL
10 mM 0.1496 mL 0.7479 mL 1.4958 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
参考文献

  • [1]. Witterland AH, et al. Etoposide phosphate, the water soluble prodrug of etoposide. Pharm World Sci. 1996 Oct;18(5):163-70.

    [2]. Cui D, et al. FBXW7 Confers Radiation Survival by Targeting p53 for Degradation.Cell Rep. 2020 Jan 14;30(2):497-509.e4.

    [3]. Bregman CL, et al. Etoposide- and BMY-40481-induced sensory neuropathy in mice.Toxicol Pathol. 1994 Sep-Oct;22(5):528-35.

    [4]. SUMMARY OF PRODUCT CHARACTERISTICS

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