Etoposide phosphate disodium(Synonyms: BMY-40481 disodium)

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Etoposide phosphate disodium (Synonyms: BMY-40481 disodium)

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)。

Etoposide phosphate disodium(Synonyms: BMY-40481 disodium)

Etoposide phosphate disodium Chemical Structure

CAS No. : 122405-33-8

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Etoposide phosphate disodium 的其他形式现货产品:

Etoposide phosphate

生物活性

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

IC50 & Target[2]

Topoisomerase II

 

体外研究
(In Vitro)

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[1].
Etoposide phosphate disodium (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 disodium (25 μM; 6 hours) delays p53 recover in FBXW7-deficient cells. In addition, FBXW7 expression is disappeared in FBXW7-/- cells[2].

Shanghai Jinpan Biotech Co Ltd 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].

Shanghai Jinpan Biotech Co Ltd 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

712.50

Formula

C29H31Na2O16P
CAS 号

122405-33-8
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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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