Etoposide phosphate

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Etoposide phosphate

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

117091-64-2

包装与价格：

包装	价格(元)
10 mM * 1 mL in Water	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品名称

磷酸依托泊苷
BMY-40481

产品介绍

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)。

生物活性

Etoposide phosphate (BMY-40481) is a potentanti-cancerchemotherapy agent and a selectivetopoisomeraseIIinhibitor 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 IC₅₀values 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].

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].

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

性状

Solid

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： PBS
Solubility: 100 mg/mL (149.58 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。