Etoposide phosphate
(Synonyms: 磷酸依托泊苷; BMY-40481) 目录号 : GC60826
Etoposidephosphate(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(topoisomeraseII)抑制剂,可以防止DNA链的重新连接。Etoposidephosphate是依托泊苷的磷酸酯前药,被认为与Etoposide活性相当。Etoposidephosphate诱导细胞周期阻滞、凋亡(apoptosis)和自噬(autophagy)。
Cas No.:117091-64-2
Sample solution is provided at 25 µL, 10mM.
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].
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]. Cell Viability Assay[2] Cell Line: FBXW+/+, FBXW-/- and p53-/- cell
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]
[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
Cas No. | 117091-64-2 | SDF | |
别名 | 磷酸依托泊苷; BMY-40481 | ||
Canonical SMILES | O=C1OC[C@]2([H])[C@H](O[C@H]3[C@@H]([C@H]([C@@H]([C@@H](CO4)O3)O[C@@H]4C)O)O)C5=C(C=C6OCOC6=C5)[C@@H](C7=CC(OC)=C(OP(O)(O)=O)C(OC)=C7)[C@]21[H] | ||
分子式 | C29H33O16P | 分子量 | 668.54 |
溶解度 | Water: 125 mg/mL (186.97 mM) | 储存条件 | Store at -20°C |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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1 mg | 5 mg | 10 mg |
1 mM | 1.4958 mL | 7.479 mL | 14.958 mL |
5 mM | 0.2992 mL | 1.4958 mL | 2.9916 mL |
10 mM | 0.1496 mL | 0.7479 mL | 1.4958 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
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