产品说明书
5-Fluorouracil
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同义名 : | 5-氟脲嘧啶 ;5-FU;NSC 19893;Trade name: Adrucil and many others.;U-8953;Ro 2-9757;Fluorouracil |
| CAS号 : | 51-21-8 | |
| 货号 : | A370752 | |
| 分子式 : | C4H3FN2O2 | |
| 纯度 : | 98% | |
| 分子量 : | 130.08 | |
| MDL号 : | MFCD00006018 | |
| 存储条件： |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(384.39 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 10 mg/mL(76.88 mM)，配合低频超声，并水浴加热至45℃助溶 |
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| 动物实验配方： |
IP 2% DMSO+water 2 mg/mL clear PO 0.5% CMC-Na 60 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | 5-Fluorouracil (5-FU), or combined with other chemotherapeutic agents, is widely used in the treatment of a range of cancers, including colorectal and breast cancers, head and neck cancers, cancers of the aerodigestive tract[1]. 5-Fluorouracil can disrupt RNA synthesis through RNA mis-incorporation by its active metabolites, as well as block dTMP synthesis through inhibition of thymidylate synthase. After entering into cells, 5-Fluorouracil can be converted to its active metabolites, fluorodeoxyuridine monophosphate (FdUMP), fluorodeoxyuridine triphosphate (FdUTP) and fluorouridine triphosphate[2]. FdUMP can inhibit the thymidylate synthase through binding to the nucleotide-binding site of thymidylate synthase, thus blocking the binding of normal substrate dUMP and inhibiting dTMP synthesis. And this will cause the disruption of DNA replication and repair[3]. FUTP can extensively incorporate into RNA and disrupt RNA processing and function[4]. Thus, 5-Fluorouracil showed cytotoxicity in various cells. | ||
| 作用机制 | The mechanism of cytotoxicity of 5-FU has been ascribed to the mis-incorporation of fluoronucleotides into RNA and DNA, as well as the inhibition of thymidylate synthase[4]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| HL-60 | Growth Inhibition Assay | 72 h | IC50=8.601 μg/mL | 24095176 | |
| HT-29 | Growth Inhibition Assay | 72 h | IC50> 25 μg/mL | 24095176 | |
| MCF-7 | Growth Inhibition Assay | 72 h | IC50=20 μg/mL | 24095176 | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
7.69mL 1.54mL 0.77mL |
38.44mL 7.69mL 3.84mL |
76.88mL 15.38mL 7.69mL |
| 参考文献 |
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