Fluorouracil (5-Fluoracil, 5-FU)

目录号:S1209 别名: NSC 19893

Fluorouracil (5-Fluoracil, 5-FU) Chemical Structure

Molecular Weight(MW): 130.08

Fluorouracil (5-Fluoracil, 5-FU)是DNA/RNA合成抑制剂,在肿瘤细胞中通过抑制胸苷酸合成酶(TS)而干扰核苷酸合成。

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产品安全说明书

DNA/RNA Synthesis抑制剂选择性比较

生物活性

产品描述 Fluorouracil (5-Fluoracil, 5-FU)是DNA/RNA合成抑制剂,在肿瘤细胞中通过抑制胸苷酸合成酶(TS)而干扰核苷酸合成。
靶点
Thymidylate synthase [1]
(Tumor cells)
体外研究

Adrucil是一种尿嘧啶类似物,在C-5位置上有一个氟原子。利用和尿嘧啶一致的转运途径快速进入细胞。Adrucil在细胞内转化成几个活性代谢物:氟脱氧尿苷单磷酸盐(FdUMP),氟脱氧尿苷三磷酸盐(FdUTP) 以及氟尿苷三磷酸盐 (FUTP)。Adrucil的代谢物FdUMP结合到TS核苷酸结合位点,与CH2THF形成稳定的三聚体,进而阻断了正常的底物dUMP的结合,抑制了dTMP的合成。Adrucil代谢物能够插入DNA,导致DNA双链断裂和细胞死亡。Adrucil的促凋亡作用可能和激活肿瘤抑制因子P53有关。P53功能缺失降低细胞对Adrucil的敏感性。[1]Adrucil抑制存活诱导各种细胞的凋亡。Adrucil 抑制鼻咽癌细胞系CNE2 和 HONE的生存能力[2],Adrucil抑制Capan-1细胞的生存能力[3],Adrucil抑制HT-29细胞的生存能力[4],IC50 分别是 9 μg/mL, 3 μg/mL, 0.22 μM, 2.5 μM。

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF-7 MoTpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkK1O|LDqGkEoB?= MYrJR|UxRTJyIN88[{9uVA>? NXS4OplXOjRyOUWxO|Y>
HT-29 NY\1XmdST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUi3NuKhcMLi NXzZNmhsUUN3ME6gNlUh|rypL33M NEjNOYUzPDB7NUG3Oi=>
HL-60 NEK5N|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVi3NuKhcMLi NVrSWJZPUUN3ME24MlYxOSEQvHevcWw> M{XrfVI1ODl3MUe2
NCI-H292 NGPhUZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\MV4o4OsLiaNMg NWDXS5NmUUN3ME6gNlUh|rypL33M MnLxNlQxQTVzN{[=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p53 / PUMA / c-PARP; 

PubMed: 25965911     


(A) HCT-116 cells were treated with various doses of 5-FU for 24 hours (B) HCT-116 cells were treated with 200 uM 5-FU, then harvested at different time points after stimulation. The expression of p53, PUMA, cleaved PARP and P-Akt(S473) were detected by western blotting in different conditions.

25965911
Immunofluorescence
caveolin-3; 

PubMed: 23646193     


Cells were stained with an antibody against caveolin-3 (green) and with DAPI (blue). (A) control cells (top images), 10 mM 5-FU (middle images), 50 mM 5-FU (bottom images). Merged images are shown at the right of each panel.

phospho-histone H3 ; 

PubMed: 23646193     


Cells were grown for 24 h, treated with 5-FU and stained with an anti-phospho-histone H3 antibody (red) and with DAPI (blue). (A) control cells, (B) 0.1 mM 5-FU and (C) 1 mM 5-FU. 

p65 / p-p65(Ser536) / p53 / p-p53(Ser15); 

PubMed: 24587255     


E–H, Immunocytochemistry of p65 and p53 induction and localization by 5-FU treatment for the indicated cell lines. p65 (red), phosphor-p65 (Ser536; red), p53 (green), phospho-p53 (Ser15; red), and DAPI (blue) staining of the nucleus without (control) and with 5-FU treatment. 

Sox2 / Oct4 / Nanog / ABCG2; 

PubMed: 27009861     


(A) Immunofluorescence staining of Sox2, Oct4 and Nanog in HBE cells with or without 5-FU treatment. In untreated HBE cells, few Sox2, Oct4 or Nanog-positive cells were observed. After 5-FU treatment, the number of Sox2, Oct4 or Nanog-positive cells increased remarkably. Nuclei were counterstained with DAPI (blue). (B) Immunofluorescence staining of ABCG2 in HBE cells with or without 5-FU treatment. 

β-catenin; 

PubMed: 30111797     


Immunofluorescence detection of β-catenin in HCT-8 cells. Scale bar, 20 μm.

non-phospho β-catenin; 

PubMed: 28588704     


Effect of enhanced WNT signaling in Ell3 OE cells. Localization of non-phosphorylated β-catenin was analyzed by immunocytochemical staining in (A) control MCF-7 and (B) Ell3 OE treated with various 5-FU concentrations.

23646193 24587255 27009861 30111797 28588704
Growth inhibition assay
Cell viability; 

PubMed: 25965911     


Cells viability was analyzed using Cell Counting Kit-8 at 0, 3, 6, 12 and 24 hours after (A) 50, 100, 200, or 400 uM 5-FU treatment in HCT116 cells.

Cell proliferation; 

PubMed: 30250641     


(A) Cell proliferation assay with resveratrol in HCT116. Cells were treated with resveratrol at 0 ~ 200 μM for 72 hours and applied to MTS assay. (B) HCT116 cells were treated with 5-FU at 0~200 μM for 72 hours. (C)HCT116 cells were treated with resveratrol at 0 ~ 200 μM combined with 5-FU at 10 μM for 72 hours and applied to MTS assay. (D) DLD1 cell proliferation assay with resveratrol at 0 ~ 200 μM for 72 hours. (E) DLD1 cells were treated with 5-FU at 0~ 200 μM for 72 hours. (F) DLD1 cells were treated with resveratrol combined with 5-FU at 10 μM for 72 hours. Error bars represent standard deviation.

25965911 30250641
体内研究 Adrucil在治疗包括结肠癌,乳腺癌等各种癌症中有广泛应用。 [1]100毫克/千克 Adrucil显著抑制患有结肠癌小鼠的结肠Colon 38的生长,肿瘤复制时间(TD),生长延缓因子(GDF),和T/C分别是26.5 days,4.4, 和14%。[5]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[4]
+ 展开
  • Cell lines: 人类结肠癌细胞系 HT-29
  • Concentrations: ~25 μM
  • Incubation Time: 7天
  • Method: 在96孔板中Adrucil处理细胞7天后测量生长抑制(4000 HT-29 细胞/孔,在含10%透析的牛胎儿血清RPMI 1640 培养基中);细胞附着过夜后加入增加浓度的Adrucil。在培养结束时,细胞用磷酸盐缓冲盐水(pH 7.4)清洗3次,用10%三氯乙酸在4 ℃下固定 60分钟。用去离子水洗5次,加入0.4% 磺酰罗丹明溶液在室温染色15分钟。未被磺酰罗丹明着色的通过1%冰乙酸漂洗去除。然后,着色的细胞蛋白质干燥,溶解于10 mM Tris-HCl。探测器在540nm波长处测定光密度值。
    (Only for Reference)
动物实验:[5]
+ 展开
  • Animal Models: 38小鼠结肠癌结肠38
  • Formulation: PBS
  • Dosages: 100毫克/千克
  • Administration: 每周一次腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 26 mg/mL (199.87 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
saline (warming)
10mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 130.08
化学式

C4H3FN2O2

CAS号 51-21-8
稳定性 powder
in solvent
别名 NSC 19893

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03196180 Not yet recruiting High Grade Cervical Intraepithelial Neoplasia|p16 Positive Neoplastic Cells Present National Cancer Institute (NCI) July 31 2019 Phase 1
NCT03196180 Not yet recruiting High Grade Cervical Intraepithelial Neoplasia|p16 Positive Neoplastic Cells Present National Cancer Institute (NCI) July 31 2019 Phase 1
NCT03883919 Not yet recruiting Pancreatic Cancer|Pancreas Cancer|Cancer of the Pancreas Washington University School of Medicine|Ipsen June 30 2019 Phase 1
NCT03883919 Not yet recruiting Pancreatic Cancer|Pancreas Cancer|Cancer of the Pancreas Washington University School of Medicine|Ipsen June 30 2019 Phase 1
NCT03784326 Not yet recruiting Clinical Stage II Esophageal Adenocarcinoma AJCC v8|Clinical Stage II Gastroesophageal Junction Adenocarcinoma AJCC v8|Clinical Stage IIA Esophageal Adenocarcinoma AJCC v8|Clinical Stage IIA Gastroesophageal Junction Adenocarcinoma AJCC v8|Clinical Stage IIB Esophageal Adenocarcinoma AJCC v8|Clinical Stage IIB Gastroesophageal Junction Adenocarcinoma AJCC v8|Clinical Stage III Esophageal Adenocarcinoma AJCC v8|Clinical Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IB Esophageal Adenocarcinoma AJCC v8|Pathologic Stage IB Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IC Esophageal Adenocarcinoma AJCC v8|Pathologic Stage IC Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage II Esophageal Adenocarcinoma AJCC v8|Pathologic Stage II Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIA Esophageal Adenocarcinoma AJCC v8|Pathologic Stage IIA Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIB Esophageal Adenocarcinoma AJCC v8|Pathologic Stage IIB Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage III Esophageal Adenocarcinoma AJCC v8|Pathologic Stage III Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIIA Esophageal Adenocarcinoma AJCC v8|Pathologic Stage IIIA Gastroesophageal Junction Adenocarcinoma AJCC v8|Pathologic Stage IIIB Esophageal Adenocarcinoma AJCC v8|Pathologic Stage IIIB Gastroesophageal Junction Adenocarcinoma AJCC v8 M.D. Anderson Cancer Center|National Cancer Institute (NCI) May 31 2019 Early Phase 1
NCT03775265 Not yet recruiting Bladder Carcinoma Infiltrating the Muscle of the Bladder Wall|Bladder Urothelial Carcinoma|Stage II Bladder Cancer AJCC v8|Stage III Bladder Cancer AJCC v8|Stage IIIA Bladder Cancer AJCC v8 National Cancer Institute (NCI) May 9 2019 Phase 3

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操作手册

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常见问题及建议解决方法

  • 问题 1:

    I was wondering if the product #s1209 (5-fluorouracil) is suitable to inject into mice ?

  • 回答:

    S1209 is suitable to inject (I.P.) into mice as indicating in this paper: http://www.ncbi.nlm.nih.gov/pubmed/8995503.

DNA/RNA Synthesis Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID