Fluorouracil (Adrucil)
(Synonyms: 5-氟脲嘧啶; 5-FU) 目录号 : GC14466
氟尿嘧啶 (Adrucil) (5-FU) 是尿嘧啶的类似物，在 C-5 位置用氟原子代替氢 。
Cas No.:51-21-8
Sample solution is provided at 25 µL, 10mM.
Fluorouracil (Adrucil) (5-FU) is an analogue of uracil with a fluorine atom at the C-5 position in place of hydrogen [1]. Fluorouracil is widely used in the treatment of a range of cancers, including colorectal and breast cancers, and cancers of the aerodigestive tract [1].
The mechanism of cytotoxicity of Fluorouracil (Adrucil) has been ascribed to the misincorporation of fluoronucleotides into RNA and DNA and to the inhibition of the nucleotide synthetic enzyme thymidylate synthase (TS) [1]. Fluorouracil (Adrucil) at the concentration of 770µM treated HCT116 parental cell line and its 5-FU-resistant derivatives, Fluorouracil (Adrucil) led to a G1(/S) arrest at 8 and 24 hours [2]. The G1 arrest was most pronounced in ContinD cells at 24 hours, whereas the S phase arrest was most pronounced in parental HCT116 cells at 24 hours [3].
Fluorouracil (Adrucil) beneficial effected in intestinal tumorigenesis in the Apcmin/+ mice model where a 60-80% reduction in polyps [4]. Fluorouracil (Adrucil) reduces body weight, exacerbates symptom severity score, increases liver weight, and decreases epididymal fat mass, and decrease in survival [5].
References:
[1]. Longley D B, Harkin D P, Johnston P G. 5-fluorouracil: mechanisms of action and clinical strategies[J]. Nature reviews cancer, 2003, 3(5): 330-338.
[2]. Takeda H, Haisa M, Naomoto Y, Kawashima R, Satomoto K, Yamatuji T, Tanaka N: Effect of 5-fluorouracil on cell cycle regulatory proteins in human colon cancer cell line. Jpn J Cancer Res. 1999, 90: 677-684.
[3]. De Angelis P M, Svendsrud D H, Kravik K L, et al. Cellular response to 5-fluorouracil (5-FU) in 5-FU-resistant colon cancer cell lines during treatment and recovery[J]. Molecular cancer, 2006, 5(1): 1-25.
[4]. J.M. Tucker, C. Davis, M.E. Kitchens, et al. Response to 5-fluorouracil chemotherapy is modified by dietary folic acid deficiency in Apc(Min/+) mice. Cancer Lett., 187 (2002), pp. 153-162
[5]. Sougiannis A T, VanderVeen B N, Enos R T, et al. Impact of 5 fluorouracil chemotherapy on gut inflammation, functional parameters, and gut microbiota[J]. Brain, behavior, and immunity, 2019, 80: 44-55.
氟尿嘧啶 (Adrucil) (5-FU) 是尿嘧啶的类似物，在 C-5 位置用氟原子代替氢 [1]。氟尿嘧啶广泛用于治疗多种癌症，包括结直肠癌、乳腺癌和呼吸消化道癌症[1]。
氟尿嘧啶的细胞毒性作用机制（ Adrucil) 归因于氟核苷酸错误掺入 RNA 和 DNA 以及核苷酸合成酶胸苷酸合酶 (TS) [1] 的抑制。浓度为 770&88888181 的氟尿嘧啶 (Adrucil)；M 处理 HCT116 亲本细胞系及其 5-FU 抗性衍生物，氟尿嘧啶 (Adrucil) 在 8 小时和 24 小时导致 G1(/S) 停滞 [2]< /sup>。在 24 小时时，ContinD 细胞中的 G1 期停滞最明显，而在 24 小时时亲代 HCT116 细胞中的 S 期停滞最明显[3]。
氟尿嘧啶 (Adrucil)在 Apcmin/+ 小鼠模型中对肠道肿瘤发生产生有益影响，其中息肉减少 60-80% [4]。氟尿嘧啶 (Adrucil) 可减轻体重，加重症状严重程度评分，增加肝脏重量，减少附睾脂肪量，并降低生存率[5]。
| Cell experiment [1]: | |
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Cell lines |
HCT116 parental cell line (ATCC CCL247) and HCT116 ContinB and ContinD resistant derivatives (all wild-type TP53 cell lines) |
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Preparation Method |
770 µM Fluorouracil (Adrucil) (5-FU) was added to the media 24 hours after seeding. Cells were harvested by trypsinization or scraping at 0, 8, and 24 hours after addition of 5-FU to the culture medium. Control wells received no Fluorouracil (Adrucil). |
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Reaction Conditions |
770µM for 0, 8, and 24 hours |
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Applications |
Cells were treated with Fluorouracil (Adrucil) (5-FU) for 24 hours and followed for up to 40 days in drug-free medium. After day 7, the cell counts for ContinD increased steadily, the cell counts for ContinB and parental cultures began to increase after about 15 and 20 days, respectively. |
| Animal experiment [2]: | |
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Animal models |
Male C57BL/6 mice, azoxymethane/dextran sodium sulfate (AOM/DSS) model of CRC |
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Preparation Method |
Fluorouracil (Adrucil) (5-FU) was dissolved in sterile PBS, pH7.4 and then sterile filtered through a 0.2µm syringe filter. Fluorouracil was administered in 3 cycles; cycle 1: 40mg/kg, cycle 2 and 3: 20mg/kg via intraperitoneal injection. Fluorouracil was prepared fresh at the beginning of each cycle. Sterile filtered PBS alone was used as the vehicle control. Each cycle consisted of 5 consecutive days of injections followed by 9days of recovery. The treatment period lasted for 5weeks and mice were sacrificed 24 hr after the final injection of the third cycle. |
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Dosage form |
Intraperitoneal injection, 40mg/kg and 20mg/kg |
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Applications |
Fluorouracil reduces tumor burden but decreases survival in AOM/DSS mice. |
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References: [1]: De Angelis P M, Svendsrud D H, Kravik K L, et al. Cellular response to 5-fluorouracil (5-FU) in 5-FU-resistant colon cancer cell lines during treatment and recovery[J]. Molecular cancer, 2006, 5(1): 1-25. |
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| Cas No. | 51-21-8 | SDF | |
| 别名 | 5-氟脲嘧啶; 5-FU | ||
| 化学名 | 5-fluoro-1H-pyrimidine-2,4-dione | ||
| Canonical SMILES | C1=C(C(=O)NC(=O)N1)F | ||
| 分子式 | C4H3FN2O2 | 分子量 | 130.1 |
| 溶解度 | ≥ 6.5 mg/mL in DMSO, ≥ 10.04 mg/mL in Water with ultrasonic and warming | 储存条件 | 4°C, protect from light |
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 7.6864 mL | 38.432 mL | 76.864 mL |
| 5 mM | 1.5373 mL | 7.6864 mL | 15.3728 mL |
| 10 mM | 0.7686 mL | 3.8432 mL | 7.6864 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
