2F-Peracetyl-Fucose
(Synonyms: 2,6-二脱氧-2-氟-L-吡喃半乳糖三乙酸酯,1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos) 目录号 : GC46549
2F-Peracetyl-Fucose是岩藻糖基转移酶（FUT）抑制剂。
Cas No.:188783-78-0
Sample solution is provided at 25 µL, 10mM.
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2F-Peracetyl-Fucose is a fucosyltransferase (FUT) inhibitor[1].
In vitro, 2F-Peracetyl-Fucose (0, 25, 50, 100 and 200μM; 24h or 1h) suppressed transforming growth factor β (TGFβ)-mediated Smad3 phosphorylation and nuclear translocation in NSCLC cells[1]. The U251-MG cells treated with 2F-Peracetyl-Fucose (200μM; 5 days) were more sensitive to temozolomide (TMZ) administration. Moreover, treatment with 2F-Peracetyl-Fucose (200μM; 24h) also inhibited the Transwell invasion of U251-MG cells[2]. 2F-Peracetyl-Fucose (300μM; 72h) had no effect on healthy NP cells and further reduced collagen type 2 (COL2) expression in inflamed Nucleus Pulposus Cells (NP cells)[3].
In vivo, After being treated with 20µg/ml of 2F-Peracetyl-Fucose for 96 hours, Calu-1-Luc cells exhibited reduced metastatic capacity in a mouse model of non-small cell lung cancer (NSCLC) metastasis[1]. 2F-Peracetyl-Fucose (500μM; 0, 1, 3, 5 and 7 days) inhibits head regeneration in Dugesia japonica after anterior pharynx amputation[4].
References:
[1] Park S, Lim JM, Chun JN, et al. Altered expression of fucosylation pathway genes is associated with poor prognosis and tumor metastasis in non‑small cell lung cancer. Int J Oncol. 2020 Feb;56(2):559-567.
[2] Wei KC, Lin YC, Chen CH, et al. Fucosyltransferase 8 modulates receptor tyrosine kinase activation and temozolomide resistance in glioblastoma cells. Am J Cancer Res. 2021 Nov 15;11(11):5472-5484.
[3] Joyce K, Mohd Isa IL, Krouwels A, et al. The role of altered glycosylation in human nucleus pulposus cells in inflammation and degeneration. Eur Cell Mater. 2021 Mar 28;41:401-420.
[4] Wang W, Yu Y, Liu H, et al. Protein Core Fucosylation Regulates Planarian Head Regeneration via Neoblast Proliferation. Front Cell Dev Biol. 2021 Jul 16;9:625823.
2F-Peracetyl-Fucose是岩藻糖基转移酶（FUT）抑制剂[1]。
在体外实验中，2F-Peracetyl-Fucose（0, 25, 50, 100和200μM; 24小时或1小时）抑制了非小细胞肺癌（NSCLC）细胞中转化生长因子β（TGFβ）介导的Smad3磷酸化及其核转位[1]。用2F-Peracetyl-Fucose（200μM; 5天）处理的U251-MG细胞对替莫唑胺（TMZ）治疗更为敏感。此外，2F-Peracetyl-Fucose（200μM; 24小时）的处理还抑制了U251-MG细胞的Transwell侵袭能力[2]。2F-Peracetyl-Fucose（300μM; 72h）对健康的髓核细胞（NP细胞）没有影响，但降低了炎症髓核细胞中Ⅱ型胶原（COL2）的表达[3]。
在体内实验中，Calu-1-Luc细胞经20µg/ml的2F-Peracetyl-Fucose处理96小时后，在小鼠非小细胞肺癌（NSCLC）转移模型中，Calu-1-Luc细胞转移能力受到抑制[1]。2F-Peracetyl-Fucose（500μM; 0, 1, 3, 5和7天）在截断了前端咽部的日本三角涡虫（Dugesia japonica）中抑制了头部再生[4]。
| Cell experiment [1]: | |
Cell lines | NCI-H3122 cells |
Preparation Method | NCI-H3122 cells were transfected with a 3TP-Luc reporter construct for 24h and then incubated with TGFβ (1ng/ml) and 2F-Peracetyl-Fucose at different concentrations (0, 25, 50, 100, and 200µM) for 24h. The relative luciferase activity was calculated compared with that of the untreated cells. |
Reaction Conditions | 0, 25, 50, 100, and 200µM; 24 and 1h |
Applications | 2F-Peracetyl-Fucose suppressed transforming growth factor β (TGFβ)-mediated Smad3 phosphorylation and nuclear translocation in NSCLC cells. |
| Animal experiment [1]: | |
Animal models | BALB/c-nude mice, male, 8 weeks old |
Preparation Method | Calu-1-Luc cells were treated with 20µg/ml 2F-Peracetyl-Fucose for 96h. BALB/c-nude mice injected intravenously with 1x106 BALB/c-nude mice-treated Calu-1-Luc cells and analyzed 2 weeks later. For in vivo bioluminescence imaging (BLI), mice were injected intraperitoneally with D-Luciferin (150mg/kg, 200µl) under gas anesthesia and imaged 10min later using the IVIS spectrum system). BLI intensity was measured using region of interest analysis. |
Dosage form | 20µg/ml; 96h |
Applications | In a mouse model of NSCLC metastasis, 2F-Peracetyl-Fucose inhibited the metastatic capacity of Calu-1-Luc cells. |
References: | |
| Cas No. | 188783-78-0 | SDF | |
| 别名 | 2,6-二脱氧-2-氟-L-吡喃半乳糖三乙酸酯,1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos | ||
| Canonical SMILES | O=C(C)O[C@@H]([C@H]([C@@H]1F)OC(C)=O)[C@@H](OC1OC(C)=O)C | ||
| 分子式 | C12H17FO7 | 分子量 | 292.3 |
| 溶解度 | Chloroform: soluble,Methanol: soluble,DMSO: 10 mg/ml | 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 | 3.4211 mL | 17.1057 mL | 34.2114 mL |
| 5 mM | 0.6842 mL | 3.4211 mL | 6.8423 mL |
| 10 mM | 0.3421 mL | 1.7106 mL | 3.4211 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。
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Quality Control & SDS
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- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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