标签归档：fluorouracil

5-Fluorouracil

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5-FluorouracilCAS号： 51-21-8分子式： C4H3FN2O2分子量： 130.08描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)参考文献

产品描述
描述

Fluorouracil (5-Fluoracil, 5-FU)是DNA/RNA合成抑制剂，通过抑制胸苷酸合成酶（TS）而干扰核苷酸合成。
纯度
>99%
储存/保存方法
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
基本信息
别名
5-氟脲嘧啶；5-FU
外观
白色或类白色结晶性粉末
可溶性/溶解性
DMSO : 13 mg/mL (100 mM)

Ethanol : 1.3 mg/mL (10 mM)
生物活性
靶点
Thymidylate synthase
In vitro(体外研究)
Adrucil is an analogue of uracil with a fluorine atom at the C-5 position in place of hydrogen. It rapidly enters the cell using the same facilitated transport mechanism as uracil. Adrucil is converted intracellularly to several active metabolites: fluorodeoxyuridine monophosphate (FdUMP), fluorodeoxyuridine triphosphate (FdUTP) and fluorouridine triphosphate (FUTP). The Adrucil metabolite FdUMP binds to the nucleotide-binding site of TS, forming a stable ternary complex with the enzyme and CH2THF, thereby blocking binding of the normal substrate dUMP and inhibiting dTMP synthesis. Metabolite of Adrucil also can be misincorporated into DNA, leading to DNA strand breaks and cell death. The pro-apoptosis effects of Adrucil may be related to its activation of tumor suppressor p53. Loss of p53 function reduces cellular sensitivity to Adrucil. Adrucil is able to inhibit the survival and induce apoptosis of a board range of cancer cells. Adrucil suppresses viabilities of the nasopharyngeal carcinoma cell line CNE2 and HONE1 , pancreatic cancer cell lines Capan-1 , and human colon carcinoma cell line HT-29 with IC50 of 9 μg/mL, 3 μg/mL, 0.22 μM, 2.5 μM, respectively.
In vivo(体内研究)
Adrucil is widely used in the treatment of a range of cancers, including colorectal and breast cancers. 100mg/kg Adrucil significantly suppresses tumor growth of murine colon carcinomas Colon 38 with tumor-doubling time (TD), growth-delay factor (GDF), and T/C of 26.5 days, 4.4, and 14%.
参考文献
参考文献
[1] Longley DB, et al. Nat Rev Cancer, 2003, 3(5), 330-338.
[2] Peters et al (2002) Induction of thymidylate synthase as a 5-fluorouracil resistance mechanism. Biochim.Biophys.Acta. 1587 194.
[3] Ghoshal and Jacob (1997) An alternative molecular mechanism of action of 5-fluorouracil, a potent anticancer drug. Biochem.Pharmacol. 53 1569.

分子结构图

5-Fluorouracil

5-Fluorouracil 5-氟尿嘧啶

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5-Fluorouracil 5-氟尿嘧啶

货号：
IF0170

品牌：
Jinpan

5-Fluorouracil 5-氟尿嘧啶

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产品简介
MDL MFCD00006018
EC EINECS 200-085-6
别名 双喃呋啶; ?氟尿嘧啶
CAS 51-21-8
分子式 C4H3FN2O2
分子量 130.08
纯度 HPLC≥98%
单位 瓶
生物活性 5-Fluorouracil 是一种有效的抗肿瘤剂，通过抑制胸苷酸合成酶从而消耗细胞内dTTP来影响嘧啶合成。[1-4]
In Vitro 5-氟尿嘧啶 (5-Fu) 和多柔比星 (Dox) 显示出协同抗癌功效。 5-Fu / Dox-DNM对人乳腺癌 (MDA-MB-231) 细胞的IC50值为0.25μg/ mL, 与Dox-DNM和5-Fu相比, 细胞毒性增加11.2倍和6.1倍。 -DNM分别为[1]。在5-氟尿嘧啶 (5-FU) 和CDDP处理的NFBD1抑制的NPC细胞中, 使用慢病毒介导的短发夹RNA消除NPC CNE1细胞系中的NFBD1表达, 并且这些细胞的敏感性升高。 NFBD1敲低导致CDDP或5-FU处理的CNE1细胞明显诱导细胞凋亡[3]。
In Vivo 5-氟尿嘧啶 (23 mg / kg, 3次/周) 持续14天, 在治疗开始后第3天诱导与急性肠道炎症相关的加速胃肠道转运, 这可能导致第7天后观察到的ENS持续变化治疗有助于延迟胃肠道转运和结肠运动障碍[1-4]。
SMILES O=C(N1)NC=C(F)C1=O
靶点 DNA/RNA Synthesis
动物实验 小鼠接受腹膜内注射5-FU (23mg / kg) , 每周3次, 通过26号针头。将5-FU溶于100％二甲基亚砜 (DMSO) 中, 使1M / L储备溶液在-20℃冷藏。然后将原料解冻并用无菌水稀释以制备0.1M / L (10％DMSO) 溶液用于腹膜内注射。计算5-FU的剂量等于每人体表面积的标准人剂量。低剂量的5-FU (10-40mg / kg) 已经显示出在小鼠癌症模型中具有抗肿瘤功效。假处理的小鼠通过26号针头每周三次通过腹膜内注射在无菌水中接受10％DMSO。注射体积按体重计算; 每次注射的最大体积不超过200μL。在第一次注射后3天 (2次治疗) , 7次 (3次治疗) 和14次 (6次治疗) , 通过颈脱位使小鼠安乐死, 并收集结肠用于体外实验。
数据来源文献 [1]. Han R, et al. Amphiphilic dendritic nanomicelle-mediated co-delivery of 5-fluorouracil and doxorubicin for enhanced therapeutic efficacy. J Drug Target. 2016 Jun 29:1-28. [Epub ahead of print]

[2]. McQuade RM, et al. Gastrointestinal dysfunction and enteric neurotoxicity following treatment with anticancer chemotherapeutic agent 5-fluorouracil. Neurogastroenterol Motil. 2016 Jun 28.

[3]. Zeng Q, et al. Knockdown of NFBD1/MDC1 enhances chemosensitivity to cisplatin or 5-fluorouracil in nasopharyngeal carcinoma CNE1 cells. Mol Cell Biochem. 2016 Jul; 418 (1-2) :137-46.

[4]. Yin L, et al. Antitumor effects of oncolytic herpes simplex virus type 2 against colorectal cancer in vitro and in vivo. Ther Clin Risk Manag. 2017 Feb 7; 13:117-130.
备注 以上数据均来自公开文献, Jinpan暂未进行独立验证, 仅供参考。These protocols are for reference only. Jinpan does not independently validate these methods.
规格 100mg 10mM*1mL (in DMSO) 200mg

具有抗肿瘤活性。是一种尿嘧啶的类似物 (nucleoside antimetabolite/analog)，可以通过抑制胸苷酸合成酶影响嘧啶的合成。