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CAS No.: 61422-45-5

Carmofur/卡莫氟 Catalog No. CSN10553

Synonyms: HCFU;1hexylcarbamoyl5fluorouracil;卡莫氟

Carmofur is an antimetabolite used as an antineoplastic agent, it's a derivative of fluorouracil.

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技术信息

生物活性

描述Carmofur is a well-studied ASAH1 (Acid ceramidase) inhibitor and antineoplastic drugwhich has been shown to have effect on several kinds of cancers, including cervical cancers, breast cancer, glioma, etc.. It shows antiproliferation and antimetastatic properties against cervical cancers, and the Wnt/β-catenin signaling pathway seems to play a role. Carmofur is capable of penetrating the blood-brain barrier, however, its extent to which it is able to penetrate brain tumors remains unknown. Carmofur is also shown as a dual FAAH (IC50 = 0.11 ± 0.025μM) and NAAA (IC50 = 0.71 ± 0.054 μM) inhibitor. It attenuated LPS-induced ALI in a PPARα- and CB2-dependent mechanism. In Raw264.7 macrophages, treatment with carmofur at 10μM for 72h effectively reduced the mRNA expression of pro-inﬂammatory factors, including IL-1β, IL-6, iNOS, and TNF-α, and down-regulated signaling proteins of the nuclear transcription factor κB (NF-κB) pathway. Oral administration of carmofur at 10mg/kg (5% PEG/5%Tween-80 as vehicle) signifcantly ameliorated the inﬂammatory responses and promoted resolution of pulmonary injury in lipopolysaccharide (LPS)-induced ALI mice. Recent study found that carmofur showed inhibition effect on 2019-nCoV.
作用机制Carmofur contains an electrophilic carbonyl reactive group that targets the catalytic cysteine. The fatty acid moiety of the carmofur molecule after catalytic cleavage of the inhibitor at its carbonyl group covalently modifies the active site Cys143 and occupies one of the hydrophobic cavities close to the enzyme active site.
参考文献

[1] Akiba T, Okeda R, et al. Metabolites of 5-fluorouracil, alpha-fluoro-beta-alanine and fluoroacetic acid, directly injure myelinated fibers in tissue culture. Acta Neuropathol. 1996 Jul;92(1):8-13.
[2] Kuzuhara S, Ohkoshi N, et al. Subacute leucoencephalopathy induced by carmofur, a 5-fluorouracil derivative. J Neurol. 1987 Aug;234(6):365-70.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.8871 mL
- 19.4356 mL
- 38.8712 mL
- 5 mM
- 0.7774 mL
- 3.8871 mL
- 7.7742 mL
- 10 mM
- 0.3887 mL
- 1.9436 mL
- 3.8871 mL

技术信息

CAS号

61422-45-5

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C11H16FN3O3

运输

蓝冰

分子量

257.26

别名

HCFU;1hexylcarbamoyl5fluorouracil;卡莫氟

溶解度

DMSO	10.0 mg/mL (38.9 mM)
Water	insoluble

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