Carmofur (Synonyms: HCFU) |
| カタログ番号GC12748 |
5-フルオロウラシルの誘導体であるカルモフール (HCFU) は、抗腫瘍薬です。カルモフールは、ラット酵素の IC50 が 79 nM の酸性セラミダーゼの阻害剤です。カルモフールは、SARS-CoV-2 のメイン プロテアーゼ (Mpro) を阻害します。 Carmofur は Vero E6 細胞の SARS-CoV-2 を 24.3 μM の EC50 で阻害します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 61422-45-5
Sample solution is provided at 25 µL, 10mM.
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Carmofur is a derivative of fluorouracil, an antimetabolite used as an antineoplastic agent. Target: Nucleoside antimetabolite/analogCarmofur, which is used in the clinic to treat colorectal cancers, is a potent AC inhibitor and that this property is essential to its anti-proliferative effects. Carmofur inhibited AC activity with a median effective concentration (IC50) of 29 ± 5 nM (mean ± standard error of the mean, s.e.m.; n = 4), whereas 5-FU had no such effect (IC50>1 mM). systemic administration of carmofur (10 or 30 mg-kg-1, intraperitoneal, i.p.) to mice produced a dose-dependent inhibition of AC activity in various tissues, including lungs and brain cortex.
References:
[1]. Realini, N., et al., Discovery of highly potent acid ceramidase inhibitors with in vitro tumor chemosensitizing activity. Sci Rep, 2013. 3: p. 1035.
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