5-FU (5-Fluorouracil)

製品コードS1209 バッチS120903

化学情報

	Synonyms	Fluorouracil, NSC 19893	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₄H₃FN₂O₂
	分子量	130.08	CAS No.	51-21-8
Solubility (25°C)*	体外	DMSO	26 mg/mL (199.87 mM)
		Water	10 mg/mL (76.87 mM)
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	5-FU (5-Fluorouracil) is a DNA/RNA synthesis inhibitor, which interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells. Fluorouracil induces apoptosis and can be used in the treatment of HIV.
in vitro	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. ^[1] 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 ^[2], pancreatic cancer cell lines Capan-1 ^[3], and human colon carcinoma cell line HT-29 ^[4] with IC50 of 9 μg/mL, 3 μg/mL, 0.22 μM, 2.5 μM, respectively.
in vivo	Adrucil is widely used in the treatment of a range of cancers, including colorectal and breast cancers. ^[1] 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%. ^[5]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Human colon carcinoma cell line HT-29
	濃度	~25 μM
	反応時間	7 days
	実験の流れ	Growth inhibition is measured after treatment of cells with Adrucil for 7 days in 96-well plates (4000 HT-29 cells/well in RPMI 1640 medium with 10% dialyzed fetal bovine serum); increasing concentrations of Adrucil are added after allowing for cell attachment overnight. At the end of incubation, cells are rinsed three times with phosphate-buffered saline (pH 7.4), fixed with 10% trichloroacetic acid for 60 min at 4 ℃, washed five times with deionized water, and stained with 0.4% sulforhoda-mine B solution for 15 min at room temperature. Unstained sulforhodamine B is removed by rinsing with 1% glacial acetic acid. Afterwards, stained cell proteins are dried and dissolved with 10 mM Tris-HCl. The optical density value is measured using a detector at 540 nm wavelength.
動物実験	動物モデル	Murine colon carcinomas Colon 38
	投薬量	100 mg/kg
	投与方法	i.p. weekly

参考

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カスタマーフィードバック

: Data from [Data independently produced by Mol Cell Biochem, 2014, 10.1007/s11010-014-2253-6]

: Data from [Data independently produced by , , J Invest Dermatol, 2018, 138(8):1716-1725]

: Data from [Data independently produced by , , Eur Rev Med Pharmacol Sci, 2016, 20(9):1699-706.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Synergistic antitumor activity between HER2 antibody-drug conjugate and chemotherapy for treating advanced colorectal cancer [ Cell Death Dis, 2024, 15(3):187]	PubMed: 38443386
A senescence restriction point acting on chromatin integrates oncogenic signals [ Cell Rep, 2024, 43(4):114044]	PubMed: 38568812
A functional personalised oncology approach against metastatic colorectal cancer in matched patient derived organoids [ NPJ Precis Oncol, 2024, 8(1):52]	PubMed: 38413740
Differential Expression of MicroRNA MiR-145 and MiR-155 Downstream Targets in Oral Cancers Exhibiting Limited Chemotherapy Resistance [ Int J Mol Sci, 2024, 25(4)2167]	PubMed: 38396844
Novel dual action PARP and microtubule polymerization inhibitor AMXI-5001 powerfully inhibits growth of esophageal carcinoma both alone and in combination with radiotherapy [ Am J Cancer Res, 2024, 14(1):378-389]	PubMed: 38323288
Molecular Mechanisms of Drug Resistance And Strategies of Sensitization in Breast Cancer [ Frontiers, 2024, 10.3389/978-2-8325-4184-5]	PubMed: none
ST6GAL1 is associated with poor response to chemoradiation in rectal cancer [ Neoplasia, 2024, 51:100984]	PubMed: 38467087
Transgelin-2, a novel cancer stem cell-related biomarker, is a diagnostic and therapeutic target for biliary tract cancer [ BMC Cancer, 2024, 24(1):357]	PubMed: 38509504
The ribosomal protein L22 binds the MDM4 pre-mRNA and promotes exon skipping to activate p53 upon nucleolar stress [ bioRxiv, 2024, 10.1101/2023.12.29.573614]	PubMed: none
The ribosomal protein L22 binds the MDM4 pre-mRNA and promotes exon skipping to activate p53 upon nucleolar stress [ bioRxiv, 2024, 10.1101/2023.12.29.573614]	PubMed: none

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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