Floxuridine (FUDR)

製品コードS1299 バッチS129903

化学情報

	Synonyms	NSC 27640, Deoxyfluorouridine	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₉H₁₁FN₂O₅
	分子量	246.19	CAS No.	50-91-9
Solubility (25°C)*	体外	DMSO	49 mg/mL (199.03 mM)
		Water	49 mg/mL (199.03 mM)
		Ethanol	10 mg/mL (40.61 mM)
* <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.

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生物活性

製品説明	Floxuridine (FUDR) is a prodrug that is rapidly catabolized to 5-fluorouracil in vivo. Floxuridine is used to treat various cancers, particularly metastases to the liver. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage and apoptosis. Floxuridine has antiviral effects against HSV and CMV.
in vitro	Floxuridine exhibits higher affinity for PEPT1 than the corresponding 5'-O-mono amino acid ester prodrugs. ^[1] Floxuridine combined with Leucovorin results in synergistic inhibitory effects on growth of human T-lymphoblast leukemia cells. ^[2] Floxuridine significantly inhibits the uptake of both [(3)H]-inosine and [(3)H]-adenosine (60-70% of control), while its amino acid ester prodrugs including Val, Phe, Pro, Asp, and Lys esters exhibits markedly decreased inhibition potency (10-30% of control). ^[3] Floxuridine inhibits cell proliferation by more than 50% relative to the untreated control cells at 36 days, the cell numbers still increases fourfold compared with the initial cell density. Floxuridine results in prolonged effects on the proliferation of human Tenon's capsule fibroblasts in vitro. ^[4] Floxuridine (FUDR) is an ideal drug for hepatic arterial infusion (HAI) due to its short half life, steep dose response curve, high total body clearance, and high hepatic extraction. ^[5]

製品説明

Floxuridine (FUDR) is a prodrug that is rapidly catabolized to 5-fluorouracil in vivo. Floxuridine is used to treat various cancers, particularly metastases to the liver. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage and apoptosis. Floxuridine has antiviral effects against HSV and CMV.

in vitro

Floxuridine exhibits higher affinity for PEPT1 than the corresponding 5'-O-mono amino acid ester prodrugs. ^[1] Floxuridine combined with Leucovorin results in synergistic inhibitory effects on growth of human T-lymphoblast leukemia cells. ^[2] Floxuridine significantly inhibits the uptake of both [(3)H]-inosine and [(3)H]-adenosine (60-70% of control), while its amino acid ester prodrugs including Val, Phe, Pro, Asp, and Lys esters exhibits markedly decreased inhibition potency (10-30% of control). ^[3] Floxuridine inhibits cell proliferation by more than 50% relative to the untreated control cells at 36 days, the cell numbers still increases fourfold compared with the initial cell density. Floxuridine results in prolonged effects on the proliferation of human Tenon's capsule fibroblasts in vitro. ^[4] Floxuridine (FUDR) is an ideal drug for hepatic arterial infusion (HAI) due to its short half life, steep dose response curve, high total body clearance, and high hepatic extraction. ^[5]

プロトコル(参考用のみ)

参考

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Dependence on the Pyrimidine Biosynthetic Enzyme DHODH Is a Synthetic Lethal Vulnerability in Mutant KRAS-Driven Cancers. [ Cell Chem Biol, 2018, 25(6):705-717]	PubMed: 29628435

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