Floxuridine (FUDR)

製品コードS1299 バッチS129905

印刷

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

12 mg/mL (48.74 mM)

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.650mg/ml (14.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 73 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.456mg/ml (1.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 9.12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	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 (FUDR) exhibits higher affinity for PEPT1 than the corresponding 5'-O-mono amino acid ester prodrugs. ^[1] When combined with Leucovorin, it results in synergistic inhibitory effects on growth of human T-lymphoblast leukemia cells. ^[2] This compound 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] It 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. It also results in prolonged effects on the proliferation of human Tenon's capsule fibroblasts in vitro. ^[4] Due to its short half life, steep dose response curve, high total body clearance, and high hepatic extraction, it is an ideal drug for hepatic arterial infusion (HAI). ^[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 (FUDR) exhibits higher affinity for PEPT1 than the corresponding 5'-O-mono amino acid ester prodrugs. ^[1] When combined with Leucovorin, it results in synergistic inhibitory effects on growth of human T-lymphoblast leukemia cells. ^[2] This compound 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] It 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. It also results in prolonged effects on the proliferation of human Tenon's capsule fibroblasts in vitro. ^[4] Due to its short half life, steep dose response curve, high total body clearance, and high hepatic extraction, it is an ideal drug for hepatic arterial infusion (HAI). ^[5]

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/18652477/
https://pubmed.ncbi.nlm.nih.gov/2950995/
https://pubmed.ncbi.nlm.nih.gov/16462026/

https://pubmed.ncbi.nlm.nih.gov/1386726/
https://pubmed.ncbi.nlm.nih.gov/19383854/

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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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