product name Floxuridine
Description: Floxuridine (also known as Deoxyfluorouridine, FDUR, NSC 27640) is an antineoplastic of the antimetabolite class, it is used in the treatment of colon carcinoma and colorectal cancer that has metastasized to the liver. It exhibits antiproliferative activity by inhibiting thymidylate synthetase and disrupting DNA replication in human cells. It induces double-strand DNA breaks and activates ATR and ATM signaling pathways. Floxuridine exhibits higher affinity for PEPT1 than the corresponding 5-O-mono amino acid ester prodrugs.
References: Mol Pharm. 2008 Sep-Oct;5(5):717-27; Cancer Treat Rep. 1987 Apr;71(4):381-9.
246.19
Formula
C9H11FN2O5
CAS No.
50-91-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 49 mg/mL (199.0 mM)
Water: 49 mg/mL (199.0 mM)
Ethanol: 49 mg/mL (199.0 mM)
Solubility (In vivo)
Synonyms
Deoxyfluorouridine, FDUR, NSC 27640
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19412337
| In Vitro |
In vitro activity: Floxuridine exhibits higher affinity for PEPT1 than the corresponding 5-O-mono amino acid ester prodrugs. Floxuridine combined with Leucovorin results in synergistic inhibitory effects on growth of human T-lymphoblast leukemia cells. 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). 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 Tenons capsule fibroblasts in vitro. 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. Kinase Assay: Cell Assay: |
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| In Vivo | |
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| Formulation & Dosage | |
| References | Mol Pharm. 2008 Sep-Oct;5(5):717-27; Cancer Treat Rep. 1987 Apr;71(4):381-9. |
