Name: Floxuridine (FUDR)
Brand: Selleck Chemicals
SKU: S1299
Rating: 5 (11 reviews)

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.

Floxuridine (FUDR) Chemical Structure

CAS: 50-91-9

Selleck's Floxuridine (FUDR) has been cited by 11 publications

Purity & Quality Control

Batch: Purity: 99.99%

99.99

Floxuridine (FUDR) Related Products

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Signaling Pathway

DNA/RNA Synthesis Signaling Pathway

Choose Selective DNA/RNA Synthesis Inhibitors

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
CCRF-CEM cell	Growth inhibition assay			Tested in vitro for the inhibition of cell growth of human T lymphoblastoid CCRF-CEM cell line (ATCC CCL 119), IC50=0.5 μM	11909716
CCRF-CEM	Growth inhibition assay			In vitro concentration required for 50% inhibition of growth of human leukemia cell line CCRF-CEM with hPAP (0.2 unit/mL), GI50=0.0006 μM	11597404
LNCaP cells	Cytotoxicity assay			Cytotoxic concentration in prostate specific antigen (PSA) producing human LNCaP cells, IC50=0.0692 μM	12161157
TSU cells	Cytotoxicity assay			Cytotoxic concentration in non prostate specific antigen (PSA) producing human TSU cells, IC50=0.058 μM	12161157
KBALB cell	Cytotoxicity assay			In vitro cell cytotoxicity against KBALB cell line (transformed fibroblast sarcoma cell line), CC50=6.00E-05 μM	12620076
KBALB-STK cell	Cytotoxicity assay			In vitro cell cytotoxicity against KBALB-STK cell lines expressed in HSV-1 TK, IC50=8.80E-05 μM	12620076
L1210 mouse leukemia cells	Growth inhibition assay		24 h	Growth inhibition in L1210 mouse leukemia cells after 24 h treatment, IC50=0.0041 μM	11728193
L1210 mouse leukemia cells	Growth inhibition assay		48 h	Growth inhibition in L1210 mouse leukemia cells after 48 hr treatment, IC50=0.00064 μM	11728193
L5178Y cell	Growth inhibition assay			Comparative inhibition of L5178Y cell growth in vitro (concentration required for 50% inhibition), IC50=0.00076 μM	6779007
L5178Y cells	Function assay			Inhibitory concentration of compound was calculated on L5178Y cells by [14C]Leu incorporation, IC50=2 μM	8246229
L1210 mouse leukemia cells	Function assay		2 h	Thymidylate synthase inhibition in L1210 mouse leukemia cells after 2 hr treatment, IC50=0.0079 μM	11728193
LM cells	Function assay		2 h	Thymidylate synthase inhibition in thymidine kinase deficient LM cells after 2 hr treatment, IC50=5.4 μM	11728193
HT1080 cells	Function assay			Cytostatic activity against human HT1080 cells by MTT assay, IC50=0.18 μM	17804231
L1210 cells	Growth inhibition assay		72 h	Cytostatic activity against mouse L1210 cells ATCC CCL219 assessed as growth reduction after 72 hrs, IC50=0.012 μM	17997319
HL60 cells	Growth inhibition assay		72 h	Cytostatic activity against human HL60 cells ATCC CCL 240 assessed as growth reduction after 72 hrs, IC50=0.012 μM	17997319
CCRF-CEM cells	Growth inhibition assay		72 h	Cytostatic activity against human CCRF-CEM cells ATCC CCL 119 assessed as growth reduction after 72 hrs, IC50=0.017 μM	17997319
L1210 cells	Growth inhibition assay		72 h	Cytostatic activity in mouse L1210 cells assessed as inhibition of cell growth after 72 hrs, IC50=0.012 μM	18078757
HL60 cells	Growth inhibition assay		72 h	Cytostatic activity in human HL60 cells assessed as inhibition of cell growth after 72 hrs, IC50=0.012 μM	18078757
CCRF-CEM cells	Growth inhibition assay		72 h	Cytostatic activity in human CCRF-CEM cells assessed as inhibition of cell growth after 72 hrs, IC50=0.017 μM	18078757
CCRF-CEM cells	Function assay		48 h	Anticancer activity against human CCRF-CEM cells after 48 hrs by sulforhodamine B assay, GI50=0.00631 μM	19744858
K562 cells	Function assay		48 h	Anticancer activity against human K562 cells after 48 hrs by sulforhodamine B assay, GI50=0.79433 μM	19744858
MOLT4 cells	Function assay		48 h	Anticancer activity against human MOLT4 cells after 48 hrs by sulforhodamine B assay, GI50=0.03981 μM	19744858
RPMI8266 cells	Function assay		48 h	Anticancer activity against human RPMI8266 cells after 48 hrs by sulforhodamine B assay, GI50=0.79433 μM	19744858
human SR cells	Function assay		48 h	Anticancer activity against human SR cells after 48 hrs by sulforhodamine B assay, GI50=0.01259 μM	19744858
A549 cells	Function assay		48 h	Anticancer activity against human A549 cells after 48 hrs by sulforhodamine B assay, GI50=0.01259 μM	19744858
EKVX cells	Function assay		48 h	Anticancer activity against human EKVX cells after 48 hrs by sulforhodamine B assay, GI50=10 μM	19744858
HOP62 cells	Function assay		48 h	Anticancer activity against human HOP62 cells after 48 hrs by sulforhodamine B assay, GI50=0.02512 μM	19744858
HOP92 cells	Function assay		48 h	Anticancer activity against human HOP92 cells after 48 hrs by sulforhodamine B assay, GI50=0.79433 μM	19744858
NCI-H226 cells	Function assay		48 h	Anticancer activity against human NCI-H226 cells after 48 hrs by sulforhodamine B assay	19744858
NCI-H23	Function assay		48 h	Anticancer activity against human NCI-H23 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM	19744858
NCI-H322	Function assay		48 h	Anticancer activity against human NCI-H322M cells after 48 hrs by sulforhodamine B assay, GI50=0.50119 μM	19744858
NCI-H460	Function assay		48 h	Anticancer activity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay, GI50=0.50119 μM	19744858
NCI-H522	Function assay		48 h	Anticancer activity against human NCI-H522 cells after 48 hrs by sulforhodamine B assay, GI50=0.002 μM	19744858
COLO205 cells	Function assay		48 h	Anticancer activity against human COLO205 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM	19744858
HCC2998 cells	Function assay		48 h	Anticancer activity against human HCC2998 cells after 48 hrs by sulforhodamine B assay, GI50=1.58489 μM	19744858
HCT116 cells	Function assay		48 h	Anticancer activity against human HCT116 cells after 48 hrs by sulforhodamine B assay, GI50=0.001 μM	19744858
HCT15 cells	Function assay		48 h	Anticancer activity against human HCT15 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM	19744858
HT-29 cells	Function assay		48 h	Anticancer activity against human HT-29 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM	19744858
KM12 cells	Function assay		48 h	Anticancer activity against human KM12 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM	19744858
SW620 cells	Function assay		48 h	Anticancer activity against human SW620 cells after 48 hrs by sulforhodamine B assay, GI50=6.30957 μM	19744858
SF268 cells	Function assay		48 h	Anticancer activity against human SF268 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM	19744858
SF295 cells	Function assay		48 h	Anticancer activity against human SF295 cells after 48 hrs by sulforhodamine B assay, GI50=0.01259 μM	19744858
SF539 cells	Function assay		48 h	Anticancer activity against human SF539 cells after 48 hrs by sulforhodamine B assay, GI50=0.03981 μM	19744858
SNB19 cells	Function assay		48 h	Anticancer activity against human SNB19 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM	19744858
SNB75 cells	Function assay		48 h	Anticancer activity against human SNB75 cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM	19744858
U251 cells	Function assay		48 h	Anticancer activity against human U251 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM	19744858
LOXIMVI cells	Function assay		48 h	Anticancer activity against human LOXIMVI cells after 48 hrs by sulforhodamine B assay, GI50=0.02512 μM	19744858
MALME-3M cells	Function assay		48 h	Anticancer activity against human MALME-3M cells after 48 hrs by sulforhodamine B assay, GI50=7.94328 μM	19744858
M14 cells	Function assay		48 h	Anticancer activity against human M14 cells after 48 hrs by sulforhodamine B assay, GI50=0.15849 μM	19744858
SK-MEL-2 cells	Function assay		48 h	Anticancer activity against human SK-MEL-2 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM	19744858
SK-MEL-28 cells	Function assay		48 h	Anticancer activity against human SK-MEL-28 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM	19744858
SK-MEL-5 cells	Function assay		48 h	Anticancer activity against human SK-MEL-5 cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM	19744858
UACC257 cells	Function assay		48 h	Anticancer activity against human UACC257 cells after 48 hrs by sulforhodamine B assay, GI50=3.16228 μM	19744858
UACC62 cells	Function assay		48 h	Anticancer activity against human UACC62 cells after 48 hrs by sulforhodamine B assay, GI50=0.03981 μM	19744858
IGROV1 cells	Function assay		48 h	Anticancer activity against human IGROV1 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM	19744858
OVCAR-3 cells	Function assay		48 h	Anticancer activity against human OVCAR-3 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM	19744858
OVCAR4 cells	Function assay		48 h	Anticancer activity against human OVCAR4 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM	19744858
OVCAR5 cells	Function assay		48 h	Anticancer activity against human OVCAR5 cells after 48 hrs by sulforhodamine B assay, GI50=6.30957 Μm	19744858
OVCAR8 cells	Function assay		48 h	Anticancer activity against human OVCAR8 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM	19744858
SKOV3 cells	Function assay		48 h	Anticancer activity against human SKOV3 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM	19744858
786-0 cells	Function assay		48 h	Anticancer activity against human 786-0 cells after 48 hrs by sulforhodamine B assay, GI50=0.1 μM	19744858
A498 cells	Function assay		48 h	Anticancer activity against human A498 cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM	19744858
ACHN cells	Function assay		48 h	Anticancer activity against human ACHN cells after 48 hrs by sulforhodamine B assay, GI50=0.03162 μM	19744858
Caki1 cells	Function assay		48 h	Anticancer activity against human Caki1 cells after 48 hrs by sulforhodamine B assay, GI50=0.03162 μM	19744858
SN12C cells	Function assay		48 h	Anticancer activity against human SN12C cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM	19744858
TK10 cells	Function assay		48 h	Anticancer activity against human TK10 cells after 48 hrs by sulforhodamine B assay, GI50=5.01187 μM	19744858
UO31 cells	Function assay		48 h	Anticancer activity against human UO31 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM	19744858
PC3 cells	Function assay		48 h	Anticancer activity against human PC3 cells after 48 hrs by sulforhodamine B assay, GI50=0.31623 μM	19744858
DU145 cells	Function assay		48 h	Anticancer activity against human DU145 cells after 48 hrs by sulforhodamine B assay, GI50=0.25119 μM	19744858
MCF7 cells	Function assay		48 h	Anticancer activity against human MCF7 cells after 48 hrs by sulforhodamine B assay, GI50=0.00631 μM	19744858
NCI/ADR-RES cells	Function assay		48 h	Anticancer activity against human NCI/ADR-RES cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM	19744858
MDA-MB-231 cells	Function assay		48 h	Anticancer activity against human MDA-MB-231 cells after 48 hrs by sulforhodamine B assay, GI50=3.98107 μM	19744858
Hs 578T cells	Function assay		48 h	Anticancer activity against human Hs 578T cells after 48 hrs by sulforhodamine B assay, GI50=3.98107 μM	19744858
MDA-MB-435 cells	Function assay		48 h	Anticancer activity against human MDA-MB-435 cells after 48 hrs by sulforhodamine B assay, GI50=3.16228 μM	19744858
MDA-N cells	Function assay		48 h	Anticancer activity against human MDA-N cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM	19744858
BT549 cells	Function assay		48 h	Anticancer activity against human BT549 cells after 48 hrs by sulforhodamine B assay, GI50=1 μM	19744858
T47D cells	Function assay		48 h	Anticancer activity against human T47D cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM	19744858
HepG2 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, EC50=18.84 μM	19917528
A549 cells	Cytotoxicity assay		72 h	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, EC50=9.74 μM	19917528
LAC cells	Cytotoxicity assay		72 h	Cytotoxicity against human LAC cells after 72 hrs by MTT assay, EC50=32.09 μM	19917528
HeLa cells	Cytotoxicity assay		72 h	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, EC50=10.26 μM	19917528
MDA-MB-231 cells	Cytotoxicity assay			Cytotoxicity against human MDA-MB-231 cells overexpressing urokinase plasminogen activator, IC50=0.21 μM	20363130
human ACHN cells	Function assay			Anticancer activity against human ACHN cells by SRB assay, GI50=2.1 μM	20732810
PC3 cells	Function assay			Anticancer activity against human PC3 cells by SRB assay, GI50=4.97 μM	20732810
MDA-MB-231 cells	Function assay			Anticancer activity against human MDA-MB-231 cells by SRB assay, GI50=0.16 μM	20732810
FM3A cells	Function assay		2 days	Cytostatic activity against mouse FM3A cells after 2 days by coulter counting analysis, IC50=0.0094 μM	21330014
HeLa cells	Function assay			Cytostatic activity against human HeLa cells in presence of 20 uM thymidine, IC50=8.5 μM	21330014
LLC cells	Cytotoxicity assay		24 h	Cytotoxicity against mouse LLC cells after 24 hrs by resazurin assay, IC50=14.2 μM	21536448
LLC cells	Cytotoxicity assay		72 h	Cytotoxicity against mouse LLC cells after 72 hrs by resazurin assay, IC50=2 μM	21536448
RAW264.7 cells	Cytotoxicity assay		72 h	Cytotoxicity against mouse RAW264.7 cells after 72 hrs by resazurin assay, IC50=30 μM	21536448
A549 cells	Cytotoxicity assay		72 h	Cytotoxicity against human A549 cells assessed as cell viability after 72 hrs by WST-8 assay, IC50=0.047 μM	22248856
A2780 cells	Cytotoxicity assay		5 days	Cytotoxicity against human A2780 cells after 5 days by MTT assay, IC50=0.026 μM	22738636
LMTK cells	Cytotoxicity assay		5 days	Cytotoxicity against thymidine kinase-deficient mouse LMTK cells after 5 days by MTT assay, IC50=4.5 μM	22738636
A549 cells	Cytotoxicity assay		72 h	Cytotoxicity against human A549 cells after 72 hrs by microplate reader method, IC50=0.0124 μM	22847019
CEM cells	Function assay		72 h	Cytostatic activity against human CEM cells expressing human ENT1 transporter after 72 hrs by cell counting in presence of NBMPR, IC50=0.8 μM	21892829
Hela cells	Function assay		72 h	Cytostatic activity against human HeLa cells after 72 hrs by cell counting, IC50=0.05 μM	21892829
CEM/0 cells	Function assay		72 h	Cytostatic activity against human CEM/0 cells after 72 hrs by cell counting, IC50=0.022 μM	21892829
L1210/0 cells	Function assay		48 h	Cytostatic activity against mouse L1210/0 cells after 48 hrs by cell counting, IC50=0.0009 μM	21892829
MCF7 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay, IC50=12.19 μM	23867603
HeLa cells	Cytotoxicity assay		72 h	Cytotoxicity against human HeLa cells after 72 hrs by SRB assay, IC50=6.5 μM	23867603
HL60 cells	Proliferation assay		72 h	Antiproliferative activity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay, IC50=0.24 μM	25644674
SW707 cells	Proliferation assay		72 h	Antiproliferative activity against human SW707 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=23.86 μM	25644674
LoVo cells	Proliferation assay		72 h	Antiproliferative activity against human LoVo cells assessed as growth inhibition after 72 hrs by SRB method, IC50=19.07 μM	25644674
BALB/3T3 cell	Proliferation assay		72 h	Antiproliferative activity against mouse BALB/3T3 cells assessed as growth inhibition after 72 hrs by SRB method, IC50=23.9 μM	25644674
HFF cells	Function assay		72 h	Antiparasitic activity against Toxoplasma gondii ATCC 50839 infected in HFF cells after 72 hrs by beta-galactosidase reporter gene assay, EC50=0.91 μM	17698618
CCRFCEM cells	Function assay			Cytostatic activity against human CCRFCEM cells by MTT assay, IC50=0.29 μM	17804231
RXF393 cells	Function assay		48 h	Anticancer activity against human RXF393 cells after 48 hrs by sulforhodamine B assay, GI50=3.98107 μM	19744858
HL-60(TB) cells	Function assay		48 h	Anticancer activity against human HL-60(TB) cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM	19744858
L1210 cells	Function assay		15 mins	Inhibition of thymidylate synthase in mouse L1210 cells assessed as inhibition of tritium release from [5-3H]deoxyuridine after preincubation for 15 mins by liquid scintillation counting, IC50=0.0006 μM	21330014
Colo-357 cells	Function assay	100 μM	15 mins	Activity at MRP5 in human Colo-357 cells assessed as 5-FdUMP accumulation at 100 uM after 15 mins	20930123
KB cells	Cytotoxicity assay		72 h	Cytotoxicity against human KB cells after 72 hrs by SRB assay, IC50=8.69 μM	23867603
Click to View More Cell Line Experimental Data

Biological Activity

Description	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
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]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT01042691	Completed	Unresectable Colorectal Liver Metastases	David Bartlett\|The Pittsburgh Foundation\|Sanofi\|University of Pittsburgh	May 2003	Phase 1
NCT00695201	Completed	Colon Cancer\|Rectal Cancer	Memorial Sloan Kettering Cancer Center\|University of Medicine and Dentistry of New Jersey\|Rutgers The State University of New Jersey\|Sanofi	August 2000	Phase 1

References

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Chemical Information & Solubility

Molecular Weight	246.19	Formula	C₉H₁₁FN₂O₅
CAS No.	50-91-9	SDF	Download Floxuridine (FUDR) SDF
Smiles	C1C(C(OC1N2C=C(C(=O)NC2=O)F)CO)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 49 mg/mL ( (199.03 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 49 mg/mL

Ethanol : 10 mg/mL

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In vivo
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