Home DNA Damage/DNA Repair DNA/RNA Synthesis Inhibitor Floxuridine (FUDR)

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Floxuridine (FUDR) DNA/RNA Synthesis Inhibitor

Kat.-Nr.S1299

Floxuridine (FUDR), ein Prodrug, das in vivo schnell zu 5-Fluorouracil katabolisiert wird, wird zur Behandlung verschiedener Krebserkrankungen, insbesondere Lebermetastasen, eingesetzt. Es hemmt die Poly(ADP-Ribose)-Polymerase und induziert DNA-Schäden und Apoptose. Diese Verbindung hat auch antivirale Wirkungen gegen HSV und CMV.
Floxuridine (FUDR) DNA/RNA Synthesis Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 246.19

Springe zu

Qualitätskontrolle

Charge: Reinheit: 99.99%
99.99

Zellkultur, Behandlung & Arbeitskonzentration

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung 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
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
LNCaP cells Cytotoxicity assay Cytotoxic concentration in prostate specific antigen (PSA) producing human LNCaP cells, IC50=0.0692 μM
TSU cells Cytotoxicity assay Cytotoxic concentration in non prostate specific antigen (PSA) producing human TSU cells, IC50=0.058 μM
KBALB cell Cytotoxicity assay In vitro cell cytotoxicity against KBALB cell line (transformed fibroblast sarcoma cell line), CC50=6.00E-05 μM
KBALB-STK cell Cytotoxicity assay In vitro cell cytotoxicity against KBALB-STK cell lines expressed in HSV-1 TK, IC50=8.80E-05 μM
L1210 mouse leukemia cells Growth inhibition assay 24 h Growth inhibition in L1210 mouse leukemia cells after 24 h treatment, IC50=0.0041 μM
L1210 mouse leukemia cells Growth inhibition assay 48 h Growth inhibition in L1210 mouse leukemia cells after 48 hr treatment, IC50=0.00064 μM
L5178Y cell Growth inhibition assay Comparative inhibition of L5178Y cell growth in vitro (concentration required for 50% inhibition), IC50=0.00076 μM
L5178Y cells Function assay Inhibitory concentration of compound was calculated on L5178Y cells by [14C]Leu incorporation, IC50=2 μM
L1210 mouse leukemia cells Function assay 2 h Thymidylate synthase inhibition in L1210 mouse leukemia cells after 2 hr treatment, IC50=0.0079 μM
LM cells Function assay 2 h Thymidylate synthase inhibition in thymidine kinase deficient LM cells after 2 hr treatment, IC50=5.4 μM
HT1080 cells Function assay Cytostatic activity against human HT1080 cells by MTT assay, IC50=0.18 μM
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
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
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
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
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
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
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
K562 cells Function assay 48 h Anticancer activity against human K562 cells after 48 hrs by sulforhodamine B assay, GI50=0.79433 μM
MOLT4 cells Function assay 48 h Anticancer activity against human MOLT4 cells after 48 hrs by sulforhodamine B assay, GI50=0.03981 μM
RPMI8266 cells Function assay 48 h Anticancer activity against human RPMI8266 cells after 48 hrs by sulforhodamine B assay, GI50=0.79433 μM
human SR cells Function assay 48 h Anticancer activity against human SR cells after 48 hrs by sulforhodamine B assay, GI50=0.01259 μM
A549 cells Function assay 48 h Anticancer activity against human A549 cells after 48 hrs by sulforhodamine B assay, GI50=0.01259 μM
EKVX cells Function assay 48 h Anticancer activity against human EKVX cells after 48 hrs by sulforhodamine B assay, GI50=10 μM
HOP62 cells Function assay 48 h Anticancer activity against human HOP62 cells after 48 hrs by sulforhodamine B assay, GI50=0.02512 μM
HOP92 cells Function assay 48 h Anticancer activity against human HOP92 cells after 48 hrs by sulforhodamine B assay, GI50=0.79433 μM
NCI-H226 cells Function assay 48 h Anticancer activity against human NCI-H226 cells after 48 hrs by sulforhodamine B assay
NCI-H23 Function assay 48 h Anticancer activity against human NCI-H23 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM
NCI-H322 Function assay 48 h Anticancer activity against human NCI-H322M cells after 48 hrs by sulforhodamine B assay, GI50=0.50119 μM
NCI-H460 Function assay 48 h Anticancer activity against human NCI-H460 cells after 48 hrs by sulforhodamine B assay, GI50=0.50119 μM
NCI-H522 Function assay 48 h Anticancer activity against human NCI-H522 cells after 48 hrs by sulforhodamine B assay, GI50=0.002 μM
COLO205 cells Function assay 48 h Anticancer activity against human COLO205 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM
HCC2998 cells Function assay 48 h Anticancer activity against human HCC2998 cells after 48 hrs by sulforhodamine B assay, GI50=1.58489 μM
HCT116 cells Function assay 48 h Anticancer activity against human HCT116 cells after 48 hrs by sulforhodamine B assay, GI50=0.001 μM
HCT15 cells Function assay 48 h Anticancer activity against human HCT15 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM
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
KM12 cells Function assay 48 h Anticancer activity against human KM12 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM
SW620 cells Function assay 48 h Anticancer activity against human SW620 cells after 48 hrs by sulforhodamine B assay, GI50=6.30957 μM
SF268 cells Function assay 48 h Anticancer activity against human SF268 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM
SF295 cells Function assay 48 h Anticancer activity against human SF295 cells after 48 hrs by sulforhodamine B assay, GI50=0.01259 μM
SF539 cells Function assay 48 h Anticancer activity against human SF539 cells after 48 hrs by sulforhodamine B assay, GI50=0.03981 μM
SNB19 cells Function assay 48 h Anticancer activity against human SNB19 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM
SNB75 cells Function assay 48 h Anticancer activity against human SNB75 cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM
U251 cells Function assay 48 h Anticancer activity against human U251 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM
LOXIMVI cells Function assay 48 h Anticancer activity against human LOXIMVI cells after 48 hrs by sulforhodamine B assay, GI50=0.02512 μM
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
M14 cells Function assay 48 h Anticancer activity against human M14 cells after 48 hrs by sulforhodamine B assay, GI50=0.15849 μM
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
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
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
UACC257 cells Function assay 48 h Anticancer activity against human UACC257 cells after 48 hrs by sulforhodamine B assay, GI50=3.16228 μM
UACC62 cells Function assay 48 h Anticancer activity against human UACC62 cells after 48 hrs by sulforhodamine B assay, GI50=0.03981 μM
IGROV1 cells Function assay 48 h Anticancer activity against human IGROV1 cells after 48 hrs by sulforhodamine B assay, GI50=2.51189 μM
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
OVCAR4 cells Function assay 48 h Anticancer activity against human OVCAR4 cells after 48 hrs by sulforhodamine B assay, GI50=10 μM
OVCAR5 cells Function assay 48 h Anticancer activity against human OVCAR5 cells after 48 hrs by sulforhodamine B assay, GI50=6.30957 Μm
OVCAR8 cells Function assay 48 h Anticancer activity against human OVCAR8 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM
SKOV3 cells Function assay 48 h Anticancer activity against human SKOV3 cells after 48 hrs by sulforhodamine B assay, GI50=1.99526 μM
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
A498 cells Function assay 48 h Anticancer activity against human A498 cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM
ACHN cells Function assay 48 h Anticancer activity against human ACHN cells after 48 hrs by sulforhodamine B assay, GI50=0.03162 μM
Caki1 cells Function assay 48 h Anticancer activity against human Caki1 cells after 48 hrs by sulforhodamine B assay, GI50=0.03162 μM
SN12C cells Function assay 48 h Anticancer activity against human SN12C cells after 48 hrs by sulforhodamine B assay, GI50=0.19953 μM
TK10 cells Function assay 48 h Anticancer activity against human TK10 cells after 48 hrs by sulforhodamine B assay, GI50=5.01187 μM
UO31 cells Function assay 48 h Anticancer activity against human UO31 cells after 48 hrs by sulforhodamine B assay, GI50=0.12589 μM
PC3 cells Function assay 48 h Anticancer activity against human PC3 cells after 48 hrs by sulforhodamine B assay, GI50=0.31623 μM
DU145 cells Function assay 48 h Anticancer activity against human DU145 cells after 48 hrs by sulforhodamine B assay, GI50=0.25119 μM
MCF7 cells Function assay 48 h Anticancer activity against human MCF7 cells after 48 hrs by sulforhodamine B assay, GI50=0.00631 μM
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
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
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
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
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
BT549 cells Function assay 48 h Anticancer activity against human BT549 cells after 48 hrs by sulforhodamine B assay, GI50=1 μM
T47D cells Function assay 48 h Anticancer activity against human T47D cells after 48 hrs by sulforhodamine B assay, GI50=1.25893 μM
HepG2 cells Cytotoxicity assay 72 h Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay, EC50=18.84 μM
A549 cells Cytotoxicity assay 72 h Cytotoxicity against human A549 cells after 72 hrs by MTT assay, EC50=9.74 μM
LAC cells Cytotoxicity assay 72 h Cytotoxicity against human LAC cells after 72 hrs by MTT assay, EC50=32.09 μM
HeLa cells Cytotoxicity assay 72 h Cytotoxicity against human HeLa cells after 72 hrs by MTT assay, EC50=10.26 μM
MDA-MB-231 cells Cytotoxicity assay Cytotoxicity against human MDA-MB-231 cells overexpressing urokinase plasminogen activator, IC50=0.21 μM
human ACHN cells Function assay Anticancer activity against human ACHN cells by SRB assay, GI50=2.1 μM
PC3 cells Function assay Anticancer activity against human PC3 cells by SRB assay, GI50=4.97 μM
MDA-MB-231 cells Function assay Anticancer activity against human MDA-MB-231 cells by SRB assay, GI50=0.16 μM
FM3A cells Function assay 2 days Cytostatic activity against mouse FM3A cells after 2 days by coulter counting analysis, IC50=0.0094 μM
HeLa cells Function assay Cytostatic activity against human HeLa cells in presence of 20 uM thymidine, IC50=8.5 μM
LLC cells Cytotoxicity assay 24 h Cytotoxicity against mouse LLC cells after 24 hrs by resazurin assay, IC50=14.2 μM
LLC cells Cytotoxicity assay 72 h Cytotoxicity against mouse LLC cells after 72 hrs by resazurin assay, IC50=2 μM
RAW264.7 cells Cytotoxicity assay 72 h Cytotoxicity against mouse RAW264.7 cells after 72 hrs by resazurin assay, IC50=30 μM
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
A2780 cells Cytotoxicity assay 5 days Cytotoxicity against human A2780 cells after 5 days by MTT assay, IC50=0.026 μM
LMTK cells Cytotoxicity assay 5 days Cytotoxicity against thymidine kinase-deficient mouse LMTK cells after 5 days by MTT assay, IC50=4.5 μM
A549 cells Cytotoxicity assay 72 h Cytotoxicity against human A549 cells after 72 hrs by microplate reader method, IC50=0.0124 μM
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
Hela cells Function assay 72 h Cytostatic activity against human HeLa cells after 72 hrs by cell counting, IC50=0.05 μM
CEM/0 cells Function assay 72 h Cytostatic activity against human CEM/0 cells after 72 hrs by cell counting, IC50=0.022 μM
L1210/0 cells Function assay 48 h Cytostatic activity against mouse L1210/0 cells after 48 hrs by cell counting, IC50=0.0009 μM
MCF7 cells Cytotoxicity assay 72 h Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay, IC50=12.19 μM
HeLa cells Cytotoxicity assay 72 h Cytotoxicity against human HeLa cells after 72 hrs by SRB assay, IC50=6.5 μM
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
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
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
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
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
CCRFCEM cells Function assay Cytostatic activity against human CCRFCEM cells by MTT assay, IC50=0.29 μM
RXF393 cells Function assay 48 h Anticancer activity against human RXF393 cells after 48 hrs by sulforhodamine B assay, GI50=3.98107 μM
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
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
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
KB cells Cytotoxicity assay 72 h Cytotoxicity against human KB cells after 72 hrs by SRB assay, IC50=8.69 μM
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Chemische Informationen, Lagerung & Stabilität

Molekulargewicht 246.19 Formel

C9H11FN2O5

 Lagerung (Ab dem Eingangsdatum)
CAS-Nr. 50-91-9 SDF herunterladen Lagerung von Stammlösungen

Synonyme NSC 27640, Deoxyfluorouridine Smiles C1C(C(OC1N2C=C(C(=O)NC2=O)F)CO)O

Löslichkeit

In vitro
Charge:

DMSO : 49 mg/mL (199.03 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : 49 mg/mL

Ethanol : 10 mg/mL

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewichtsrechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus

In vitro
Floxuridine (FUDR) weist eine höhere Affinität zu PEPT1 auf als die entsprechenden 5'-O-Monoaminosäureester-Prodrugs. In Kombination mit Leucovorin führt es zu synergistischen hemmenden Effekten auf das Wachstum menschlicher T-Lymphoblasten-Leukämiezellen. Diese Verbindung hemmt signifikant die Aufnahme von sowohl [(3)H]-Inosin als auch [(3)H]-Adenosin (60-70 % der Kontrolle), während ihre Aminosäureester-Prodrugs, einschließlich Val-, Phe-, Pro-, Asp- und Lys-Ester, eine deutlich verringerte Hemmwirkung aufweisen (10-30 % der Kontrolle). Es hemmt die Zellproliferation um mehr als 50 % im Vergleich zu den unbehandelten Kontrollzellen nach 36 Tagen, wobei die Zellzahl immer noch um das Vierfache im Vergleich zur anfänglichen Zelldichte ansteigt. Es führt auch zu verlängerten Effekten auf die Proliferation menschlicher Tenon-Kapsel-Fibroblasten in vitro. Aufgrund seiner kurzen Halbwertszeit, der steilen Dosis-Wirkungs-Kurve, der hohen Gesamtkörperclearance und der hohen hepatischen Extraktion ist es ein ideales Medikament für die hepatische arterielle Infusion (HAI).
Literatur
  • [4] https://pubmed.ncbi.nlm.nih.gov/1386726/
  • [5] https://pubmed.ncbi.nlm.nih.gov/19383854/

Klinische Studieninformationen

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer Rekrutierung Erkrankungen Sponsor/Kooperationspartner Startdatum Phasen
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

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