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Floxuridine (FUDR) DNA/RNA Synthesis remmer

Name: Floxuridine (FUDR)
Brand: Selleck Chemicals
SKU: S1299
Rating: 5 (14 reviews)

Cat.nr.S1299

Floxuridine (FUDR), een prodrug die in vivo snel wordt gekataboliseerd tot 5-fluorouracil, wordt gebruikt voor de behandeling van verschillende kankers, met name metastasen naar de lever. Het remt Poly(ADP-Ribose) polymerase en induceert DNA-schade en apoptose. Dit middel heeft ook antivirale effecten tegen HSV en CMV.

Floxuridine (FUDR) DNA/RNA Synthesis remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 246.19

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Kwaliteitscontrole

Batch: Zuiverheid: 99.99%

99.99

Gerelateerde doelwitten	HDAC PARP ATM/ATR DNA-PK WRN Topoisomerase PPAR Sirtuin Casein Kinase eIF
Overig DNA/RNA Synthesis Inhibitoren	CX-5461 (Pidnarulex) B02 SCR7 Favipiravir (T-705) EED226 RK-33 BMH-21 Triapine (3-AP) Carmofur YK-4-279

Celkweek, behandeling & werkzame concentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving
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
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit

Molecuulgewicht	246.19	Formule	C₉H₁₁FN₂O₅	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	50-91-9	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	NSC 27640, Deoxyfluorouridine			Smiles	C1C(C(OC1N2C=C(C(=O)NC2=O)F)CO)O

Oplosbaarheid

In vitro
Batch:

DMSO : 49 mg/mL (199.03 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : 49 mg/mL

Ethanol : 10 mg/mL

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
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.
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.
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.
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.
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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	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.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

In vitro

Floxuridine (FUDR) vertoont een hogere affiniteit voor PEPT1 dan de overeenkomstige 5'-O-mono aminozuurester prodrugs. In combinatie met Leucovorin resulteert het in synergetische remmende effecten op de groei van menselijke T-lymfoblasten leukemiecellen. Deze verbinding remt significant de opname van zowel [(3)H]-inosine als [(3)H]-adenosine (60-70% van de controle), terwijl de aminozuurester prodrugs waaronder Val, Phe, Pro, Asp en Lys esters een duidelijk verminderde remmende potentie vertonen (10-30% van de controle). Het remt de celproliferatie met meer dan 50% ten opzichte van de onbehandelde controlecellen na 36 dagen, waarbij het aantal cellen nog steeds verviervoudigt in vergelijking met de initiële celdichtheid. Het resulteert ook in langdurige effecten op de proliferatie van menselijke Tenonkapsel fibroblasten in vitro. Vanwege de korte halfwaardetijd, steile dosis-respons curve, hoge totale lichaamsclearing en hoge hepatische extractie is het een ideaal medicijn voor hepatische arteriële infusie (HAI).

Referenties

[1] https://pubmed.ncbi.nlm.nih.gov/18652477/
[2] https://pubmed.ncbi.nlm.nih.gov/2950995/
[3] https://pubmed.ncbi.nlm.nih.gov/16462026/

[4] https://pubmed.ncbi.nlm.nih.gov/1386726/
[5] https://pubmed.ncbi.nlm.nih.gov/19383854/

Informatie over klinische proeven

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
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

Technische ondersteuning

Gebruiksaanwijzing

Tel: +1-832-582-8158 Ext:3

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