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Fludarabine inhibiteur de STAT1

Réf. CatalogueS1491

Fludarabine est un inhibiteur de l'activation de STAT1 qui provoque une déplétion spécifique de la protéine STAT1 (et de l'ARNm), mais pas des autres STATs. C'est également un inhibiteur de la synthèse de l'ADN dans les cellules musculaires lisses vasculaires. Fludarabine induit l'apoptose.

Fludarabine STAT inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 285.23

Aller à

Contrôle Qualité

Lot : Pureté : 99.96%

99.96

Cibles apparentées	EGFR JAK Pim
Autre STAT Inhibiteurs	Napabucasin (BBI608) Stattic NSC 74859 (S3I-201) Cryptotanshinone (Tanshinone C) C188-9 (TTI-101) SH-4-54 BP-1-102 AS1517499 Nifuroxazide HO-3867

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Formulation	Description de lactivité	PMID
Jeko-1	Function Assay	20 μM	24 h		inhibits expression of IDO	25940712
MV-4-11	Apoptosis Assay	2.5 μM	48 h		induces apoptosis slightly	25111583
THP-1	Apoptosis Assay	2.5 μM	48 h		induces apoptosis slightly	25111583
MOLM 13	Apoptosis Assay	2.5 μM	48 h		induces apoptosis slightly	25111583
KBM3/Bu2506	Apoptosis Assay	2.5 μM	48 h		induces apoptosis slightly	25111583
Nalm-6	Growth Inhibition Assay				IC50=18 μM	25061101
Reh	Growth Inhibition Assay				IC50=30 μM	25061101
U2937	Growth Inhibition Assay				IC50=16 μM	25061101
Mec-1	Growth Inhibition Assay				IC50＞500 μM	25061101
RPMI-8226	Growth Inhibition Assay				IC50=500 μM	25061101
Molt-4	Growth Inhibition Assay				IC50=180 μM	25061101
Nalm-6-FluR	Growth Inhibition Assay				IC50=250 μM	25061101
Raji	Function Assay	3 μM	24/48/72 h		induces accumulations of p53, p63 and p73	24940695
PBMC	Function Assay	50/100 μM	24 h	DMSO	inhibits STAT1 phosphorylation	24911872
MDA-231	Function Assay	100 μM	24 h	DMSO	decreases IDO expression	24911872
624.38mel	Function Assay	50 μM	24 h	DMSO	decreases IDO expression	24911872
MDA-231	Function Assay	50-200 μM	24 h	DMSO	inhibits IDO activity independently of mRNA levels	24911872
624.38mel	Function Assay	50-200 μM	24 h	DMSO	inhibits IDO activity independently of mRNA levels	24911872
HMECs	Function Assay	100 μM	36 h		inhibits IFNγ and LPS induced STAT1 phosphorylation and IRF1 expression	24211327
HMECs	Function Assay	100 μM	36 h		inhibits IFNα mediated phosphorylation of STAT1 and STAT3, but not of STAT2	24211327
BJAB	Apoptosis Assay	5 μM	24 h		induces cell apoptosis	24057147
I-83	Apoptosis Assay	5 μM	24 h		induces cell apoptosis	24057147
NALM6	Apoptosis Assay	5 μM	24 h		induces cell apoptosis	24057147
DU-145	Growth Inhibition Assay	0-10 μg/ml	48 h		inhibits cell growth in a dose-dependent manner	23734815
Nalm-6	Function Assay	10 μM	1/2/4 h		induces autophagy	23681223
Reh	Function Assay	10 μM	1/2/4 h		induces autophagy	23681223
Nalm-6	Growth Inhibition Assay				IC50 ∼10 μM	23681223
Reh	Growth Inhibition Assay				IC50 ∼10 μM	23681223
HEC1A	Growth Inhibition Assay	100-500 μM	24 h		inhibits cell growth in a dose-dependent manner	23595697
AN3CA	Growth Inhibition Assay	100-500 μM	24 h		inhibits cell growth in a dose-dependent manner	23595697
HEC50B	Growth Inhibition Assay	100-500 μM	24 h		inhibits cell growth slightly	23595697
HEC1A	Apoptosis Assay	20/100 μM	24 h		induces apoptosis in a dose-dependent manner	23595697
AN3CA	Apoptosis Assay	20/100 μM	24 h		induces apoptosis in a dose-dependent manner	23595697
HEC50B	Apoptosis Assay	20/100 μM	24 h		induces apoptosis slightly	23595697
EHEB	Apoptosis Assay	40 μM	24 h		induces apoptosis	23497075
A549	Growth Inhibition Assay				IC50=15.7±2.8 µM	23377192
A549 GAPDH-deficient	Growth Inhibition Assay				IC50=18.5±2.3 µM	23377192
CLL	Apoptosis Assay	10 μM	24-96 h		induces apoptotic cell death	22207686
MEC1	Apoptosis Assay	100 μM	72 h		induces apoptosis significantly	22132973
U937	Apoptosis Assay	0.8 μM	4-48 h		induces apoptosis slightly	22074700
U937	Apoptosis Assay	1 μM	96 h		induces apoptosis slightly	22023523
Daudi	Apoptosis Assay	20 μM	96 h		induces apoptosis slightly	22023523
J45.01	Apoptosis Assay	1 μM	96 h		induces apoptosis slightly	22023523
RPMI 8226	Growth Inhibition Assay				IC50=25.9 ± 3.7 μM	21948264
CEM	Growth Inhibition Assay				IC50=2.4 ± 0.4 μM	21948264
Raji	Growth Inhibition Assay				IC50=0.47 ± 0.04 μM	21948264
U937	Growth Inhibition Assay				IC50=0.24 ± 0.04 μM	21948264
K562	Growth Inhibition Assay				IC50=0.44 ± 0.05 μM	21948264
NALM-6	Apoptosis Assay	10 μM	24 h		induces cell apoptosis slightly	21699383
JMV-3	Apoptosis Assay	10 μM	24 h		induces cell apoptosis slightly	21699383
EHEB	Function Assay	5-50 μM	24 h		decreases p21 expression significantly	21168391
JVM-2	Function Assay	30 μM	24 h		decreases p21 expression	21168391
KBM3/Bu2506	Growth Inhibition Assay				IC20=0.67 µM	20933509
KBM3/Bu2506	Growth Inhibition Assay	0.6 μM	24 h		increases the cell fraction in S-phase	20933509
MDA-MB-231	Growth Inhibition Assay				IC50=4.0 μM	20447390
MCF-7	Growth Inhibition Assay				IC50=15.0 μM	20447390
HLE-B3	Function Assay	25 μM	48 h		blocks IFN-γ–induced STAT1 phosphorylation and IDO expression	20435158
K562	Growth Inhibition Assay		72 h		IC50=3.3 nM	20307198
BW-225	Growth Inhibition Assay				IC20=1.37 ×10−8 μM	18661380
OH-65	Growth Inhibition Assay				IC20=1.37 ×10−8 μM	18661380
GR-145	Growth Inhibition Assay				IC20=2.74 × 10−8 μM	18661380
A549	Growth Inhibition Assay				IC20=5.48 × 10−8 μM	18661380
CaSki	Growth Inhibition Assay				IC20=1.37 × 10−7 μM	18661380
ZMK-1	Growth Inhibition Assay				IC20=1.37 × 10−6 μM	18661380
SKW6.4	Apoptosis Assay	0.01-10 μM	24/48 h		induces cell death in both time- and dose- dependent manner	18092340
RPMI 8226	Growth Inhibition Assay		24 h		IC50=1.54 μM	17976186
MM.1S	Growth Inhibition Assay		48 h		IC50=13.48 μM	17976186
MM.1R	Growth Inhibition Assay		48 h		IC50=33.79 μM	17976186
U937	Growth Inhibition Assay				IC50=3,200 ± 560 nM	15930361
CLL5	Antitumor assay		48 hrs		Antitumor activity against CLL5 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis, EC50 = 0.16 μM.	24673739
K562	Cytotoxicity assay		72 hrs		Cytotoxicity against human paclitaxel-resistant K562 cells after 72 hrs by MTT assay, IC50 = 0.26 μM.	20605656
CLL3	Antitumor assay		48 hrs		Antitumor activity against CLL3 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis, EC50 = 0.35 μM.	24673739
CLL4	Antitumor assay		48 hrs		Antitumor activity against CLL4 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis, EC50 = 0.64 μM.	24673739
CEM-DNR-B	Cytotoxicity assay		72 hrs		Cytotoxicity against human CEM-DNR-B cells after 72 hrs by MTT assay, IC50 = 1.01 μM.	20605656
primary CLL	Cytotoxicity assay				Cytotoxicity against human primary CLL cells, LD50 = 1.1 μM.	25148392
CLL6	Antitumor assay		48 hrs		Antitumor activity against CLL6 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis, EC50 = 1.6 μM.	24673739
CLL2	Antitumor assay		48 hrs		Antitumor activity against CLL2 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis, EC50 = 2.66 μM.	24673739
HCT116	Cytotoxicity assay		72 hrs		Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay, IC50 = 6.6 μM.	25462277
PBMC	Cytotoxicity assay		48 hrs		Cytotoxicity against patient PBMC after 48 hrs by CellTitre-Blue assay in presenc of mouse M210B4 cells, IC50 = 10 μM.	25562417
CHO	Function assay				Binding affinity determined by displacement of specific binding of [125I]N-(4-amino-3-iodophenethyl)-adenosine in membranes of CHO cells stably transfected with the rat adenosine A3 receptor, Ki = 10.4 μM.	7707320
JVM2	Antitumor assay				Antitumor activity against human JVM2 cells assessed as cell viability after 48 hrs by FACS analysis, EC50 = 10.4 μM.	24673739
HeLa	Antitumor assay				Antitumor activity against human HeLa cells assessed as cell viability by MTT assay, EC50 = 16 μM.	24673739
CLL1	Antitumor assay		48 hrs		Antitumor activity against CLL1 cells isolated from CLL patient assessed as cell viability after 48 hrs by FACS analysis, EC50 = 17.1 μM.	24673739
CEM	Cytotoxicity assay		72 hrs		Cytotoxicity against human CEM cells after 72 hrs by MTT assay, IC50 = 19.49 μM.	20605656
T47D	Cytotoxicity assay		72 hrs		Cytotoxicity against human T47D cells after 72 hrs by SRB assay, IC50 = 46.2 μM.	25462277
A549	Cytotoxicity assay		72 hrs		Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 47.44 μM.	20605656
CCRF-CEM	Function assay	10 uM	1 to 60 mins		Drug transport in human CCRF-CEM cells assessed as ENT1-mediated uptake at 10 uM after 1 to 60 mins by liquid scintillation counting analysis	23388705
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
MG 63 (6-TG R)	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
BT-12	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
BT-12	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
NB-EBc1	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
SK-N-SH	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
Rh41	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
BT-37	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
MG 63 (6-TG R)	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
Rh30	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
OHS-50	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Daoy	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells	29435139
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D caspase screen for TC32 cells	29435139
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) cells	29435139
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Saos-2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells	29435139
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Informations chimiques, stockage et stabilité

Poids moléculaire	285.23	Formule	C₁₀H₁₂FN₅O₄	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	21679-14-1	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	FaraA, Fludarabinum, NSC 118218			Smiles	C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)CO)O)O)F)N

Solubilité

In vitro
Lot:

DMSO : 57 mg/mL (199.83 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
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 Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	4.000mg/ml (14.02mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 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.
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 Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	8.000mg/ml (28.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 160 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.
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.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Targets/IC₅₀/Ki	STAT1 (Vascular smooth muscle cells)
In vitro	Fludarabine inhibe efficacement la prolifération des cellules RPMI 8226 avec une IC50 de 1,54 μg/mL. L'IC50 de ce composé contre les cellules MM.1S et MM.1R est respectivement de 13,48 μg/mL et 33,79 μg/mL. En revanche, les cellules U266 sont résistantes à ce produit chimique avec une IC50 de 222,2 μg/mL. Le traitement par ce composé entraîne une augmentation du nombre de cellules en phase G1 du cycle cellulaire, accompagnée d'une réduction concomitante des cellules en phase S du cycle cellulaire de manière temps-dépendante. Il induit un blocage du cycle cellulaire et déclenche l'apoptose dans les cellules MM. Il déclenche le clivage temps-dépendant de la caspase-8, -9, et -3, -7, suivi du clivage de la PARP. Il augmente l'expression de Bax de manière temps-dépendante, tandis que l'expression de Bak ne change pas. Après une exposition à ce produit chimique pendant 12 heures, les cellules RPMI 8226 montrent une perte de potentiel membranaire avec 61,05% des cellules exprimant une faible fluorescence de la rhodamine 123 par rapport à 8,62% des cellules dans le contrôle non traité. Pour améliorer la solubilité, il est formulé sous forme de monophosphate (F-ara-AMP, fudarabine), qui est instantanément et quantitativement déphosphorylé en nucléoside parent après perfusion intraveineuse. À l'intérieur des cellules, une rephosphorylation se produit, ce qui conduit au triphosphate d'arabinoside de fluoroadénine (F-ara-ATP), le métabolite cytotoxique majeur de F-ara-A. Il peut également induire une stimulation pro-inflammatoire des cellules monocytaires, comme évalué par une augmentation de l'expression de l'ICAM-1 et de la libération d'IL-8. Ce composé n'affecte pas la croissance des lignées cellulaires de cancer de l'ovaire, alors qu'il induit une inhibition marquée et dose-dépendante de la prolifération dans les lignées cellulaires de mélanome. C'est un inhibiteur de STAT1 qui réduit spécifiquement STAT1 sans affecter les autres membres de la famille STAT. En plus de l'accumulation cytoplasmique, le cisplatine à faible dose répétée (RLDC) induit l'expression de HMGB1, qui est fortement supprimée par le knockdown de STAT1. De manière cohérente, ce produit chimique supprime l'expression de HMGB1 pendant le traitement RLDC de manière dose-dépendante dans les cellules tubulaires rénales traitées par RLDC.
In vivo	Les tumeurs traitées avec du PBS se développent rapidement pour atteindre environ 10 fois leur volume initial en 25 jours, tandis que les tumeurs traitées avec Fludarabine à 40 mg/kg augmentent moins de 5 fois. Un effet antitumoral significatif de 40 mg/kg de ce composé sur la croissance tumorale de RPMI8226 est démontré. Les tumeurs RPMI8226 traitées avec 40 mg/kg de ce produit chimique au jour 10 augmentent les noyaux apoptotiques. Ce composé est efficace pour supprimer les xénogreffes de myélome RPMI8226 chez les souris SCID.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/17976186/ [2] https://pubmed.ncbi.nlm.nih.gov/10428391/ [3] https://pubmed.ncbi.nlm.nih.gov/16546701/ [4] https://pubmed.ncbi.nlm.nih.gov/8983288/ [5] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10240827/

Applications

Méthodes	Biomarqueurs	PMID
Western blot	procaspase-9 / procaspase-3 p-p53 / p53 STAT1	27223263
Immunofluorescence	α-SMA / Vimentin	28322315
Growth inhibition assay	Cell viability	24956101

Informations sur lessai clinique

(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	Phases
NCT05390814	Recruiting	Primary Central Nervous System Lymphoma	Assistance Publique - Hôpitaux de Paris	December 18 2023	Phase 1
NCT05201183	Withdrawn	Acute Myeloid Leukemia\|Chronic Myeloid Leukemia\|Acute Lymphocytic Leukemia\|Myelodysplastic Syndromes	Naoyuki G. Saito M.D. Ph.D.\|Indiana University	October 2023	Phase 1\|Phase 2
NCT05917405	Recruiting	Acute Myeloid Leukemia in Remission	Nantes University Hospital	September 14 2023	Phase 2

Support technique

Instructions de manipulation

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

Si vous avez dautres questions, veuillez laisser un message.

Foire aux questions

Question 1:
how to re-suspend and deliver it for in vivo experiments?

Réponse :
For S1491, we tested a vehicle: 30% Propylene glycol, 5% Tween 80, 65% D5W that you can resuspend this compound in at up to 30mg/ml. It is a suspension and can only be given via oral gavage.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):