solo para uso en investigación

Fludarabine STAT1 inhibitor

Name: Fludarabine
Brand: Selleck Chemicals
SKU: S1491
Rating: 5 (207 reviews)

Cat. No.: S1491

Fludarabine is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis.

Fludarabine STAT inhibitor Chemical Structure

Estructura química

Peso molecular: 285.23

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.96%

99.96

Dianas relacionadas	EGFR JAK Pim
Otros STAT Inhibidores	Napabucasin (BBI608) Stattic NSC 74859 (S3I-201) Cryptotanshinone (Tanshinone C) C188-9 (TTI-101) SH-4-54 BP-1-102 AS1517499 HO-3867 Nifuroxazide

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Formulación	Descripción de la actividad	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
Haga clic para ver más datos experimentales de líneas celulares

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	285.23	Fórmula	C₁₀H₁₂FN₅O₄	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	21679-14-1	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	FaraA, Fludarabinum, NSC 118218			Smiles	C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)CO)O)O)F)N

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 57 mg/mL (199.83 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Targets/IC₅₀/Ki	STAT1 (Vascular smooth muscle cells)
In vitro	Fludarabine inhibe eficazmente la proliferación de células RPMI 8226 con una IC50 de 1,54 μg/mL. La IC50 de este compuesto contra las células MM.1S y MM.1R es de 13,48 μg/mL y 33,79 μg/mL, respectivamente. Por el contrario, las células U266 son resistentes a este químico con una IC50 de 222,2 μg/mL. El tratamiento con este compuesto resulta en un aumento del número de células en la fase G1 del ciclo celular, acompañado de una reducción concomitante de células en la fase S del ciclo celular de manera dependiente del tiempo. Induce un bloqueo del ciclo celular y desencadena la apoptosis en las células de mieloma múltiple. Desencadena la escisión dependiente del tiempo de caspasa-8, -9, y -3, -7, seguida de la escisión de PARP. Aumenta la expresión de Bax de manera dependiente del tiempo, mientras que la expresión de Bak no cambia. Después de la exposición a este químico durante 12 horas, las células RPMI 8226 muestran una pérdida de potencial de membrana con el 61,05% de las células expresando baja fluorescencia de rodamina 123 en comparación con el 8,62% de las células en el control no tratado. Para mejorar la solubilidad, se formula como monofosfato (F-ara-AMP, fudarabina), que se desfosforila instantánea y cuantitativamente al nucleósido original tras la infusión intravenosa. Dentro de las células se produce una refosforilación que conduce al trifosfato de arabinósido de fluoroadenina (F-ara-ATP), el principal metabolito citotóxico de F-ara-A. También puede inducir la estimulación proinflamatoria de células monocíticas, según se evaluó por el aumento de la expresión de ICAM-1 y la liberación de IL-8. Este compuesto no afecta el crecimiento de las líneas celulares de cáncer de ovario, mientras que induce una inhibición marcada y dosis-dependiente de la proliferación en las líneas celulares de melanoma. Es un inhibidor de STAT1 que reduce específicamente STAT1 sin afectar a otros miembros de la familia STAT. Además de la acumulación citoplasmática, el cisplatino en dosis bajas repetidas (RLDC) induce la expresión de HMGB1, que está marcadamente suprimida por el silenciamiento de STAT1. Consistentemente, este químico suprime la expresión de HMGB1 durante el tratamiento con RLDC de manera dosis-dependiente en células tubulares renales tratadas con RLDC.
In vivo	Los tumores tratados con PBS crecen rápidamente hasta aproximadamente 10 veces su volumen inicial en 25 días, mientras que los tumores con Fludarabine a 40 mg/kg aumentan menos de 5 veces. Se demuestra un efecto antitumoral significativo de 40 mg/kg de este compuesto en el crecimiento tumoral de RPMI8226. Los tumores RPMI8226 tratados con 40 mg/kg de este químico en el día 10 aumentan los núcleos apoptóticos. Este compuesto es eficaz para suprimir los xenoinjertos de mieloma RPMI8226 en ratones SCID.
Referencias	[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/

Aplicaciones (Applications)

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

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
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

Preguntas frecuentes (Frequently Asked Questions)

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

Respuesta:
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):