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Fludarabine inibitore di STAT1

N. Cat.S1491

Fludarabine è un inibitore dell'attivazione di STAT1 che causa una deplezione specifica della proteina STAT1 (e dell'mRNA) ma non di altre STAT. È anche un inibitore della sintesi del DNA nelle cellule muscolari lisce vascolari. Fludarabine induce l'apoptosi.

Fludarabine STAT inibitore Chemical Structure

Struttura chimica

Peso molecolare: 285.23

Vai a

Controllo Qualità

Lotto: Purezza: 99.96%

99.96

Target correlati	EGFR JAK Pim
Altro STAT Inibitori	Napabucasin (BBI608) Stattic NSC 74859 (S3I-201) Cryptotanshinone (Tanshinone C) C188-9 (TTI-101) SH-4-54 BP-1-102 AS1517499 Nifuroxazide HO-3867

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Formulazione	Descrizione dellattività	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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Informazioni chimiche, conservazione e stabilità

Peso molecolare	285.23	Formula	C₁₀H₁₂FN₅O₄	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	21679-14-1	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	FaraA, Fludarabinum, NSC 118218			Smiles	C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)CO)O)O)F)N

Solubilità

In vitro
Lotto:

DMSO : 57 mg/mL (199.83 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Targets/IC₅₀/Ki	STAT1 (Vascular smooth muscle cells)
In vitro	Fludarabine inibisce efficacemente la proliferazione delle cellule RPMI 8226 con un IC50 di 1,54 μg/mL. L'IC50 di questo composto contro le cellule MM.1S e MM.1R è rispettivamente di 13,48 μg/mL e 33,79 μg/mL. Al contrario, le cellule U266 sono resistenti a questo agente chimico con un IC50 di 222,2 μg/mL. Il trattamento con questo composto provoca un aumento del numero di cellule nella fase G1 del ciclo cellulare, accompagnato da una concomitante riduzione delle cellule nella fase S del ciclo cellulare in modo tempo-dipendente. Induce un blocco del ciclo cellulare e innesca l'apoptosi nelle cellule MM. Innesca la scissione tempo-dipendente di caspasi-8, -9, e -3, -7, seguita dalla scissione di PARP. Aumenta l'espressione di Bax in modo tempo-dipendente, mentre l'espressione di Bak non cambia. Dopo l'esposizione a questo agente chimico per 12 ore, le cellule RPMI 8226 mostrano una perdita del potenziale di membrana con il 61,05% delle cellule che esprimono una bassa fluorescenza di rodamina 123 rispetto all'8,62% delle cellule nel controllo non trattato. Per migliorare la solubilità, è formulato come monofosfato (F-ara-AMP, fudarabina), che viene istantaneamente e quantitativamente defosforilato nel nucleoside genitore dopo infusione endovenosa. All'interno delle cellule si verifica una rifosforilazione che porta al trifosfato di arabinoside di fluoroadenina (F-ara-ATP), il principale metabolita citotossico di F-ara-A. Può anche indurre una stimolazione pro-infiammatoria delle cellule monocitiche, come valutato dall'aumento dell'espressione di ICAM-1 e del rilascio di IL-8. Questo composto non influenza la crescita delle linee cellulari del cancro ovarico, mentre induce una marcata e dose-dipendente inibizione della proliferazione nelle linee cellulari del melanoma. È un inibitore di STAT1 che riduce specificamente STAT1 senza influenzare altri membri della famiglia STAT. Oltre all'accumulo citoplasmatico, il cisplatino a basse dosi ripetute (RLDC) induce l'espressione di HMGB1, che è marcatamente soppressa dal knockdown di STAT1. Coerentemente, questo composto sopprime l'espressione di HMGB1 durante il trattamento con RLDC in modo dose-dipendente nelle cellule tubulari renali trattate con RLDC.
In vivo	I tumori trattati con PBS crescono rapidamente fino a circa 10 volte il loro volume iniziale in 25 giorni, mentre i tumori con Fludarabine a 40 mg/kg aumentano meno di 5 volte. Viene dimostrato un significativo effetto antitumorale di 40 mg/kg di questo composto sulla crescita tumorale di RPMI8226. I tumori RPMI8226 trattati con 40 mg/kg di questo agente chimico al giorno 10 aumentano i nuclei apoptotici. Questo composto è efficace nel sopprimere gli xenotrapianti di mieloma RPMI8226 nei topi SCID.
Riferimenti	[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/

Applicazioni

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

Informazioni sullo studio clinico

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
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

Supporto tecnico

Istruzioni per la manipolazione

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

Per qualsiasi altra domanda, si prega di lasciare un messaggio.

Domande Frequenti

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

Risposta:
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):