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Fludarabine STAT1 inhibitor

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.

Chemical Structure

Molecular Weight: 285.23

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Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	EGFR JAK Pim
Other STAT Inhibitors	Napabucasin (BBI608) Stattic NSC 74859 (S3I-201) Cryptotanshinone (Tanshinone C) SH-4-54 C188-9 (TTI-101) BP-1-102 HO-3867 Nifuroxazide AS1517499

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 57 mg/mL (199.83 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	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 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	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.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Average weight of animals: g

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% Tween 80

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	285.23	Formula	C₁₀H₁₂FN₅O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	21679-14-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	FaraA, Fludarabinum, NSC 118218			Smiles	C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)CO)O)O)F)N

Mechanism of Action

Targets/IC₅₀/Ki	STAT1 (Vascular smooth muscle cells)
In vitro	Fludarabine efficiently inhibits the proliferation of RPMI 8226 cells with IC50 of 1.54 μg/mL. The IC50 of this compound against MM.1S and MM.1R cells is 13.48 μg/mL and 33.79 μg/mL, respectively. In contrast, U266 cells are resistant to this chemical with IC50 of 222.2 μg/mL. This compound treatment results in increased number of cells in the G1 phase of cell cycle, accompanied with a concomitant reduction of cells at the S phase of cell cycle in a time-dependent manner. It induces a cell cycle block and triggers apoptosis in MM cells. It triggers time-dependent cleavage of caspase-8, -9, and -3, -7, followed by PARP cleavage. It increases expression of Bax in a time-dependent fashion, while the expression of Bak doesn't change. After exposure to this chemical for 12 hours, RPMI 8226 cells shows a loss of membrane potential with 61.05% of the cells expressing low fluorescence of rhodamine 123 compared with 8.62% of cells in untreated control. To enhance solubility, it is formulated as the monophosphate (F-ara-AMP, fudarabine), which is instantaneously and quantitatively dephosphorylated to the parent nucleoside upon intravenous infusion. Inside the cells rephosphorylation occurs which leads to fuoroadenine arabinoside triphosphate (F-ara-ATP), the major cytotoxic metabolite of F-ara-A. It can also induce pro-inflammatory stimulation of monocytic cells, as evaluated by increased expression of ICAM-1 and IL-8 release. This compound does not affect the growth of ovarian cancer cell lines, whereas it induces marked and dose-dependent inhibition of proliferation in melanoma cell lines. It is an inhibitor of STAT1 that specifically reduces STAT1 without affecting other STAT family members. In addition to cytoplasmic accumulation, repeated low-dose cisplatin (RLDC) induces HMGB1 expression, which is marked suppressed by STAT1 knockdown. Consistently, this chemical suppresses HMGB1 expression during RLDC treatment dose-dependently in RLDC-treat renal tubular cells.
In vivo	Tumors treated with PBS grow rapidly to approximately 10-fold their initial volume in 25 day, whereas, the tumors in the Fludarabine at 40 mg/kg increase less than 5-fold. A significant antitumor effect of 40 mg/kg of this compound on RPMI8226 tumor growth is demonstrated. RPMI8226 tumors treated with 40 mg/kg of this chemical at day 10 increase apoptotic nuclei. This compound is effective in suppressing RPMI8226 myeloma xenografts in SCID mice.
References	[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

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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	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

Tech Support

Handling Instructions

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

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Frequently Asked Questions

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

Answer:
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.

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