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ITF2357

Cat. No. M1730
ITF2357 Structure
Synonym:

Givinostat, Gavinostat

Size Price Availability Quantity
10mg USD 180 In stock
50mg USD 580 In stock
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Quality Control
Biological Activity

ITF2357 (Givinostat, Gavinostat) is a histone deacetylase inhibitor with potential anti-inflammatory, anti-angiogenic, and antineoplastic activities.The IC50 vale for maize HDAC preparations HD2, HD-1B and HD-1A are  10, 7.5 and 16 nM respectively. ITF2357 (Givinostat, Gavinostat) inhibits class I and class II histone deacetylases (HDACs) and several pro-inflammatory cytokines.This reduces expression of tumour necrosis factor (TNF), interleukin 1α and β, and interleukin 6. ITF2357 (Givinostat,Gavinostat) also has activity against cells expressing JAK (2V617F), a mutated form of the janus kinase 2 (JAK2) enzyme that is implicated in the pathophysiology of many myeloproliferative diseases, including polycythaemia vera.

Protocol
Cell Experiment
Cell lines Purified monocytes
Preparation method Caspase 3/7 Determinations
Monocytes were isolated from freshly obtained unfractionated PBMCs by anti-CD14–labeled magnetic beads (CD14 MicroBeads, Miltenyi Biotec, Bergisch Gladbach, Germany) and incubated at 50,000 cells/well in flat-bottom 96-well plates in the presence of increasing concentrations of ITF2357 for 1 h. Thereafter, LPS (10 ng/mL) was added for an additional 24-h incubation. The activity of caspase 3/7 was then determined by Apo-ONE Homogeneous Caspase-3/7 Assay (Promega), and the amount of fluorescence was detected by fluorimetric plate reader (Victor-2; Perkin Elmer).
Concentrations 0~ 1000 nM
Incubation time 24 h
Animal Experiment
Animal models ConA-induced hepatitis in BALB/C mice
Formulation One milligram of ITF2357 was added to 1 mL water and heated to 90° C until dissolved
Dosages 5 mg/kg
Administration gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 475.97
Formula C24H27N3O4.HCl.H2O
CAS Number 732302-99-7
Purity 98.20%
Solubility DMSO
Storage at -20°C
References

Pharmacokinetics, safety and inducible cytokine responses during a phase 1 trial of the oral histone deacetylase inhibitor ITF2357 (givinostat).
Furlan A et al. Mol Med. 2011 May-Jun;17(5-6):353-62. PMID: 21365126.

Inhibition of HDAC activity by ITF2357 ameliorates joint inflammation and prevents cartilage and bone destruction in experimental arthritis.
Joosten LA et al. Mol Med. 2011 May-Jun;17(5-6):391-6. PMID: 21327299.

Effects of the histone deacetylase inhibitor ITF2357 in autoinflammatory syndromes.
Bodar EJ et al. Mol Med. 2011 May-Jun;17(5-6):363-8. PMID: 21274502.

The oral histone deacetylase inhibitor ITF2357 reduces cytokines and protects islet β cells in vivo and in vitro.
Lewis EC et al. Mol Med. 2011 May-Jun;17(5-6):369-77. PMID: 21193899.

ITF2357 interferes with apoptosis and inflammatory pathways in the HL-60 model: a gene expression study.
Galimberti S et al. Anticancer Res. 2010 Nov;30(11):4525-35. PMID: 21115902.

The histone deacetylase inhibitor ITF2357 reduces production of pro-inflammatory cytokines in vitro and systemic inflammation in vivo.
Leoni F, et al. Mol Med. 2005 Jan-Dec;11(1-12):1-15. PMID: 16557334.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ITF2357, Givinostat, Gavinostat supplier, HDAC, inhibitors

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