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.
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Source | Int J Cancer (2014). Figure 3. ITF2357 |
| Method | western blot | |
| Cell Lines | SU-DHL-4 and DOHH-2 cells | |
| Concentrations | 0.2 μM | |
| Incubation Time | 24 h | |
| Results | The cytostatic and cytotoxic effects of ITF2357 appeared instead to be more closely associated with c-Myc reduction |
| 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 |
| Molecular Weight | 475.97 |
| Formula | C24H27N3O4.HCl.H2O |
| CAS Number | 732302-99-7 |
| Solubility (25°C) | DMSO 75 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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