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Givinostat (ITF2357)

  Cat. No.:  DC7432   Featured
Chemical Structure
732302-99-7
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Field of application
Givinostat (ITF2357) is a potent HDAC inhibitor for maize HD2, HD1B and HD1A with IC50 of 10 nM, 7.5 nM and 16 nM. Phase 1/2.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 732302-99-7
Chemical Name: (6-((diethylamino)methyl)naphthalen-2-yl)methyl (4-(hydroxycarbamoyl)phenyl)carbamate hydrochloride hydrate
Synonyms: ITF2357, ITF-2357, ITF 2357, ITF2357 HCl, ITF2357 hydrochloride, Givinostat HCl, gavinostat, Givinostat HCl hydrate
SMILES: CCN(CC1=CC2=C(C=C1)C=C(C=C2)COC(NC3=CC=C(C=C3)C(NO)=O)=O)CC.O.Cl
Formula: C24H30ClN3O5
M.Wt: 475.97
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Givinostat hydrochloride monohydrate is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively.
In Vivo: Givinostat (ITF2357) at 10 mg/kg is used as a positive control and, as expected, reduced serum TNFα by 60%. Strikingly, pretreatment of ITF3056 starting at 0.1 mg/kg significantly reduces the circulating TNFα by nearly 90%. To achieve a significant increase in serum IL-1β production, a higher dose of LPS is injected (10 mg/kg), and blood is collected after 4 h. Similarly, when pretreated with lower doses of ITF3056 (1 or 5 mg/kg), there is a 22% reduction for 1 mg/kg and 40% for 5 mg/kg[1].
In Vitro: Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 100 and 200 nM, there is no reduction[1]. As shown by the CCK-8 assay, Givinostat inhibits JS-1 cell proliferation in a concentration-dependent manner. Treatment with Givinostat ≥500 nM is associated with significant inhibition of JS-1 cell proliferation (P<0.01). Also, the cell inhibition rate significantly differs between the group cotreated with Givinostat ≥250 nM plus LPS and the group without LPS treatment (same Givinostat concentration) (P<0.05)[2].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
Cat. No. Product name Field of application
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