ChemicalBook--->CAS DataBase List--->199657-29-9

199657-29-9

199657-29-9 Structure

199657-29-9 Structure
IdentificationBack Directory
[Name]

Givinostat (hydrochloride)
[CAS]

199657-29-9
[Synonyms]

Givinostat Hcl
ITF-2357 hydrochloride
Givinostat (ITF2357) HCl
Gavinostat hydrochloride
Givinostat (hydrochloride)
Givinostat (ITF2357) hydrochloride
GAVINOSTAT HYDROCHLORIDE;ITF-2357 HYDROCHLORIDE
[6-[(Diethylamino)methyl]-2-naphthalenyl]methyl-N-[4-[(hydroxyamino)carbonyl]phenyl]carbamate hydrochloride
[Molecular Formula]

C24H28ClN3O4
[MOL File]

199657-29-9.mol
[Molecular Weight]

457.95
Chemical PropertiesBack Directory
[storage temp. ]

Store at -20°C
[solubility ]

DMSO:45.8(Max Conc. mg/mL);100.01(Max Conc. mM)
Hazard InformationBack Directory
[Biological Activity]

Givinostat (ITF-2357) hydrochloride is an HDAC inhibitor, inhibits HDAC1 and HDAC3 with IC50 of 198 nM and 157 nM, respectively.
[in vitro]

Givinostat (hydrochloride) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduces 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.
[in vivo]

Givinostat (ITF2357) at 10 mg/kg is used as a positive control and reduces serum TNFα by 60%. Pretreatment of Givinostat (ITF-2357) 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.

[target]

hHDAC3

157 nM (IC 50 )

hHDAC1

198 nM (IC 50 )

hHDAC11

292 nM (IC 50 )

hHDAC6

315 nM ( IC 50 )

hHDAC2

325 nM (IC 50 )

hHDAC10

340 nM (IC < sub> 50 )

hHDAC7

524 nM (IC 50 )

hHDAC5

532 nM (IC 50 )

hHDAC9

541 nM (IC 50 )

hHDAC8

854 nM (IC 50 < /sub> )

hHDAC4

1059 nM (IC 50 )

HD1-B

7.5 nM (IC 50 )

HD1-A

16 nM (IC 50 )

HD2

10 nM (IC 50 )

[storage]

Store at -20°C
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