Givinostat (hydrochloride)
Givinostat (hydrochloride) Basic information
- Product Name:
- Givinostat (hydrochloride)
- Synonyms:
-
- Givinostat Hcl
- [6-[(Diethylamino)methyl]-2-naphthalenyl]methyl-N-[4-[(hydroxyamino)carbonyl]phenyl]carbamate hydrochloride
- Givinostat (hydrochloride)
- Givinostat (ITF2357) HCl
- Gavinostat hydrochloride
- GAVINOSTAT HYDROCHLORIDE;ITF-2357 HYDROCHLORIDE
- ITF-2357 hydrochloride
- Givinostat (ITF2357) hydrochloride
- CAS:
- 199657-29-9
- MF:
- C24H28ClN3O4
- MW:
- 457.96
- Mol File:
- 199657-29-9.mol
Givinostat (hydrochloride) Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- DMSO:45.8(Max Conc. mg/mL);100.01(Max Conc. mM)
- form
- Solid
- color
- White to off-white
Givinostat (hydrochloride) Usage And Synthesis
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
Givinostat (hydrochloride)Supplier
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- 021-58955995
- sales@medchemexpress.cn
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