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| | Givinostat (hydrochloride) Basic information |
| Product Name: | Givinostat (hydrochloride) | | Synonyms: | Givinostat (hydrochloride);Givinostat Hcl;[6-[(Diethylamino)methyl]-2-naphthalenyl]methyl-N-[4-[(hydroxyamino)carbonyl]phenyl]carbamate 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 | | EINECS: | | | Product Categories: | | | 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) |
| | 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) Preparation Products And Raw materials |
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