199657-29-9
| 中文名称 | 199657-29-9 |
|---|---|
| 中文同义词 | 化合物 T6279L;化合物GIVINOSTAT HYDROCHLORIDE |
| 英文名称 | Givinostat (hydrochloride) |
| 英文同义词 | 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号 | 199657-29-9 |
| 分子式 | C24H28ClN3O4 |
| 分子量 | 457.96 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 199657-29-9.mol |
| 结构式 |  |
199657-29-9 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | DMSO：45.8（最大浓度 mg/mL）；100.01（最大浓度 mM） |
|
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 50 ) |
hHDAC7 524 nM (IC 50 ) |
hHDAC5 532 nM (IC 50 ) |
hHDAC9 541 nM (IC 50 ) |
hHDAC8 854 nM (IC 50 ) |
hHDAC4 1059 nM (IC 50 ) |
HD1-B 7.5 nM (IC 50 ) |
HD1-A 16 nM (IC 50 ) |
HD2 10 nM (IC 50 ) |
Givinostat (ITF2357) 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. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 100 and 200 nM, there is no reduction. Givinostat (ITF-2357) inhibits JS-1 cell proliferation in a concentration-dependent manner in the CCK-8 assay. Treatment with Givinostat (ITF-2357) ≥500 nM is associated with significant inhibition of JS-1 cell proliferation. Also, the cell inhibition rate significantly differs between the group cotreated with Givinostat (ITF-2357) ≥250 nM plus LPS and the group without LPS treatment.
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.