体外活性
Givinostat hydrochloride inhibits JS-1 cell proliferation in a concentration-dependent manner. Givinostat hydrochloride (≥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 hydrochloride ≥250 nM plus LPS and the group without LPS treatment[3]. Givinostat hydrochloride (25, 50, and 100 nM) reduces IL-1β secretion more than 70%. Givinostat hydrochloride 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, but at 100 and 200 nM, there is no reduction[4].
体内活性
Givinostat hydrochloride (10 mg/kg) reduces serum TNFα by 60%. Pretreatment of Givinostat hydrochloride (0.1 mg/kg) significantly reduces the circulating TNFα by nearly 90%[4].
Cas No.
199657-29-9
分子式
C24H28ClN3O4
分子量
457.95
别名
ITF2357 hydrochloride;ITF2357 HCl;ITF 2357;ITF2357;ITF-2357;Givinostat HCl
储存和溶解度
DMSO:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years