199657-29-9
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- CAS号:
- 199657-29-9
- 英文名:
- Givinostat (hydrochloride)
- 英文别名:
- ITF2357 HCl;Givinostat Hcl;ITF-2357 hydrochloride;Gavinostat hydrochloride;Givinostat (ITF2357) HCl;Givinostat (hydrochloride);Givinostat HCl. gavinostat;Givinostat (ITF2357) hydrochloride;GAVINOSTAT HYDROCHLORIDE;ITF-2357 HYDROCHLORIDE;inhibit,Givinostat hydrochloride,Histone deacetylases,Givinostat,Inhibitor,HDAC
- 中文名:
- 199657-29-9
- 中文别名:
- 化合物 T6279L;化合物GIVINOSTAT HYDROCHLORIDE
- CBNumber:
- CB03041408
- 分子式:
- C24H28ClN3O4
- 分子量:
- 457.96
- MOL File:
- 199657-29-9.mol
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199657-29-9化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMSO:45.8(Max Conc. mg/mL);100.01(Max Conc. mM)
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199657-29-9性质、用途与生产工艺
Givinostat (ITF-2357) hydrochloride 是 HDAC 抑制剂，抑制 HDAC1 和 HDAC3，IC50 分别为 198 nM 和 157 nM。
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hHDAC3
157 nM (IC
50
)
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hHDAC1
198 nM (IC
50
)
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hHDAC11
292 nM (IC
50
)
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hHDAC6
315 nM (IC
50
)
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hHDAC2
325 nM (IC
50
)
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hHDAC10
340 nM (IC
50
)
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hHDAC7
524 nM (IC
50
)
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hHDAC5
532 nM (IC
50
)
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hHDAC9
541 nM (IC
50
)
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hHDAC8
854 nM (IC
50
)
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hHDAC4
1059 nM (IC
50
)
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HD1-B
7.5 nM (IC
50
)
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HD1-A
16 nM (IC
50
)
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HD2
10 nM (IC
50
)
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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.
199657-29-9
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199657-29-9, 199657-29-9 相关搜索:
- 化合物GIVINOSTAT HYDROCHLORIDE
- 化合物 T6279L
- 199657-29-9
- inhibit,Givinostat hydrochloride,Histone deacetylases,Givinostat,Inhibitor,HDAC
- ITF2357 HCl
- Givinostat HCl. gavinostat
- Givinostat (ITF2357) hydrochloride
- ITF-2357 hydrochloride
- GAVINOSTAT HYDROCHLORIDE;ITF-2357 HYDROCHLORIDE
- Gavinostat hydrochloride
- Givinostat (ITF2357) HCl
- [6-[(Diethylamino)methyl]-2-naphthalenyl]methyl-N-[4-[(hydroxyamino)carbonyl]phenyl]carbamate hydrochloride
- Givinostat Hcl
- Givinostat (hydrochloride)