| 中文名称: | [4-[(羟基氨基)羰基]苯基]氨基甲酸 [6-[(二乙基氨基)甲基]-2-萘基]甲酯 | ||||
|---|---|---|---|---|---|
| 英文名称: | [4-[(Hydroxyamino)carbonyl]phenyl]carbamic acid [6-[(diethylamino)methyl]-2-naphthalenyl]methyl ester | ||||
| 别名: | [4-[(羟基氨基)羰基]苯基]氨基甲酸 [6-[(二乙基氨基)甲基]-2-萘基]甲酯 [4-[(Hydroxyamino)carbonyl]phenyl]carbamicacid[6-[(diethylamino)methyl]-2-naphthalenyl]methylester;Givinostat;Givinostat(ITF-2357);Carbamicacid,N-[4-[(hydroxyamino)carbonyl]phenyl]-,[6-[(diethylamino)methyl]-2-naphthalenyl]methylester;Gavinostat;[6-(diethylaminomethyl)naphthalen-2-yl]methylN-[4-(hydroxycarbamoyl)phenyl]carbamate;CS-2025;Givinostat(freebase) | ||||
| CAS No: | 497833-27-9 | 分子式: | C24H27N3O4 | 分子量: | 421.49 |
| CAS No: | 497833-27-9 | ||||
| 分子式: | C24H27N3O4 | ||||
| 分子量: | 421.49 | ||||
密度：
1.259g/ml
包装规格：
2mg 5mg in glass bottle
产品简介：
Givinostat (ITF-2357) 是 HDAC 抑制剂。抑制 HDAC1 和 HDAC3，IC50 分别为 198 nM 和 157 nM。
溶解性：
可溶于 dmso
储备液保存：
-80°C, 6 months
-20°C, 1 month
-20°C, 1 month
靶点：
hHDAC3:157nM (IC50);hHDAC1:198nM (IC50);hHDAC11:292nM (IC50);hHDAC6:315nM (IC50);hHDAC2:325nM (IC50);hHDAC10:340nM(IC50)
hHDAC7:524nM (IC50);hHDAC5: 532nM (IC50);hHDAC9: 541nM(IC50);hHDAC8:854nM (IC50);hHDAC4:1059nM (IC50);HD1-B:7.5nM (IC50)
HD1-A:16nM (IC50);HD2: 10nM(IC50)
hHDAC7:524nM (IC50);hHDAC5: 532nM (IC50);hHDAC9: 541nM(IC50);hHDAC8:854nM (IC50);hHDAC4:1059nM (IC50);HD1-B:7.5nM (IC50)
HD1-A:16nM (IC50);HD2: 10nM(IC50)
体外研究：
Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF-2357) 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. As shown by the CCK-8 assay, Givinostat (ITF-2357) inhibits JS-1 cell proliferation in a concentration-dependent manner. Treatment with Givinostat ≥500 nM is associated with significant inhibition of JS-1 cell proliferation (P<0.01). Also, the cell inhibition rate significantly differs between the group cotreated with Givinostat ≥250 nM plus LPS and the group without LPS treatment (same Givinostat concentration) (P<0.05).
体内研究：
Givinostat (ITF2357) at 10 mg/kg is used as a positive control and, as expected, reduced serum TNFα by 60%. Strikingly, pretreatment of ITF3056 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. Similarly, when pretreated with lower doses of Givinostat (ITF-2357) (1 or 5 mg/kg), there is a 22% reduction for 1 mg/kg and 40% for 5 mg/kg.
保存条件：
2-8°C
注意事项：
1、为了您的安全和健康，请穿实验服并戴一次性手套操作。
2、以上信息仅做参考交流之用。
2、以上信息仅做参考交流之用。
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)
参考文献 & 客户发表文献
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稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
