Givinostat hydrochloride monohydrate - CAS:732302-99-7 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	Givinostat hydrochloride monohydrate
英文名称:	Givinostat hydrochloride monohydrate
别名:	N-[4-[(羟基氨基)羰基]苯基]氨基甲酸 [6-[(二乙基氨基)甲基]-2-萘基]甲酯盐酸盐水合物;Givinostat (ITF2357) 抑制剂;Givinostat (ITF2357) 国华试剂 ITF-2357 hydrochloride monohydrate
CAS No:	732302-99-7	分子式:	C₂₄H₂₇N₃O₄^.HCl^.H₂O	分子量:	475.97
CAS No:	732302-99-7
分子式:	C₂₄H₂₇N₃O₄^.HCl^.H₂O
分子量:	475.97

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

G10403 Givinostat hydrochloride monohydrate ≥95% (psaitong)

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包装规格：

5mg 10mg 25mg 50mg in glass bottle

溶解性：

溶于DMSO（≥100mg/mL）

产品描述：

基本信息

产品编号：G10403
产品名称：Givinostat hydrochloride monohydrate
CAS:	732302-99-7	储存条件	粉末	-20℃	四年

分子式：	C24H27N3O4.HCl.H2O		溶于液体	-80℃	六个月
分子量	475.97			-20℃	一个月
化学名：	[6-(diethylaminomethyl)naphthalen-2-yl]methyl N-[4-(hydroxycarbamoyl)phenyl]carbamate;hydrate;hydrochloride
Solubility (25°C)	体外	DMSO	≥100mg/mL (210.10mM)
		Ethanol
		Water
	体内	现配现用
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.1010mL	10.5049mL	21.0097mL
5mM	0.4202mL	2.1010mL	4.2019mL
10mM	0.2101mL	1.0505mL	2.1010mL

生物活性

产品描述

一种HDAC 抑制剂，抑制 HDAC1 和 HDAC3，IC50 分别为 198nM 和 157nM。

靶点/IC₅₀

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)

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 (ITF2357) 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 50nM Givinostat (ITF2357), but at 100 and 200nM, there is no reduction[1]. As shown by the CCK-8 assay, Givinostat (ITF2357) inhibits JS-1 cell proliferation in a concentration-dependent manner. Treatment with Givinostat (ITF2357) ≥500nM 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 ≥250nM 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 4h. Similarly, when pretreated with lower doses of Givinostat (ITF2357) (1 or 5 mg/kg), there is a 22% reduction for 1mg/kg and 40% for 5mg/kg.

推荐实验方法(仅供参考)

细胞实验：

Cell Assay

After the JS-1 cell line is cultured in DMEM with 10% fetal bovine serum for 24 h, 30 wells of JS-1 cells are divided into two groups. In the first group, the culture medium is replaced by complete medium with final Givinostat concentrations of 0nM,125nM, 250nM, 500nM, and 1000nM. In the second group, Givinostat of relevant concentrations is added concomitantly with 100nM of LPS solution. Three replicates are performed for each group. After inoculation at 37°C and 5% CO2 for 24 h,each well (100μL) is incubated with 10μL of CCK-8 solution. The plates are incubated at 37 °C for 1 h and the absorbance is measured at 450nm using a microplate reader.

动物实验:

Animal Administration

Mice

C57BL/6 mice are housed in the animal facility for at least 5 days before use. For the comparison study, Givinostat (ITF2357) at 10 mg/kg is administered orally, and Givinostat (ITF2357) is injected intraperitoneally. One hour after administration of the compounds, the animals are treated intraperitoneally with LPS from Salmonella typhimurium at a dose of 2.5 mg/kg. 90min after the LPS treatment, mice are sacrificed, and sera are collected and stored at -80°C until further analysis of cytokine productions.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入输出 )

* = *

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果