Givinostat hydrochloride monohydrate - CAS:732302-99-7

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Givinostat hydrochloride monohydrate (Synonyms:ITF-2357 hydrochloride monohydrate)

目录号 : KM9410 CAS No. : 732302-99-7 纯度 : ≥98%

Data Sheet 产品使用指南

Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride monohydrate) 是 HDAC 抑制剂，抑制 HDAC1 和 HDAC3，IC₅₀ 分别为 198 nM 和 157 nM。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg	询价	In-stock
200mg	询价	In-stock

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生物活性

Givinostat hydrochloride monohydrate (ITF-2357 hydrochloride monohydrate) is a HDAC inhibitor with an IC₅₀ of 198 and 157 nM for HDAC1 and HDAC3, respectively.

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 50 nM Givinostat (ITF2357), but at 100 and 200 nM, there is no reduction. As shown by the CCK-8 assay, Givinostat (ITF2357) inhibits JS-1 cell proliferation in a concentration-dependent manner. Treatment with Givinostat (ITF2357) ≥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 (ITF2357) (1 or 5 mg/kg), there is a 22% reduction for 1 mg/kg and 40% for 5 mg/kg.

分子式

C₂₄H₂₈N₃O₄+^.Cl-^.H₂O

分子量

475.97

CAS号

732302-99-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (210.10 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1010 mL	10.5049 mL	21.0097 mL
5 mM	0.4202 mL	2.1010 mL	4.2019 mL
10 mM	0.2101 mL	1.0505 mL	2.1010 mL

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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.17 mg/mL (4.56 mM); Clear solution

此方案可获得 ≥ 2.17 mg/mL (4.56 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.17 mg/mL (4.56 mM); Clear solution

此方案可获得 ≥ 2.17 mg/mL (4.56 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.17 mg/mL (4.56 mM); Clear solution

此方案可获得 ≥ 2.17 mg/mL (4.56 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 21.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

临床试验

科研文献

纯度： ≥98%

Data Sheet

产品使用指南

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