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Givinostat HCl monohydrate

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Chemical Structure| 732302-99-7 同义名 : ITF2357;Givinostat;ITF-2357 hydrochloride monohydrate;Givinostat hydrochloride monohydrate
CAS号 : 732302-99-7
货号 : A113603
分子式 : C24H30ClN3O5
纯度 : 99%+
分子量 : 475.965
MDL号 : MFCD28502062
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(220.6 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 2.5 mg/mL(5.25 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：

PO 0.5% CMC-Na 12 mg/mL suspension

生物活性
靶点

  • HD1

    HD1-A, IC50:16 nM

    HD1-B, IC50:7.5 nM

  • HD2

    HD2, IC50:10 nM
描述 Givinostat (ITF2357) significantly suppresses total LPS-induced IL-1β production compared to ITF3056. At concentrations of 25, 50, and 100 nM, Givinostat reduces IL-1β secretion by more than 70%. It also suppresses IL-6 production in PBMCs stimulated with TLR agonists and IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, with no further reduction at higher concentrations [1]. According to the CCK-8 assay results, Givinostat (ITF2357) demonstrates a concentration-dependent inhibition of JS-1 cell proliferation. Treatment with Givinostat (ITF2357) at concentrations ≥500 nM significantly inhibits JS-1 cell proliferation (P<0.01). Moreover, the rate of cell inhibition differs significantly between the group co-treated with Givinostat at concentrations ≥250 nM plus LPS and the group treated with the same concentration of Givinostat without LPS (P<0.05) [2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.10mL

0.42mL

0.21mL

10.50mL

2.10mL

1.05mL

21.01mL

4.20mL

2.10mL
参考文献

[1]Hoffmann G, et al. A novel sirtuin 2 (SIRT2) inhibitor with p53-dependent pro-apoptotic activity in non-small cell lung cancer. J Biol Chem. 2014 Feb 21;289(8):5208-16.

[2]Wang YG, et al. Givinostat inhibition of hepatic stellate cell proliferation and protein acetylation. World J Gastroenterol. 2015 Jul 21;21(27):8326-39.