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Merck
CN

SML1772

Sigma-Aldrich

Givinostat hydrochloride hydrate

≥95% (HPLC)

别名:

Diethyl-[6-(4-hydroxycarbamoyl-phenyl carbamoyloxymethyl)-naphthalen-2-yl methyl]-ammonium chloride, ITF2357, N-[4-[(Hydroxyamino)carbonyl]phenyl]-carbamic acid, [6-[(diethylamino)methyl]-2-naphthalenyl]methyl ester hydrochloride

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About This Item

经验公式(希尔记法):
C24H27N3O4 · HCl · H2O
分子量:
475.97
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77

质量水平

检测方案

≥95% (HPLC)

形式

powder

储存条件

desiccated

颜色

white to beige

溶解性

DMSO: 20 mg/mL, clear

储存温度

−20°C

SMILES字符串

[H]Cl.[H]O[H].CCN(CC)CC1=CC=C(C=C(COC(NC2=CC=C(C(NO)=O)C=C2)=O)C=C3)C3=C1

InChI

1S/C24H27N3O4.ClH.H2O/c1-3-27(4-2)15-17-5-7-21-14-18(6-8-20(21)13-17)16-31-24(29)25-22-11-9-19(10-12-22)23(28)26-30;;/h5-14,30H,3-4,15-16H2,1-2H3,(H,25,29)(H,26,28);1H;1H2

InChI key

FKGKZBBDJSKCIS-UHFFFAOYSA-N

应用

Givinostat hydrochloride hydrate has been used as a histone deacetylase inhibitor to test its effect on the human immunodeficiency virus reactivation in CD4+ T-cell model.

生化/生理作用

Givinostat (ITF2357) is a hydroxamate HDAC inhibitor that inhibits class I and class II enzymes. Givinostat posseses a very promising activity profile in multiple myeloma and acute myelogenous leukemia in vitro and in vivo. Givinostat also has anti-inflammatory activity and inhibits the secretion of the tumor necrosis factor-alpha (TNF-α), IL-1, and IL-6. Givinostat has been in multiple Phase 2 studies for both inflammatory diseases (Duchenne Muscular Dystrophy , Juvenile arthritis, Polycythemia Vera) and blood cancers (myelomas and lymphomas).
Givinostat is known to mediate the reduction of the human immunodeficiency virus release in macrophages.

象形图

Exclamation mark

警示用语:

Warning

危险声明

危险分类

Acute Tox. 4 Oral

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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Francesca Curreli et al.
Viruses, 12(6) (2020-06-07)
Combination antiretroviral therapy (cART) is successful in maintaining undetectable levels of HIV in the blood; however, the persistence of latent HIV reservoirs has become the major barrier for a HIV cure. Substantial efforts are underway in finding the best latency-reversing

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