SML1772

Givinostat hydrochloride hydrate

≥95% (HPLC)

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₂₄H₂₇N₃O₄ · HCl · H₂O
• CAS Number: 732302-99-7
• Molecular Weight: 475.97
• MDL number: MFCD18385007
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: powder
• storage condition: desiccated
• color: white to beige
• solubility: DMSO: 20 mg/mL, clear
• storage temp.: −20°C
• SMILES string: [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

Description

Application

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.

Biochem/physiol Actions

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.

Safety Information

• pictograms: GHS07
• signalword: Warning
• hcodes: H302
• pcodes: P264 - P270 - P301 + P312 - P501
• Hazard Classifications: Acute Tox. 4 Oral
• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable