ITF2357

Bezeichnung:ITF2357

CAS-Nr732302-99-7

Englisch Name:ITF2357

CBNumberCB12561481

SummenformelC24H30ClN3O5

Molgewicht475.9651

MOL-Datei732302-99-7.mol

ITF2357 physikalisch-chemischer Eigenschaften

storage temp.	-20°C
Löslichkeit	≥23.8 mg/mL in DMSO; insoluble in EtOH; ≥2.9 mg/mL in H2O with gentle warming and ultrasonic
Aggregatzustand	powder
Farbe	white to beige
CAS Datenbank	732302-99-7

Gefahreninformationscode (GHS)

ITF2357 Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
Givinostat Hydrochloride Hydrate is a potent inhibitor of HDAC with IC50?of 7.5-16 nM. It is used in the treatment of muscular dystrophy.
Verwenden
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.
Biologische Aktivität
itf2357, also known as givinostat, is a potent inhibitor of both class i and class ii histone deacetylase (hdac) as well as a potent inhibitor of hematopoietic colony formation by jakev617f-bearing progenitor cells from chronic myeloproliferative neoplasms in vitro. previous studies has shown that itf2357 induces apoptosis of multiple myeloma (mm) and acute myelogenous leukemia (aml) cells following induction of p21 and down-modulation of bcl-2 and mcl-1 proteins and inhibits the production of pro-inflammatory cytokines (such as il-1, il-6, tumor necrosis factor (tnf)-α and interferon (ifn)-γ) by peripheral blood mononuclear cells as well as the production of il-6 and vascular endothelium growth factor (vegf) by mesenchymal stromal cells.katia todoerti, valentina barbui, olga pedrini, marta linett, gianluca fossati, paolo mascagni, alessandro rambaldi, antonino neri, martino introna, luigia lombardi, and josee golay. pleiotropi anti-myeloma activity of itf2357: inhibition of interleukin-6 receptor signaling and repression of mir-19a and mir-19b. haematologica 2010; 95(2): 260-269
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).
target
HDAC

ITF2357 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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