| Identification | Back Directory | [Name]
ITF2357 | [CAS]
732302-99-7 | [Synonyms]
ITF2357
CS-1443
ITF2357 (Givinostat)
Givinostat(HCl hydrate)
Givinostat Hydrochloride Hydrate
ITF2357 hydrochloride monohydrate
Gavinostat hydrochloride monohydrate
Givinostat (ITF2357) HCl monohydrate
Givinostat (hydrochloride monohydrate)
Givinostat (ITF2357) hydrochloride monohydrate
(6-((diethylamino)methyl)naphthalen-2-yl)methyl 4-(hydroxycarbamoyl)phenylcarbamate hydrochloride hydrate
N-[4-[(Hydroxyamino)carbonyl]phenyl]carbamic acid [6-[(diethylamino)methyl]-2-naphthalenyl]methyl ester hydrochloride hydrate | [EINECS(EC#)]
200-258-5 | [Molecular Formula]
C24H30ClN3O5 | [MDL Number]
MFCD18385007 | [MOL File]
732302-99-7.mol | [Molecular Weight]
475.965 |
| Chemical Properties | Back Directory | [storage temp. ]
-20°C | [solubility ]
≥23.8 mg/mL in DMSO; insoluble in EtOH; ≥2.9 mg/mL in H2O with gentle warming and ultrasonic | [form ]
powder | [color ]
white to beige | [InChIKey]
FKGKZBBDJSKCIS-UHFFFAOYSA-N | [SMILES]
C(OCC1=CC=C2C(=C1)C=CC(CN(CC)CC)=C2)(=O)NC1=CC=C(C(NO)=O)C=C1.[H]Cl.[H]O[H] | [CAS DataBase Reference]
732302-99-7 |
| Hazard Information | Back Directory | [Uses]
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. | [Biological Activity]
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). | [in vivo]
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[1]. | [target]
HDAC | [IC 50]
hHDAC3: 157 nM (IC50); hHDAC1: 198 nM (IC50); hHDAC11: 292 nM (IC50); hHDAC6: 315 nM (IC50); hHDAC2: 325 nM (IC50); hHDAC10: 340 nM (IC50); hHDAC7: 524 nM (IC50); hHDAC5: 532 nM (IC50); hHDAC9: 541 nM (IC50); hHDAC8: 854 nM (IC50); hHDAC4: 1059 nM (IC50); HD1-B: 7.5 nM (IC50); HD1-A: 16 nM (IC50); HD2: 10 nM (IC50) | [storage]
Store at -20°C |
|
| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
Sigma-Aldrich
|
| Telephone: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
|