Drug General Information
Drug ID
D0GH3Q
Former ID
DCL000852
Drug Name
ITF2357
Synonyms
Givinostat; Carbamic acid, N-(4-((hydroxyamino)carbonyl)phenyl)-, (6-((diethylamino)methyl)-2-naphthalenyl)methyl ester, hydrochloride (1:1)
Drug Type
Small molecular drug
Indication Myelofibrosis; Essential thrombocythemia; Polycythemia vera [ICD9: 238.71, 289.0, 289.83, 289.9, 776.4; ICD10:C94.4, D47.1, D47.3, D75.1, D75.2, D75.8, P61.1] Phase 2 [537520], [542513]
Company
Italfarmaco
Structure
Download
2D MOL

3D MOL

Formula
C24H27N3O4
InChI
InChI=1S/C24H27N3O4/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)
InChIKey
YALNUENQHAQXEA-UHFFFAOYSA-N
CAS Number
CAS 497833-27-9
PubChem Compound ID
PubChem Substance ID
Target and Pathway
Target(s) Histone deacetylase 1 Target Info Inhibitor [537114], [537520]
Tyrosine-protein kinase JAK2 Target Info Inhibitor [537114], [537520]
KEGG Pathway Cell cycle
Notch signaling pathway
Thyroid hormone signaling pathway
Huntington's disease
Amphetamine addiction
Alcoholism
Epstein-Barr virus infection
Pathways in cancer
Transcriptional misregulation in cancer
Viral carcinogenesis
MicroRNAs in cancer
Chronic myeloid leukemiahsa04062:Chemokine signaling pathway
PI3K-Akt signaling pathway
Signaling pathways regulating pluripotency of stem cells
Jak-STAT signaling pathway
Cholinergic synapse
Prolactin signaling pathway
Adipocytokine signaling pathway
Leishmaniasis
Toxoplasmosis
Tuberculosis
Measles
Influenza A
Herpes simplex infection
NetPath Pathway TCR Signaling Pathway
PANTHER Pathway Wnt signaling pathway
p53 pathwayP00031:Inflammation mediated by chemokine and cytokine signaling pathway
Interferon-gamma signaling pathway
JAK/STAT signaling pathway
PDGF signaling pathway
PI3 kinase pathway
CCKR signaling map ST
Pathway Interaction Database Regulation of nuclear SMAD2/3 signaling
Notch signaling pathway
E2F transcription factor network
Presenilin action in Notch and Wnt signaling
Signaling events mediated by HDAC Class I
Regulation of Telomerase
Glucocorticoid receptor regulatory network
Sumoylation by RanBP2 regulates transcriptional repression
Regulation of Androgen receptor activity
IL3-mediated signaling events
Validated nuclear estrogen receptor alpha network
Retinoic acid receptors-mediated signaling
Hedgehog signaling events mediated by Gli proteins
Regulation of nuclear beta catenin signaling and target gene transcription
Validated targets of C-MYC transcriptional repression
Regulation of retinoblastoma protein
Notch-mediated HES/HEY networkendothelinpathway:Endothelins
ErbB4 signaling events
GMCSF-mediated signaling events
IL4-mediated signaling events
IL27-mediated signaling events
Signaling events mediated by PTP1B
IL12-mediated signaling events
S1P3 pathway
SHP2 signaling
CXCR4-mediated signaling events
IL5-mediated signaling events
IFN-gamma pathway
ErbB2/ErbB3 signaling events
IL6-mediated signaling events
PDGFR-beta signaling pathway
IL23-mediated signaling events
Signaling events mediated by Stem cell factor receptor (c-Kit)
EPO signaling pathway
Notch-mediated HES/HEY network
Reactome G0 and Early G1
p75NTR negatively regulates cell cycle via SC1
Formation of the beta-catenin:TCF transactivating complex
NOTCH1 Intracellular Domain Regulates Transcription
SMAD2/SMAD3:SMAD4 heterotrimer regulates transcription
Constitutive Signaling by NOTCH1 PEST Domain Mutants
Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants
HDACs deacetylate histones
Deactivation of the beta-catenin transactivating complex
NoRC negatively regulates rRNA expression
RNA Polymerase I Transcription Initiation
Factors involved in megakaryocyte development and platelet productionR-HSA-1059683:Interleukin-6 signaling
MAPK3 (ERK1) activation
MAPK1 (ERK2) activation
GPVI-mediated activation cascade
Prolactin receptor signaling
RMTs methylate histone arginines
G beta:gamma signalling through PI3Kgamma
Interleukin-3, 5 and GM-CSF signaling
RAF activation
RAF/MAP kinase cascade
Interferon gamma signaling
Regulation of IFNG signaling
Interleukin receptor SHC signaling
Growth hormone receptor signaling
Factors involved in megakaryocyte development and platelet production
WikiPathways SIDS Susceptibility Pathways
Notch Signaling Pathway
TGF beta Signaling Pathway
IL-6 signaling pathway
Apoptosis-related network due to altered Notch3 in ovarian cancer
Transcriptional activity of SMAD2/SMAD3:SMAD4 heterotrimer
Notch Signaling Pathway
Retinoblastoma (RB) in Cancer
Neural Crest Differentiation
TWEAK Signaling Pathway
Integrated Breast Cancer Pathway
Signalling by NGF
RNA Polymerase I, RNA Polymerase III, and Mitochondrial Transcription
Mitotic G1-G1/S phases
Factors involved in megakaryocyte development and platelet production
Cell Cycle
Androgen receptor signaling pathwayWP733:Serotonin Receptor 2 and STAT3 Signaling
Type II interferon signaling (IFNG)
EPO Receptor Signaling
EGF/EGFR Signaling Pathway
IL-4 Signaling Pathway
Kit receptor signaling pathway
IL-3 Signaling Pathway
Mesodermal Commitment Pathway
Interleukin-2 signaling
Signaling by SCF-KIT
Prolactin receptor signaling
Growth hormone receptor signaling
JAK/STAT
BDNF signaling pathway
Oncostatin M Signaling Pathway
Interleukin-11 Signaling Pathway
AGE/RAGE pathway
TSLP Signaling Pathway
IL17 signaling pathway
Leptin signaling pathway
TSH signaling pathway
Interleukin-3, 5 and GM-CSF signaling
Interferon gamma signaling
IL-5 Signaling Pathway
References
Ref 537520Emerging drugs for the therapy of primary and post essential thrombocythemia, post polycythemia vera myelofibrosis. Expert Opin Emerg Drugs. 2009 Jun 24.
Ref 542513(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7490).
Ref 537114Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
Ref 537520Emerging drugs for the therapy of primary and post essential thrombocythemia, post polycythemia vera myelofibrosis. Expert Opin Emerg Drugs. 2009 Jun 24.

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